Drug, bio-affecting and body treating compositions inventions 06/06

20060142179 - 4-aminopyridine and a pharmaceutical composition for treatment of neuronal disorders: where R1 and R2 are each independently H or a C1-C4 hydrocarbon; R3 is H, and R4 is a moiety capable of crossing the blood brain barrier selected from the group consisting of: an amino acid, a peptide, transferrin, gluconate, lactate, citrate, malate, fumarate, benzoate, salicylate, pyruvate and propionate. The...

20060142180 - Cholinergic modulation of microglial activation via alpha-7 nicotinic receptors: Novel therapeutic targets in the treatment of neuroimmunological and neurodegenerative disorders. Accordingly, methods of treating a neurodegenerative disorder in a patient, as well as inhibiting the release of a proinflammatory cytokine, comprising the step of contacting a target cell with a therapeutically effective amount of a cholinergic agonist, such as...

20060142178 - Method of treating cancer: The present invention is directed to a method of treating cancer which comprises administration of a compound which selectively inhibits the activity of one or two of the isoforms of Akt, a serine/threonine protein kinase. The invention is particularly directed to the method wherein the compound is dependent on the...

20060142181 - Compound and method of treating neurogenic conditions using non-steroidal anti-inflammatory drug complexes: M is a metal ion Ca(II), Mg(II), Cu(II) or Ni(II); n is an integer 1 or 2; R is BBB peptide, transferrin, membrane transporter peptide, TAT peptide, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin,...

20060142182 - Piracetam and piracetam analog conjugate and a pharmaceutical composition for treatment of neuronal disorders: where R1 is H, C1-C4 alkyl and OH; R2 in is H, C1-C4 alkyl and OH; R3 is H and C1-C4 alkyl; R4 is H and C1-C4 alkyl; n is an integer between 0 and 2 inclusive; R5 is a nullity, NHR7C(O)—, C6H4—, C6H4—O—; R7 is C2-C6 alkyl; and R6...

20060142183 - Method and composition for treatment and/or prevention of antibiotic-resistant microorganism infections: The present invention related to a new composition, use and method to improve the cure of infections caused by antibiotic resistant microbial pathogens, in particular beta-lactam resistant microorganisms. Lactoferrin (LF) or Lactoferricin (LFC) can be administrated alone or in combination with antibiotic to affect growth, physiology and morphology of targeted...

20060142184 - Protein based oral lubricant: The present invention relates to formulations containing phosphoprotein, designed for use as oral lubricant or as artificial saliva, methods of using the formulations and processes for the preparation of the formulations....

20060142186 - Leuprolide acetate and acetylcholinesterase inhibitors or nmda receptor antagonists for the treatment of alzheimer's disease: Methods of treating, mitigating, slowing the progression of, or preventing Alzheimer's Disease include administration of gonadotropin-releasing hormone analogues in combination with acetylcholinesterase inhibitors and/or N-methyl-D-aspartate receptor antagonists....

20060142187 - Methods for modulating cell-to-cell adhesion using an agonist of c1inh-type protein activity: The present invention is based, at least in part, on the discovery that plasma C1INH contains a sialyl Lewisx related moiety on its N-glycan and is capable of binding selectin molecules. The invention provides methods for modulating cell-to-cell adhesion or cell migration comprising contacting a cell with a C1INH-type protein...

20060142185 - Use of lupin conglutin for the treatment of type ii diabetes: A method for the use of lupin conglutin gamma or of proteins showing homology higher than 50% with lupin conglutin gamma, for the preparation of a medicament, food supplements or foods for the treatment of type II diabetes, pharmaceutical and nutritional compositions containing lupin conglutin gamma, and the use of...

20060142199 - Cd-44 like protein: The present invention concerns a novel CD44-like protein receptor. In particular, isolated nucleic acid molecules are provided encoding the CD44-like protein. CD44-like polypeptides are also provided, as are screening methods for identifying agonists and antagonists capable of enhancing or inhibiting CD44-like protein-mediated signaling. The invention further concerns therapeutic methods for...

20060142198 - Compositions for treating wounds and processes for their preparation: The present invention provides a process for obtaining growth factors by treating a growth factor starting material to release growth factors from the growth factor starting material and recovering growth factors from the treated growth factor starting material. The growth factor obtained can be used in compositions to treat humans....

20060142200 - Compounds and methods for lowering cholesterol levels without inducing hypertrigylceridemia: This invention provides methods of lowering cholesterol, delaying the onset of atherosclerosis, or treating atherosclerosis in a mammal without inducing hypertriglyceridemia. These methods involve administrating to or expressing in a mammal, an apoE polypeptide or nucleic acid that, when administered to or expressed in a mammal, lowers the total serum...

20060142189 - Methods and agents for treating axonal damage, inhibition of neurotransmitter release and pain transmission, and blocking calcium influx in neurons: The present invention pertains to methods to promote outgrowth of, or extension across a substrate of, neuronal cells by inhibiting the interaction between the cytoplasmic tail of the L1-CAM cell surface adhesion molecule and the cytoskeletal protein ankyrin. The invention also pertains to a method to treat diseases characterized by...

20060142194 - Methods and compounds for treating brain amyloidosis: The present invention discloses the use of (i) a fragment of the amyloid precursor protein (APP); or, (ii) a derivative of (i); or, (iii) a functional mimetic of (i) or (ii), in the preparation of a medicament for modulating CNS levels and/or activity of a member of the neprilysin family....

20060142188 - Monkey alpha-7 nicotinic acetylcholine receptor and methods of use thereof: Monkey alpha-7 neuronal nicotinic acetylcholine receptor polypeptides, as well as the DNA (RNA) encoding such polypeptides, are disclosed. Also disclosed are methods for utilizing such polypeptides in diagnostic assays for identifying mutations in nucleic acid sequences encoding the polypeptides of the present invention, for detecting altered levels of the polypeptide...

20060142195 - Non-neurotoxic plasminogen activating factors for treating of stroke: The invention pertains to the use and production of non-neurotoxic plasminogen activating factors e.g. of Desmodus rotundus (DSPA) for the therapeutic treatment of stroke in humans in order to provide a new therapeutic concept for treating stroke in humans....

20060142193 - Selective inhibition of rock1 in cardiac therapy: The present invention is directed to the treatment and/or prevention of disease as it relates to Rho kinase. In specific embodiments, disease is treated and/or prevented through the administration of an agent that selectively inhibits ROCK1. In specific embodiments, it inhibits ROCK1 and not ROCK2. In other specific embodiments, the...

20060142192 - Soluble zcytor21, anti-zcytor21 antibodies and binding partners and methods of using in inflammation: The present invention relates ZcytoR21 antagonists, such as soluble receptors and anti-ZcytoR21 antibodies, that are useful in blocking, inhibiting, reducing, antagonizing or neutralizing the activity of IL-17C. IL-17C is a cytokine that is involved in inflammatory processes and human disease. ZcytoR21 is a receptor for IL-17C. The present invention includes...

20060142190 - Synthetic peptide, inhibitor to dna viruses: The present invention relates to the identification of the active domain of Herpoxin, a DNA virus-inhibiting-protein which was isolated from cobra venom in U.S. Pat. No. 5,648,339 and has a molecular weight of 13.5 kDa We have isolated a fragment of Herpoxin which contains the active domain and which we...

20060142197 - Tnf receptor and steroid hormone in a combined therapy: The present invention relates to the use of a TNF Receptor together with a steroid hormone to produce a pharmaceutical composition for the treatment of lethal bacterial and viral infections as well as autoimmune and inflammatory diseases. It also relates to said pharmaceutical compositions for the simultaneous separate or sequential...

20060142196 - Uses of gdnf and gdnf receptor: GDNFRα, GDNFRα extracellular domain (ECD), GDNFRα variants, chimeric GDNFRα (e.g., GDNFRα immunoadhesin), and antibodies which bind thereto (including agonist and neutralizing antibodies) are disclosed. Various uses for these molecules are described, including methods to modulate cell activity and survival by response to GDNFRα-ligands, for example GDNF, by providing GDNFRα to...

20060142191 - Viral complement control proteins for eye disorders: The present invention provides compositions and methods for treating and/or preventing age related macular degeneration and other conditions involving macular degeneration or choroidal neovascularization. Certain of the compositions comprise a poxvirus complement control protein or a complement binding fragment or variant thereof. Other compositions comprise a poxvirus complement control protein...

20060142201 - Novel x-conotoxin peptides (-1): An isolated, synthetic or recombinant χ-conotoxin peptide comprising the following sequence of amino acids: Xaa1 Xaa2 Gly Val Cys Cys Gly Tyr Lys Leu Cys His Pro Cys SEQ ID NO. 3 where Xaa1 is a N-terminal Xaa1 is a N-terminal pyroglutamate (pGlu) or D-pyroglutamate (DpGlu) residue; and Xaa2 is...

20060142202 - Compositions and methods for targeted delivery of immune response modifiers: The present invention provides immunomodulatory compositions include an immune response modifier moiety coupled to a targeting moiety. In another aspect, the invention provides methods of providing targeted delivery of an IRM, generating a localized immune response, and treating a condition in a subject. Generally, the methods include administering to the...

20060142203 - Compositions and methods comprising protein activated receptor antagonists: Compositions and methods comprising protein activated receptor antagonists are provided More particularly, the present invention relates to the use of proteins, peptides and biomolecules that bind to protein activated receptor 2, and inhibit the processes associated with the activation of that receptor. More specifically, the present invention provides novel compositions...

20060142205 - Compositions capable of reducing elevated blood urea concentration: The invention includes a method of reducing urea concentration in a subject's serum. Such a method comprises administering to the subject (e.g., a mammal such as a human) a composition comprising an oligopeptide (or oligopeptides) having activity in reducing urea concentration in the subject's serum as determined by a mouse...

20060142204 - Pyrrolidine derivatives for use in treating heaptitis c virus infection: The present invention relates to novel hepatitis C virus (“HCV”) protease inhibitors or other flavivirus protease inhibitors having the general structure (I) or (II), pharmaceutical compositions containing one or more such inhibitors, methods for preparing such inhibitors, uses of these compounds to treat hepatitis C and related disorders together with...

20060142207 - Compositions and methods for treating cancer: Methods and compositions are provided for the treatment of cancer that take advantage of the increased uptake of glucose-anti-neoplastic agent conjugates in cancer cells relative to normal cells....

20060142208 - Compounds and methods for the treatment of airway diseases and for the delivery of airway drugs: Chronic obstructive airway diseases are treated by administering an osmotically active compound such as a salt, sugar, sugar alcohol, or organic osmolyte to the afflicted airway surface. The compound may be administered as a liquid or dry powder aerosol formulation. Diseases that can be treated by the method include cystic...

20060142209 - Glucopyranosyloxypyrazole derivatives and medicinal use thereof: while the other represents a lower alkyl group or a halo(lower alkyl) group; R1 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkenyl group, a cyclic lower alkyl group, etc.; R2 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkoxy group, a...

20060142206 - Novel difluorinated gem compounds, preparation methods thereof and applications of same: This invention relates to a mini-type electric vehicle, which is mainly used for individual person or traffic in a certain field. It includes frame, seat, front & rear wheel, driving device, battery, steering system and front wheel suspension device. A casing, where the battery is placed on, protrudes forward at...

20060142210 - Glucopyranosyl-substituted benzene derivatives, medicaments containing such compounds, their use and process for their manufacture: Glucopyranosyl-substituted benzene derivatives defined according to claim 1, including the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders....

20060142211 - Chromones and chromone derivatives and uses thereof: The present invention relates to chromones, novel chromone derivatives, and pharmaceutical formulations containing the same and methods of use thereof. Uses of the present invention include, but are not limited to, use for the prevention and treatment of septic shock, organ injury and other disorders. The compounds described herein can...

20060142213 - Methods for treating neuropathological states and neurogenic inflammatory states and methods for identifying compounds useful therein: The present invention provides methods for treating neuropathological states and neurogenic inflammatory states in a subject. The present invention also provides methods for identifying compounds that can be used to treat such states. Preferably, the compounds alter the distribution of NMDA glutamate receptor NR1 subunit in cells, and/or alter the...

20060142212 - Nutrient pharmaceutical formulation comprising polyphenols and use in treatment of cancer: A nutrient pharmaceutical formulation composition useful for treating cancer comprising ascorbic acid, L-lysine, L-proline and at least one polyphenol compound selected from the group consisting of epigallocatechin gallate, epicatechin gallate, epigallocatechin, epicatechin, catechin and the use of the composition in treating cancer and other tumors are provided. A nutrient pharmaceutical...

20060142214 - 3,6-bicyclolides: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the...

20060142216 - Parasiticidal composition: An anti-parasiticidal composition presented as a topical “pour-on” product for treating animals infected by parasites which are known to be susceptible to salicylanilides, especially closantel, alone or together with at least one other anti parasitic compound of the avermectin or milbemycin type and offers enhanced bioavailability of the salicylanilide by...

20060142215 - Tetracyclic bicyclolides: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the...

20060142217 - Carbohydrate based anti-bacterials: A method of inhibiting bacterial growth by contacting a bacteria with at least one disaccharide compound of General Formula I,...

20060142227 - Amphiphylic peptide-pna conjugates for the delivery of pna through the blood brain barrier: The invention provides molecules comprising a nucleic acid, a hydrophobic moiety and a positively charge moiety, useful in the delivery of a nucleic acid sequence across a cellular membrane. The invention further relates to the use of these molecules for the delivery of a nucleic acid sequence to the brain...

20060142236 - Antisense oligonucleotide modulation of raf gene expression: Oligonucleotides are provided which are targeted to nucleic acids encoding human raf and capable of inhibiting raf expression. The oligonucleotides may have chemical modifications at one or more positions and may be chimeric oligonucleotides. Methods of inhibiting the expression of human raf using oligonucleotides of the invention are also provided....

20060142231 - Dna damage repair inhibitors for treatment of cancer: DNA Damage Repair Inhibitors for Treatment of Cancer The present invention relates to the recognition that inhibition of the base excision repair pathway is selectively lethal in cells which are deficient in HR dependent DNA DSB repair. Methods and means relating to the treatment of cancers which are deficient in...

20060142230 - Double-stranded ribonucleic acid molecules having ribothymidine: The invention relates to a double-stranded RNA (dsRNA) molecule comprising between about 15 base pairs and about 40 base pairs, wherein at least one ribonucleotide of the dsRNA is a 5′-methyl-pyrimidine, and a method of using such modified dsRNA molecule to increase stability of RNA when in contact with a...

20060142233 - Gene expression and genetic changes implicated in alcoholism: Polynucleotides, polypeptides, kits and methods are provided related to regulated genes characteristic of alcoholism....

20060142234 - Injectable non-aqueous suspension: The present invention relates generally to compositions and methods for administering a biologically active agent, and more specifically to injectable non-aqueous suspensions....

20060142218 - Method of controlling telomere length: A method of controlling telomere length wherein the method comprises introducing into a cell a DNA encoding Mre11 protein or a DNA encoding a protein comprising Mre11 protein wherein a part of the nuclease domain, the C-terminal domain or the whole thereof is modified or deleted....

20060142235 - Method of reducing and treating uvb-induced immunosuppression: Methods of preventing and/or treating UV-induced immunosuppression by administration of immune response modifier compounds are disclosed herein. Suitable immune response modifier compounds include agonists of one or more TLRs....

20060142228 - Methods and compositions concerning sirna's as mediators of rna interference: The present invention concerns an isolated siRNA of from about 5 to about 20 nucleotides that mediates RNA interference. Also disclosed are methods of reducing expression of a target gene in a cell comprising obtaining at least one siRNA of 5, 6, 7, 8, 9, 10, 11, 12, 13, 14,...

20060142223 - Methods for xenotopic expression of nucleus-encoded plant and protist peptides and uses thereof: The present invention provides a method for introducing a functional peptide encoded by a plant or protist nucleic acid sequence into a mitochondrion of a mammalian cell, and a pharmaceutical composition comprising the nucleic acid sequence. The present invention also provides a method for correcting a phenotypic deficiency in a...

20060142229 - Methods of treating lupus based on antibody affinity and screening methods and compositions for use thereof: The invention provides methods identifying individuals suitable for treatment for lupus and methods of monitoring treatment, based on measuring antibody affinities, as well as of treating lupus based on measuring antibody affinities. The treatment entails administration of a conjugate comprising a non-immunogenic valency platform molecule and at least two double...

20060142224 - Modulation of immunostimulatory activity of immunostimulatory oligonucleotide analogs by positional chemical changes: The invention relates to the therapeutic use of oligonucleotides or oligonucleotide analogs as immunostimulatory agents in immunotherapy applications. The invention provides methods for enhancing the immune response caused by immunostimulatory oligonucleotide compounds....

20060142222 - Novel gene relating to fibrotic conditions: This discloses a novel human or rat polypeptide useful in improving and/or preventing organ fibrosis and a polynucleotide encoding the aforementioned polypeptide, an expression vector containing the aforementioned polynucleotide, and a cell transfected with the aforementioned expression vector. The aforementioned polynucleotide shows a remarkable decrease in the expression dose in...

20060142232 - Oligomeric compositions and methods: The activated oligomer compounds described herein are capable of forming bio-reversible covalent bonds with plasma proteins, in particular with human serum albumin. The plasma protein-oligomer complexes of the present invention exhibit enhanced cellular entry and significantly enhanced serum half-life....

20060142219 - Pharmaceutical compositions comprising an hiv envelope protein and cd4: Pharmaceutical composition for treating/preventing HIV comprising (i) a polynucleotide encoding HIV envelope protein and (ii) a polynucleotide encoding CD4 receptor protein or; (i) a polynucleotide encoding HIV envelope protein and (ii) a CD4 receptor protein or; a fixed cell expressing an HIV envelope protein complexed with a CD4 receptor protein....

20060142220 - Protein modification: The present invention relates to a method for changing the half-life of a glycosylated compound by the modification of its O-linked carbohydrates. This modification is preferably carried out enzymatically and aimed at extending the half-life of the compound. Both in vivo and in vitro modification protocols may be used....

20060142226 - Rna interference mediated inhibition of cholesteryl ester transfer protein (cetp) gene expression using short interfering nucleic acid (sina): This invention relates to compounds, compositions, and methods useful for modulating cholesteryl ester transfer protein (CETP) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of CETP gene...

20060142225 - Rna interference mediated inhibition of cyclin dependent kinase-2 (cdk2) gene expression using short interfering nucleic acid (sina): This invention relates to compounds, compositions, and methods useful for modulating cyclin dependent kinase-2 (CDK2) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of CDK2 gene expression...

20060142221 - Vaccine: The invention relates to polynucleotides for DNA vaccination which polynucleotides encode an HIV envelope protein or fragment or immunogenic derivative fused to an additional HIV protein selected from a non-structural protein or capsid protein or fragment or immunogenic derivative thereof. Preferably the HIV envelope molecule is gp120 and preferred fusions...

20060142237 - Method for treatment of multiple sclerosis: Use of an A3 adenosine receptor agonist in the preparation of a pharmaceutical composition for the treatment of an individual suffering from multiple sclerosis. The composition is preferably orally administered. Also disclosed is a pharmaceutical composition for the treatment of multiple sclerosis that comprises an effective amount of an A3...

20060142238 - Chemical compounds: Phosphoramidate derivatives of nucleotides and their use in the treatment of cancer are described. The base moieties of, for example, each of deoxyuridine, cytarabine, gemcitabine and citidine may be substituted at the 5-position. The phosphoramidate moiety has attached to the P atom an aryl-O moiety and an α-amino acid moiety....

20060142240 - Mutagenic nucleoside analogs for the treatment of viral disease: The present invention relates to methods of treating viral disease using mutagenic nucleoside analogs....

20060142239 - Potassium or sodium salt of (-)-2-(4-hydroxyphenyl)ethyl!-thio-3-'4-{4-'(methzlsulfonzl)oxy !phenoxy}phenyl!propanoic acid and their use in medicine: A method for the production of a vascular damaging effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer involving a solid tumour, such as colorectal cancer, which comprises one of: the administration of...

20060142241 - Methods and compositions for reducing neurodegeneration in amyotrophic lateral sclerosis: The present disclosure is related to clear aqueous solutions of one or more bile acids and either an aqueous soluble starch conversion product or a non-starch polysaccharide. Solutions of the disclosure may be administered to a subject in conjunction with a pharmaceutical compound having a therapeutic effect in subjects with...

20060142242 - Starch derivatives and other derivatives, production processes therefor, and wound healing applications therefor: Novel phosphate starch derivatives are useful in wound healing. Novel phosphorylated cottons are useful in wound healing. Silver-derivatized wound care products are provided which survive washing and remain part of the wound care product. Silver-derivatized wound care products are provided that have favorable elastase-sequestering activity while advantageously appearing white-colored, without...

20060142244 - Geranyl compounds: v

20060142243 - Use of n-acetyl-d-glucosamine for preparing medicines for urogenital tract infection's treatment and prevention: The present invention discloses a use of N-acetyl-D-glucosamine in the manufacture of a medicament for treatment of urogenital tract infection. N-acetyl-D-glucosamine exhibits a function of suppressing the transplantation of exotic microorganisms and promoting the repair of topical skin tissue, and the formulation comprising it as a main active component is...

20060142246 - 2-methylene-19,26,27-trinor-(20s)-1alpha-hydroxyvitamin d3 and its uses: This invention discloses 2-methylene-19,26,27-trinor-(20S)-vitamin D analogs, and specifically 2-methylene-19,26,27-trinor-(20S)-1α-hydroxyvitamin D3 and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis...

20060142245 - Inhibitors of hedgehog signaling pathways, compositions and uses related thereto: The present invention makes availables assays and reagents inhibiting paracrine and/or autocrine signals produced by a hedgehog protein or aberrant activation of a hedgehog signal transduction pathway, e.g., which involve the use of a steroidal alkaloid or other small molecule....

20060142247 - Tricyclic heterocycles: e

20060142248 - Xanthurenic acid derivative pharmaceutical compositions and methods related thereto: R4 and R8 are independently H, (═O); hydroxy; or optionally substituted saccharide, aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or —P(O)(ORa)(ORb) or —NRaRb, where Ra and Rb are independently H, or optionally substituted aliphatic, cycloalkyl or heterocycloalkyl, aryl or heteroaryl; or a prodrug or pharmaceutically acceptable salt thereof; and a pharmaceutically...

20060142249 - Ophthalmic use: The present invention relates to the use of a GABA-C-antagonist in the preparation of a medicament for the treatment of myopia....

20060142250 - Protein tyrosine phosphatase inhibitors and methods of use thereof: The present invention provides compounds of Formula (I) and Formula (II) that are useful for modulating the biological activity of the protein tyrosine phosphatase-1b (PTP1B) enzyme. Compounds of this invention can be used to treat diseases and/or conditions in which the PTP1B enzyme is a factor. Such diseases and/or conditions...

20060142251 - Anti-microbial agents derived from methionine sulfoximine analogues: Novel antimicrobial compositions containing analogues of L-methionine-SR-sulfoximine (MSO) that are effective in treating intracellular pathogen infections are provided. Specifically, the compositions provided are MSO analogues having superior antimicrobial activity with significantly less toxicity as compared to MSO. These MSO analogues are suitable for use in treating infection in animals including...

20060142252 - Tubulin binding agents and corresponding prodrug constructs: A diverse set of tubulin binding agents have been discovered which are structurally characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl-aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare...

20060142253 - Methods for treating neoplastic, angiogenic, vascular, fibroblastic, and/or immunosuppressive irregularities of the eye and/or joint via administration of combretastatin based medicaments, and iontophoretic devices for delivering combretastatin based medi: A method for treating neoplastic, angiogenic, vascular, fibroblastic, immunosuppressive, infectious, metabolic, and/or constitutional irregularities of the eye and/or joint of a living subject, comprising the steps of: providing a living subject, wherein the living subject includes an affected ocular and/or joint area having a neoplastic, angiogenic, fibroblastic, immunosuppressive, infectious, metabolic,...

20060142254 - Antipyretic preparation containing xylitol: The invention relates to an antipyretic preparation intended to be administered by any means other than orally, characterized in that it comprises xylitol, and more particularly to an antipyretic preparation characterized in that it consists of an antipyretic and a synergistic amount of xylitol. The invention also relates to the...

20060142255 - Hypocholesteremic preparations containing phytostenolesters of conjugated fatty acids, and methods of reducing serum cholesterol levels using the same: A hypocholesteremic preparation containing at least one phytostenol ester of a conjugated fatty acid having from about 6 to about 24 carbon atoms is disclosed. Methods of reducing serum cholesterol content in a mammal via administration of hypocholesteremic preparations described herein are also disclosed....

20060142256 - Composition comprising a combination of an aromatase inhibitor, a progestin and an oestrogen and its use for the treatment of endometricosis: The invention relates to a method of treating endometriosis using a combination of an aromatase inhibitor, a progestin and an oestrogen. The invention also relates to pharmaceutical formulations comprising said combination....

20060142257 - Male contraceptive formulation comprising norethisterone: A formulation for male contraception comprising a progestin possessing both estrogenic and androgenic properties is remarkably effective for spermatogenesis suppression in males. The progestin Norethisterone (NET), particularly its derivatives Norethisterone acetate and Norethisterone enanthate in sufficient doses induce oligozoospermia or azoospermia in males. Formulations further comprising an androgen, such as...

20060142258 - Estrogen replacement therapy: This invention relates to methods and pharmaceutical compositions for providing estrogen replacement therapy in penmenopausal, menopausal, and postmenopausal women through the continuous administration of conjugated estrogens....

20060142259 - Compounds, pharmaceutical compositions and methods for inhibiting hiv infectivity: Compounds that possess anti-infective activity are described. Methods of using these compounds for the treatment or prevention of infectious diseases such as acquired immunodeficiency syndrome (AIDS) are also described. The compounds inhibit HIV infectivity and do not exhibit significant cytotoxicity in HIV producing cells....

20060142260 - Water-soluble anionic bacteriochlorophyll derivatives and their uses: The invention provides anionic water-soluble tetracyclic and pentacyclic bacteriochlorophyll derivatives (Bchls) containing at least one, preferably two or three, negatively charged groups and/or acidic groups that are converted to negatively charged groups at the physiological pH, preferably Bchls having a group COO<−>, COS<−>, SO3<−>, PO3<2−>, COOH, COSH, SO3H, and/or PO3H2...

20060142261 - Crystalline anhydrous cefdinir and crystalline cefdinir hydrates: A novel crystalline cefdinir anhydrate and novel crystalline cefdinir hydrates, ways to make them and use them, compositions comprising them and made with them, and methods of treatment using them are disclosed....

20060142262 - Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto: n

20060142264 - Novel amide derivatives: Compounds of structural Formula (I) where A is a lipophilic group including an aliphatic bridging group, B is a lipophilic group, D is a group having at least one amino or substituted amino group and R is hydrogen, alkyl or cycloalkyl, and pharmaceutically acceptable salts and individual isomers thereof, which...

20060142265 - Compositions comprising multiple bioactive agents, and methods of using the same: In part, the present invention is directed to compositions comprising a FabI inhibitor and at least one other bioactive agent. In another part, the present invention is directed to antibacterial compositions comprising a compound of formulas I-III and at least one other antibacterial agent....

20060142263 - New substituted pyrrolidinones, their manufacture and their use as medicaments:

20060142266 - Compounds and their uses: This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP....

20060142268 - 1,4,5,6-tetrahydroimidazo[4,5-d]benzazepine derivative or salt thereof: To provide a compound having a superior arginine vasopressin antagonism. A novel 1,4,5,6-tetrahydroimidazo[4,5-d]benzazepine derivative or a pharmaceutically acceptable salt thereof....

20060142267 - Dihydro-dibenzo[b,e]oxepine based selective estrogen receptor modulators, compositions and methods: The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2(C2-C6 alkyl); R0, R2 and R3 are each independently —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), —OSO2(C2-C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino,...

20060142269 - New compounds: e

20060142270 - Preventing or treating agent for glaucoma: A preventing or treating agent for glaucoma is provided. This drug has a strong action of reducing intraocular pressure such that the intraocular pressure can be reduced even from the normal intraocular pressure. More specifically, a prophylactic or therapeutic agent for glaucoma, a preventing or treating agent for ocular hypertension,...

20060142271 - Novel lapacho compounds and methods of use thereof: The invention provides new synthetic lapacho derivatives as well as methods of use thereof. These compounds can be used in pharmaceutical compositions for the treatment or prevention of cell proliferation disorders. These compounds can also be used in the treatment or prevention of psoriasis or cancer or precancerous conditions....

20060142272 - Pyrrolo [2, 1-c] [1, 4] benzodiazepine-anthraquinone conjugates useful as antitumour agents: e

20060142275 - Prenyl transferase inhibitors:

20060142274 - Use of selected cgrp antagonists for combating menopausal hot flushes: The invention relates to the use of selected CGRP antagonists, the physiologically acceptable salts thereof or the hydrates of the hydrates of the salts thereof for combating menopausal hot flushes....

20060142273 - Use of selected cgrp-antagonists in combination with other antimigraine drugs for the treatment of migraine: The present invention relates to a process for the treatment or prevention of indications which are selected from among the group comprising headaches, migraine and cluster headaches, this process comprising the joint administration of a therapeutically effective amount of a selected CGRP antagonist (A), a physiologically acceptable salt thereof or...

20060142276 - Therapeutic agent for senile dementia: e

20060142278 - Mitotic kinesin inhibitors: The present invention relates to bicyclic dihydrepyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals....

20060142277 - Substituted aralkyl derivatives: The present invention relates to novel substituted aralkyl derivatives of the general formula (I) and (IIIa), their derivatives, their analogs, their tautomeric forms, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, pharmaceutical compositions containing them, use of these compounds in medicine and the intermediates involved in their preparation....

20060142279 - Treatment of latent tuberculosis: a pharmaceutically acceptable salt, a quaternary amine, a N-oxide, a tautomeric form or a stereochemically isomeric form thereof wherein R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2, 3 or 4; R2 is hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy,...

20060142280 - Cyclothiocarbamate derivatives as progesterone receptor modulators: p

20060142281 - Indolinone derivatives:

20060142282 - Combination effective for the treatment of impotence: This invention relates to the treatment of erectile dysfunction with a combination of (1) a compound selected from α-adrenergic receptor antagonists, and (2) a compound selected from agents which elevate cGMP levels. Sildenafil or a pharmaceutically acceptable salt thereof is preferred as the cGMP PDE elevator. Also included are compositions...

20060142283 - Crystalline form iv of linezolid: The present invention provides a novel crystalline form of linezolid referred to herein as Form IV as well as methods for the preparation and use of Form IV. The present invention provides pharmaceutical compositions that comprise therapeutically effective amounts of Form IV that can be used to treat patients suffering...

20060142284 - Novel compounds: The present invention relates to anilinopyrazole derivatives, methods for the preparation of such anilinopyrazoles, and use of such anilinopyrazoles in the treatment of certain diseases or conditions. In particular, the present invention relates to a nilinopyrazole derivatives useful as CDK2 inhibitors and use of the anilinopyrazoles in the treatment of...

20060142285 - Pharmaceutical composition comprising n-aryl n' morpholino/piperidino thiocarbamide derivatives for treating and preventing diabetes, diabetic complications, insulin resistance and insulin resistance syndrome: e

20060142286 - Cyclic hydroxylamine as psychoactive compounds: A compound of formula (I): in which X represents O or CH2; R3 and R4 each independently represent hydrogen or C1-6 alkyl; p represent 0 or 1; and R represents a five- or six-membered saturated or unsaturated ring selected from: formula (II), (III) and (IV); or R represents a five-...

20060142288 - Combinations and methods for headaches: The present invention provides pharmaceutical agents for preventing headaches, especially headaches associated with migraine, tension headaches, and chronic daily headaches. The prophylactic treatments in accordance with the present invention can reduce the frequency of headaches, such as migraine attacks, as well as reducing their severity and duration when they do...

20060142290 - Compositions for affecting weight loss: Disclosed are compositions for affecting weight loss comprising a first compound and a second compound, where the first compound is an opioid antagonist and the second compound causes increased agonism of a melanocortin 3 receptor (MC3-R) or a melanocortin 4 receptor (MC4-R) compared to normal physiological conditions. Also disclosed are...

20060142289 - Method of treating migraine headaches: Methods and compositions for treating humans suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or a condition where inhibiting reuptake of norepinephrine is a benefit are disclosed. The compositions comprise a compound having a pharmacological selectivity of serotonin (Ki)/norepinephrine (Ki) of at least about...

20060142287 - Use of a combination of dppe with other chemotherapeutic agents for the treatment of breast cancer: An improved adjuvant treatment of stage I or II breast cancer in which patients are administered a chemotherapeutic agent active in breast cancer is provided in which a diphenyl compound which is a potent antagonist of histamine binding at the intracellular histamine receptor is initially administered prior to administration of...

20060142291 - Use of formaldehyde and formaldehyde-releasing compounds in a composition for controlling mycobacteria: The invention relates to the use of a bactericide selected from formaldehyde and formaldehyde-releasing compounds in a composition for controlling mycobacteria, for example in a cooling lubricant....

20060142292 - Water-soluble phenylpyridazine derivative and medicine containing the same: Wherein, R1, R2, R3, X, Y, Z and n have the same meaning as defined in the specification; or a salt thereof, or a medicine containing the compound. The present invention provides water-soluble phenylpyridazine derivatives and medicines containing them, which have excellent inhibitory activity against interleukin-β production, high water solubility...

20060142293 - Phthalazinone derivatives: e

20060142294 - Novel compounds for treatment of cancer and disorders associated with angiogenesis function: Novel compounds for treatment of cancer and disorders associated with angiogenesis function. Also disclosed are a method of preparing the compounds, pharmaceutical compositions and packaged products containing the compounds, a method of using these molecules to treat cancer (e.g., leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian...

20060142295 - Method of treating cancer with quinolone carboxylic acid derivatives: This invention relates to a method of treating a hyper-proliferative disorder comprising the administration of an effective amount of a compound of Formula (I) to a patient in need thereof....

20060142296 - 4(phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain or gastrointestinal disorders: Compounds of general formula:[Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, and R3 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain....

20060142297 - Combination product of inhibitor of the src family of non-recetpor tyrosine kinases and gemcitabine: The invention concerns a combination comprising an inhibitor of Src kinase and the cytotoxic agent gemcitabine, a pharmaceutical composition comprising such a combination and its use in the treatment or prophylaxis of cancer, particularly of pancreatic cancer....

20060142298 - Aminium salts of 1,2,3-triazoles as prodrugs of drugs including antiviral agents: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with new aminium salts of 1,2,3-triazoles which can be used as prodrugs to improve the solubility or pharmaceutical properties of 1,2,3-triazole containing compounds. More particularly, the present disclosure...

20060142299 - Crystalline aripiprazole solvates: Alcoholates of aripiprazole are useful as pharmaceuticals and/or as intermediates in making aripiprazole Form A or Form B....

20060142300 - Anhydrous crystalline forms of i and ii of 1-cyclopropyl-6-fluoro-8-methoxy-7-(3-methyl-1- piperazinyl) 4-oxo-1, 4-dihydroquinoline-3-carboxylic acid (gatifloxacin): The present invention relates to the novel anhydrous crystalline forms I and II of 1-cyclopropyl-6-fluoro-8-methoxy-7-(3-methyl-1-piperazinyl)4-oxo-1, 4-dihydroquinoline-3-carboxylic acid (gatifloxacin) which can be depicted as Formula (I). The present invention also relates to methods of making the anhydrous Forms I and II of Gatifloxacin, use of the forms and methods for preparing...

20060142302 - Chemical compounds: R6 represents C1-4 alkyl, C3-7 cycloalkyl, NH(C1-4 alkyl) or N(C1-4alkyl)2; m is zero or an integer from 1 to 3; n is an integer from 1 to 3; or a pharmaceutically acceptable salt or solvate thereof; compositions containing the same, processes for their preparation and methods for their use in...

20060142301 - Substituted 1-benzyl-4-substituted piperazine analogues: Such compounds may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are...

20060142303 - Oxy substituted chalcones as antihyperglycemic and antidyslipidemic agents: The present invention provides novel substituted chalcone derivatives which exhibit anti-hyperglycemic and anti-dyslipedemic activity. The invention also provides a method for treating type II diabetes and associated hyperlipidemic conditions in a mammal by administering the compounds of the present invention and compositions containing these derivatives....

20060142304 - Method for treating or preventing pruritic and neurogenic skin disorders: This invention relates to methods of treatments, compositions, and kits for providing rapid relief to the user for pruritic and neurogenic skin disorders. The invention also provides methods of treatments, compositions, and kits for preventing such conditions....

20060142305 - Hydroxyamidine and hydroxyguanidine compounds as urokinase inhibitors: The present invention relates to novel compounds for inhibiting the urokinase plasminogen activator (uPA), which have high bioavailability and oral administerability, and also to the use thereof as therapeutic active compounds for the treatment of urokinase- or/and urokinase receptor-associated disorders such as, for example, tumors and metastasizing. The invention relates...

20060142307 - Aminopyrazine analogs for treating glaucoma and other rho kinase-mediated diseases and conditions: Methods for using aminopyrazine analogs to treat rho kinase-mediated diseases or rho kinase-mediated conditions, including controlling intraocular pressure and treating glaucoma, are disclosed. Ophthalmic pharmaceutical compositions useful in the treatment of eye diseases such as glaucoma, and additionally useful for controlling intraocular pressure, the compositions comprising an effective amount of...

20060142306 - Sodium channel blockers: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers....

20060142308 - Synergistic combination comprising roflumilast and formoterol: The invention relates to the combined administration of roflumilast and formoterol for the treatment of respiratory tract disorders....

20060142309 - 8-heteroaryl xanthine adenosine a2b receptor antagonists: The present invention also relates to the preparation of the compounds, pharmaceutical formulations thereof, and their use in medicine as potent or selective A2B adenosine receptor antagonists and their uses for treating asthma, autoimmune diseases and retinal vascular diseases....

20060142310 - Process for the preparation of chiral 8-(-3-aminopiperidin-1-yl) xanthines: The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines....

20060142311 - Prodan-containing nucleotide and use thereof: wherein R3 is —OH, ═O, or —NH2, with the proviso that when R3 is —OH or —NH2, R4 is H; when R3 is ═O, R4 is —NH2; and when R3 is ═O, H is attached to the 1-position N of the purine ring, and the bond between the 1-position N...

20060142312 - C6-aryl and heteroaryl substituted pyrido[2,3-d] pyrimidin-7-ones: The present invention provides substituted 2-aminopyridines of formula I, wherein R1, A1, W, X, and Y are as defined in the specification, useful in treating cell proliferative disorders. The novel compounds of the present invention are potent inhibitors of cyclin-dependent kinases 4 (Cdk4)....

20060142313 - Rho-kinase inhibitors: Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds of the present invention are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease....

20060142314 - Rho-kinase inhibitors: Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds of the present invention are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease....

20060142316 - Combination therapy: The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human, which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour,...

20060142315 - Substituted biaryl piperazinyl-pyridine analogues: The present invention relates to dihydrofolate reductase inhibitors having an aromatic group and a heteroaromatic group linked by a methylene group; and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such dihydrofolate reductase inhibitors. More particularly, the present invention relates to dihydrofolate reductase inhibitors...

20060142317 - 3-substituted 3,4-dihydro-thieno[2,3-d]pyrimidin-4-one derivatives, production and use thereof: The invention relates to 3,4-dihydro-thieno[2,3-d]pyrimidin-4-one derivatives which are substituted in position 3 by 5-membered heteroaryl which may be fused to an aryl or heteroaryl radical, where the heteroaryl and, if appropriate, the fused aryl or heteroaryl radical may have 1, 2 or 3 substituents selected independently of one another from...

20060142318 - Compounds for treating fundic disaccomodation: wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y2 is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or...

20060142319 - Pyridyl-substituted spiro-hydantoin crystalline forms and process: wherein Z is N or CR4b; K and L are independently O or S; Ar is an optionally substituted aryl or heteroaryl; A1, A2, G, and Q are linkers; and R2, R4a, R4c, and R16 are defined in the specification. The process includes the reaction of N-substituted glycine compound and...

20060142320 - Polymorphic forms of naltrexone: This invention relates to the discovery of novel polymorphic forms of naltrexone, including solvates, hydrates, anhydrous and other crystalline forms and combinations thereof. These novel forms of naltrexone impart advantages in pharmaceutical formulations incorporating them, including sustained release, or long acting, formulations....

20060142321 - 5-ht7 receptor antagonists: The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some some 2,2a,4,5-tetrahydro-1H-3-aza-acenaphthylen substituted sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT...

20060142322 - 2-alkyl/aryl sulphonyl-1,2,3,4-tetrahydro-9h-pyrido (3,4-b) indole-3-carboxylic acid esters/amides useful as antithrombotic agents: e

20060142323 - Dual binding site acetylcholinesterase inhibitors for the treatment of alzheimer's disease: A family of compounds of formula (I) wherein: X is one of the following radicals: which behaves as dual site acetyl-cholinesterase inhibitors and which are especially useful for the treatment of cognitive disorders as senile dementia, cerebrovascular dementia, mild cognition impairment, attention deficit disorder, and/or neurodegenerative dementing disease with aberrant...

20060142324 - Aryl fused 2,4-disubstituted pyridines: nk3 receptor ligands: Disclosed are compounds of formula (I) or pharmaceutically acceptable non-toxic salts or pharmaceutically acceptable solvates thereof wherein: (II) represents (a), (b), (c) or (d) and W, X, Y, A, B, C, D, E are variables as described herein. These compounds are highly selective agonists or antagonists at NK3 receptors or...

20060142325 - Fused bicyclic-substituted amines as histamine-3 receptor ligands: s

20060142330 - 1-heterocyclylalkyl-3-sulfonylazaindole or -azaindazole derivatives as 5-hydroxytryptamine-6 ligands: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor....

20060142327 - Beta 3 adrenergic agonists: The present invention relates to a β3 adrenergic receptor agonist of formula (1) or a pharmaceutical salt thereof; useful for treating Type II diabetes and/or obesity....

20060142328 - Beta 3 adrenergic agonists: The present invention relates to a β3 adrenergic receptor agonist of formula (I) or a pharmaceutical salt thereof; useful for treating Type II diabetes and/or obesity....

20060142329 - Beta 3 adrenergic agonists: The present invention relates to a β3 adrenergic receptor agonist of formula (I) or a pharmaceutical salt thereof; useful for treating Type II diabetes and/or obesity....

20060142326 - Use of pyrazolopyridines for the treatment of cognitive deficits: The invention relates to methods which are used to improve, increase or facilitate the cognition of individuals with neurodegenerative pathologies. More specifically, the invention relates to the use of compounds from the family of pyrazolopyridines in order to improve the cognitive faculties of individuals with neurodegenerative diseases. The invention can...

20060142331 - Novel 8-aza-bicyclo[3.2.1]octane derivatives and their use as monoamine neurotransmitter re-uptake inhibitors: This invention relates to novel 8-aza-bicyclo[3.2.1]octane derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention....

20060142332 - 5-ht7 receptor antagonists: The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some some tetrahydroisoquinoline substituted sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT...

20060142333 - Vanilloid receptor modulators: e

20060142335 - Substituted carbamic acid quinolin-6-yl esters useful as acetylcholinesterase inhibitors: The present invention relates to new substituted carbamic acid quinoline-6-yl esters of formulae 1 and 2 where R1=alkyl, aryl; R2=H, alkyl, aralkyl useful as acetylcholinesterase inhibitors, and which show potent antiacetylcholinesterase activity and have potential therapeutic use for prevention or cure of acetylcholinesterase related disorders including peripheral as well as...

20060142334 - Tetrahydroquinoline derivatives: The present invention relates to tetrahydroquinoline derivatives having gene formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are H or Me; R3 is H, hydroxy, (1-4C)alkoxy, (di)(1-4C)alkylamino(2-4C)alkoxy or (2-6)heterocycloakl(2-4C)alkoxy; R4 is H, OH, (1-4C)alkoxy or R7; R5 is H, OH, (1-4C)alkoxy or R7, with the proviso...

20060142336 - N-sulfonylpiperidines as metalloproteinase inhibitors (tace): Compounds of formula (1), wherein Z is —CONR15OH or —N(OH)CHO and X is —(CR9R10)t-Q-(CR11R12)u- (where t and u are independently 0 or 1 with the proviso that t and u cannot both be 0);are inhibitors of metalloproteinases and in particular TACE....

20060142337 - Piperidine derivative and use thereof: wherein Ar is an aryl group optionally having substituents, R is a C1-6 alkyl group, R1 is a hydrogen atom, a hydrocarbon group optionally having substituents, an acyl group or a heterocyclic group optionally having substituents, X is an oxygen atom or an imino group optionally having substituents, ring A...

20060142338 - 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases: In its many embodiments, the present invention provides a novel class of compounds as inhibitors of type 3 17β-hydroxysteroid dehydrogenase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition,...

20060142339 - Aminosulfonyl substituted 4-(aminomethyl)-piperidine benzamides as 5ht 4-antagonists: The present invention is concerned with novel compounds of formula (I) having 5HT4-antagonistic properties. The invention further relates to methods for preparing such novel compounds, pharmaceutical compositions comprising said novel compounds as well as the use as a medicine of said compounds....

20060142341 - Bicyclic benzamides of 3- or 4-substituted 4-(aminomethyl)-piperidine derivatives: a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R1 and R2 taken together form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl; R3 is hydrogen or halo; R4 is...

20060142342 - Bicyclic benzamides of 3- or 4-substituted 4-(aminomethyl)-piperidine derivatives: a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R1 and R2 taken together form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl; R3 is hydrogen or halo; R4 is...

20060142340 - Hydroxycarbonylphenyl substituted 4-(aminomethyl)-piperidine benzamides as 5ht4 antagonists: The present invention is concerned with novel compounds of formula (I) having 5HT4-antagonistic properties. The invention further relates to methods for preparing such novel compounds, pharmaceutical compositions comprising said novel compounds as well as the use as a medicine of said compounds....

20060142343 - Pyrrolines: e

20060142344 - Method for treating hiv infection through co-administration of tipranavir and gw695634: A method for treating HIV infection through co-administration of tipranavir and GW695634....

20060142345 - 3,5 disubstituted indazole compounds, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation: 3,5 disubstituted indazole compounds that modulate and/or inhibit cell proliferation, such as the activity of protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating CDK dependent diseases to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic...

20060142346 - S-lansoprazole compositions and methods: Methods and compositions are disclosed utilizing optically pure (−) lansoprazole for the treatment of ulcers in humans while substantially reducing the concomitant liability of adverse effects associated with the racemic mixture of lansoprazole. The optically pure (−) isomer is also useful for the treatment of gastroesophageal reflux. (−) Lansoprazole is...

20060142347 - Compounds and methods for the treatment or prevention of flavivirus infections: t

20060142348 - Aryl sulfonamide peri-substituted bicyclics for occlusive artery disease:

20060142349 - Methods of modulating the activities of alpha-7 nicotinic acetylcholine receptor: The present invention provides methods for identifying compounds useful in modulating α7 nicotinic acetylcholine receptors. The invention also provides compounds that prevent, suppress or inhibit desensitization of an α7 nicotinic acetylcholine receptor, and which resensitize such receptors. Pharmaceutical compositions, and methods of treatment, particularly in regard of neurological diseases are...

20060142350 - 2-(butyl-1-sulfonylamino)-n-[1(r)-(6-methoxypyridin-3-yl)propyl] benzamide, its use as a medicament, and pharmaceutical preparations comprising it: e

20060142351 - Method of increasing systemic tryptophan with niacin compounds: Chronic infection with retroviruses, such as HIV, induce a number of metabolic derangements. The present invention relates to a method for increasing systemic tryptophan with niacin compounds....

20060142352 - Compounds useful for the treatment of cancer, compositions thereof and methods therewith: The present invention generally relates to compounds and compositions useful for the modulation of ligase activity. The invention further relates to Compounds of the Invention, compositions thereof, and methods for treating or preventing cancer, a neoplastic disorder, acute or chronic renal failure, an inflammatory disorder, an immune disorder, a cardiovascular...

20060142353 - Cetylpyridinium salt of an anti-inflammatory agent and pharmaceutical compositions containing it: Cetylpyridinium salt of diclofenac....

20060142354 - Use of epothilone derivatives for the treatment of hyperparathyroidism: t

20060142355 - Carboxylic acid peri-substituted bicyclics for occlusive artery disease:

20060142357 - Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1: wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a...

20060142356 - Novel therapeutic method and compositions for topical administration: According to the invention there is provided a pharmaceutical composition suitable for topical administration to the skin which comprises farglitazar, or a pharmaceutically acceptable salt thereof, and a physiologically acceptable carrier and its use in the treatment of skin conditions....

20060142358 - Kynurenine 3-hydroxylase inhibitors for the treatment of diabetes: The present invention relates to the use of at least one compound with inhibitory activity on kynurenine 3-hydroxylase for the preparation of a medicament for the prevention and/or treatment of diabetes....

20060142359 - Cyclopenta[c]isoxazole-3-amines used as protective agents for materials: e

20060142361 - Azole derivatives and methods for making the same: The present invention is broadly directed to azole derivatives that exhibit antifungal activity and methods for making the same. In one aspect, the invention includes carboxylic acid and phosphate ester derivatives of fluconazole that exhibit antifungal activity. In addition, the invention comprises methods for synthesizing the derivatives and pharmaceutical compositions...

20060142360 - Compound: wherein each T is independently selected from H, hydrocarbyl, —F—R, and a bond with one of D, E, P or Q, or together with one of P and Q forms a ring; Z is a suitable atom the valency of which is m; D, E and F are each independently...

20060142362 - Heteroarylacetamide inhibitors of factor xa: e

20060142363 - Imidazolidinedione analogs useful as anticoagulants and antithrombotics:

20060142365 - Benzimidazole compounds and antiviral uses thereof: The present invention relates to novel benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses benzimidazole compounds that inhibit membrane fusion associated events such as viral transmission, reduce viral load or otherwise treat viral infections. The invention also encompasses the use of benzimidazole compounds as inhibitors of...

20060142364 - Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof: Compounds of formula (I) or pharmaceutically acceptable salts thereof: Formula (I) wherein R1, R2, RF1, RF2 and Z are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain....

20060142366 - Novel heteroaryl-substituted acetone derivatives as inhibitors of phospholipase a2: The invention relates to novel heteroaryl substituted acetone derivatives which inhibit the enzyme phospholipase A2, pharmaceutical preparations containing these compounds and a method of producing these compounds....

20060142368 - Compounds and methods for inducing apoptosis in proliferating cells: Compounds useful for inducing apoptosis in proliferative cells, particularly cancer cells, including but not limited to prostate cancer, leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, bladder cancer, lymphoma, and breast cancer. These compounds are particularly useful in the treatment of androgen-independent cancers, including...

20060142367 - Pyrazole compound: m

20060142369 - Delta 1-pyrrolines used as pesticides:

20060142370 - Sumanene and method for manufacturing the same:

20060142371 - 3,6-disubstituted azabicyclo [3.1.0] hexane derivatives useful as muscarinic receptor: This invention generally relates to the derivatives of 3,6 disubstituted azabicyclo[3.1.0]hexanes. The compounds of this invention are muscarinic receptor antagonists which are useful, inter-alia, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to a process for the...

20060142372 - Benzofurane derivatives and the use the same as antidepressants and anxiolytics: Novel benzofuran derivatives of the formula (I) in which R1, R2, X, Y, Z and m have the meanings indicated in Patent Claim 1, they have a strong affinity to the 5-HT1A receptors. The compounds inhibit serotonin reuptake, exhibit serotonin-agonistic and -antagonistic properties and are suitable as antidepressants, anxiolytics, antipsychotics,...

20060142373 - Medicaments for the treatment or prevention of fibrotic diseases: v

20060142374 - Crystal for oral solid drug and oral solid drug for dysuria treatment containing the same: A crystal for oral solid medicament comprised of indoline compound (KMD-3213) which exerts α1-adrenaline receptor blocking effect, is useful as a therapeutic agent for dysuria and is represented by the formula: (I) wherein in the powder X-ray diffraction pattern, the compound is characterized by main peaks of 5.5°±0.2°, 6.1°±0.2°, 9.8°±0.2°,...

20060142375 - Method for augmenting the effects of serotonin reuptake inhibitors: A method of treating a subject for a serotonergic neurotransmission dysregulation disorder, comprises administering the subject a serotonin enhancer (e.g., a serotonin reuptake inhibitor) in an amount effective to treat the disorder; and concurrently administering the subject 5-hydroxytryptophan in an amount effective to enhance the activity of the serotonin enahancer,...

20060142376 - Method for obtaining an antiepileptic agent: A process for obtaining the pharmaceutical active ingredient, levetiracetam, by means of deaminomethylation of a sufficiently pure enantiomer intermediate (S)-(II), or by means of deaminomethylation of an addition salt thereof with an acid, wherein R1 and R2 are either the same or different (C1-C6)-alkyl radicals, or else R1 and R2...

20060142378 - Amino-functionalized 1,2,4-trioxanes useful as antimalarial agents and process for preparation thereof: p

20060142377 - Orally active, antimalarial, anticancer, artemisinin-derived trioxane dimers with high selectively, stability and efficacy and methods of making the same: In only two steps and in 65% overall yield, natural trioxane artemisinin (I) was converted on gram scale into C-10-carba trioxane dimer (3). This new, very stable dimer was then transformed easily in one additional step into four different dimers (4-7). Alcohol and diol dimers (4 and 5) and ketone...

20060142379 - Use of ap-1 activators to treat glaucoma and ocular hypertension: Compositions comprising AP-1 activators and methods of use for treating glaucoma and ocular hypertension are disclosed....

20060142380 - 2-phenylpyran-4-one derivatives as selective cox-2 inhibitors: The present invention relates to 2-phenylpyran-4-derivatives of general formula (I), processes for their preparation, pharmaceutical compositions containing them, and their medical uses....

20060142381 - Furancarboxamides: e

20060142382 - Skin lightening composition: A composition which comprises (i) tranexamic acid or a salt thereof, (ii) L-cysteine, a derivative thereof or a salt thereof and, as occasion demands, (iii) L-ascorbic acid, a derivative thereof or a salt thereof....

20060142383 - 3d-structure model of sars coronavirus 3cl protease and anti-sars drugs: The present invention discloses 3D-structure of SARS-CoV Viral 3CL Protease obtained through molecular simulation. The 3D-structure is used as a drug target for screening the existing medical database CMC (Comprehensive Medicinal Chemistry, MDL Information System, Inc.), and a group of compounds which have the activity of inhibiting SARS-CoV virus 3CL...

20060142384 - 2-oxyamino-1-cyclopentene-1-nitriles as material protective agents: e

20060142386 - Bis(thio-hydrazide amides) for increasing hsp70 expression:

20060142385 - Inhibitors of matrix metalloproteinase:

20060142387 - Chemical compounds: This invention relates to non-steroidal compounds that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds....

20060142388 - 2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative: (wherein R1 and R2 are the same or different, and each represents a hydrogen atom, C1-10alkyl group, etc; X represents a hydrogen atom or a fluorine atom; and Y represents an amino group, —SR3, —S(O)nR7, —SCHR3R4, —S(O)nCHR3R4, —NHCHR3R4, —N(CHR3R4)(CHR5R6), —NHCOR3 or —OCOR7), a pharmaceutically acceptable salt thereof, or a hydrate...

20060142389 - Pharmaceutically useful salts of carboxylic acid derivatives: A compound selected from one or more of the following: a (1R,2S)-2-hydroxyindan-1-amine salt of (2S)-2-ethoxy-3-(4-{2-[hexyl(2-phenylethyl)amino]-2-oxoethoxy}phenyl)propanoic acid; an L-arginine salt of (2S)-2-ethoxy-3-(4-{2-[hexyl(2-phenylethyl)amino-2-oxoethoxyphenyl)propanoic acid; a tert-butylamine salt of (2S)-2-ethoxy-3-(4-{2-[hexyl(2-phenylethyl)amino-2-oxoethoxyphenyl)propanoic acid; a choline salt of (2S)-2-ethoxy-3-(4-{2-[hexyl(2-phenylethyl)amino]-2-oxoethoxy}phenyl)propanoic acid; an adamantylamine salt of (2S)-2-ethoxy-3-(4-{2-[hexyl(2-phenylethyl)amino]-2-oxoethoxy}phenyl)propanoic acid; a N-benzyl-2-phenylethanaminium salt of (2S)-2-ethoxy-3-(4-{2-[hexyl(2-phenylethyl)amino]-2-oxoethoxy}phenyl)propanoic acid; a N-benzyl-2-(benzylamino) ethanaminium salt...

20060142391 - Ppargamma-activating pharmaceutical composition: The present invention relates to PPARγ-activating pharmaceutical compositions comprising a hydroxylated derivative of a C20-22 polyunsaturated fatty acid or a pharmaceutically acceptable salt thereof, preferably PPARγ-activating pharmaceutical compositions containing a hydroxylated derivative of docosahexaenoic acid (DHA) or a hydroxylated derivative of eicosapentaenoic acid (EPA) or a pharmaceutically acceptable salt thereof,...

20060142390 - Treatment for severe melancholic depression: Methods for treating severe melancholic depression, comprising administering, to a subject, a preparation comprising EPA, or metabolite(s) thereof....

20060142392 - Process for preparing (2s)-3-(4-{2-[amino]-2-oxoethoxy}phenyl)-2-ethoxypropanoic acid derivatives: t

20060142393 - Bis(thio-hydrazide amides) for treatment of hyperplasia:

20060142395 - Modulation of intracellular calcium signaling by n-acylethanolamines: The present invention includes compositions and methods for neuroprotection by modulating intracellular calcium concentrations by administering an effective amount of an N-acylethanolamine to a subject....

20060142394 - Use of proteases for decomposing allergens: The invention relates to the use of an active ingredient for inhibiting dust mite feces and/or mold spores as well as for denaturing the keratin of animal hair as well as plant pollen or plant spores, consisting of an enzyme such as auxillase, alcalase, bromelain, alpha-chymotrypsin, collagenase, pepsin, pronase, thrombin...

20060142396 - Use of gaba agonists for the treatment of spastic disorders, convulsions, epilepsy, and neuroprotection: A method of treating a neuronal disorder is provided that includes the intravenous administration to a subject suffering or predisposed to a neuronal disorder a therapeutically effective amount of gamma-aminobutyramide or a pharmaceutically acceptable salt thereof. Gamma-aminobutyramide has sufficient stability for intravenous administration and is able to cross the blood-brain...

20060142397 - Use of a pparalpha agonist and metormin for decreasing the serum triglycerides: The present invention relates to the combined use of a PPARα agonist and metformin for decreasing serum triglycerides....

20060142398 - Method and composition for adminstering an nmda receptor antagonist to a subject: The invention provides methods and compositions for administering an NMDA receptor antagonist (e.g., memantine) to a subject....

20060135406 - Compositions and methods for treating pathologies that necessitate suppression of gastric acid secretion: The present invention is related to novel oral compositions comprising an irreversible gastric H+/K+-ATPase proton pump inhibitor (PPI) as a gastric acid secretion inhibitor, pentagastrin (PG) or a PG analogue as an activator of parietal cells in the gastric lumen. In a preferred embodiment, the composition further comprises at least...

20060135401 - Novel method of selecting immunosuppressant having little thrombocytopenic effect: The invention relates to a novel method for selecting an immunosuppressive agent with a less thrombocytopenia effect. According to the invention, a method for selecting an immunosuppressive agent which has a potent immunosuppressive activity but a lower thrombocytopenia effect, said method comprising measuring an IL-2 transcription inhibitory activity in a...

20060135402 - Oral administration of calcitonin: Disclosed is a particular method of orally administering pharmaceutical compositions comprising calcitonin in combination with oral delivery agents, prior to the consumption of food in humans, and a method of treatment of disorders responsive to the action of calcitonin employing such method of administration; also oral calcitonin pharmaceutical compositions with...

20060135405 - Process for producing sterile suspensions of slightly soluble basic peptide complexes, sterile suspensions of slightly soluble basic peptide complexes, pharmaceutical formulations containing them, and the use thereof as medicaments: The present invention provides a novel process for producing sterile suspensions of slightly soluble basic peptide complexes. The present invention further provides a novel process for producing sterile lyophilizates of slightly soluble basic peptide complexes. In addition, a novel process for producing sterile suspensions suitable for the parenteral administration of...

20060135403 - Therapeutic formulations for the treatment of beta-amyloid related diseases: The method is used for preventing or treating an amyloid-β related disease in a subject. The method comprises administering to a subject in need thereof an effective amount of a first agent that prevents or treats amyloid-β related disease, and a second agent that is (i) a peptide or peptidomimetic...

20060135404 - Water soluble paclitaxel derivatives: Disclosed are water soluble compositions of paclitaxel and docetaxel formed by conjugating the paclitaxel or docetaxel to a water soluble polymer such as poly-glutamic acid, poly-aspartic acid or poly-lysine. Also disclosed are methods of using the compositions for treatment of tumors, auto-immune disorders such as rheumatoid arthritis. Other embodiments include...

20060135407 - Phosphoprotein preparations for bioactive metal ion delivery and teeth remineralisation: The invention provides, in one aspect, compositions for delivering a bioactive metal ion to a mammal, the compositions comprising (a) an effective amount of a source of the bioactive metal ion, (b) a phosphoprotein preparation obtained by partially cross linking a partial hydrolysate of casein or a caseinate, and (c)...

20060135408 - Glycogen synthase kinase-3 inhibitors: Novel conjugates that are capable of inhibiting GSK-3 activity, a process of producing same, pharmaceutical compositions including same and methods of using same in the treatment of GSK-3 mediated conditions are disclosed. Methods of treating affective disorders using GSK-3 inhibitors are further disclosed....

20060135409 - Process for and intermediates in the preparation of canfosfamide and its salts: A process for and intermediates in the preparation of canfosfamide and its salts. Some of the intermediates have anticancer activity....

20060135410 - Targeted delivery to legumain-expressing cells: The present invention relates to new agents and methods useful for preventing, treating and diagnosing diseases such as cancer. For example, the invention relates to prodrug agents useful for targeting and delivering cytotoxic drugs to cancerous cells....

20060135412 - Methods for the treatment of alzheimers disease and compositions therefore: The invention discloses previously unknown modifiers of Aβ secretion. These proteins are identified as suitable targets for the development of new therapeutics to treat, prevent or ameliorate pathological conditions associated with Aβ secretion, including Alzheimer's Disease. The invention also relates to methods to treat, prevent or ameliorate said pathological conditions...

20060135411 - Treatment of inflammatory bowel disease: This invention relates to methods of treatment of inflammatory bowel disease, and especially to treatment of this condition with cyclic peptidic and peptidomimetic compounds which have the ability to modulate the activity of G protein-coupled receptors. The compounds preferably act as antagonists of the C5a receptor, and are active against...

20060135413 - Depsipeptide for therapy of kidney cancer: The present invention provides a therapeutic agent of kidney cancer, which comprises FK228 of the formula (I) or a salt thereof. FK228 or a salt thereof, which is an active ingredient in the present invention, shows a superior antitumor activity in vivo against kidney cancer....

20060135414 - Deuterated cyclosporine analogs and their use as immunomodulating agents: Cyclosporine derivatives are disclosed which possess enhanced efficacy and reduced toxicity over naturally occurring and other presently known cyclosporins and cyclosporine derivatives. The cyclosporine derivatives of the present invention are produced by chemical and isotopic substitution of the cyclosporine A (CsA) molecule by: (1) Chemical substitution and optionally deuterium substitution...

20060135415 - Immunomodulation and effect on cell processes relating to serotonin family receptors and the blood-brain barrier: The present invention relates to the discovery that signaling via a serotonin type 1B, 2, 4 and 6 receptor is important in T cell activation such that inhibiting such signaling, such as by using fluphenazine, can be used to modulate the immune response, cell proliferation, and apoptosis, among other cell...

20060135429 - Compositions and methods for inducing apoptosis in tumor cells: A method is described for using an E-domain peptide for the induction of apoptosis in a cancer cells. In particular, the invention relates to methods for using a-type E-domain peptide from trout IGF and/or a b-type E-domain peptide from human IGF for the induction of apoptosis in a broad spectrum...

20060135427 - Formulations of human growth hormone comprising a non-naturally encoded amino acid: Formulations of modified human growth hormone polypeptides are provided....

20060135425 - Intravenous injection of plasminogen non-neurotoxic activators for treating cerebral stroke: The invention refers to the use of non-neurotoxic plasminogen activating factors, e.g., from Desmodus rotundus (DSPA) or genetically modified plasminogen activating factors, for example of human origin, for the therapeutic treatment of stroke in mammals....

20060135428 - Long lasting anti-angiogenic peptides: Modified anti-angiogenic peptides are disclosed. The modified peptides are capable of forming a peptidase stabilized anti-angiogenic peptide. The modified anti-angiogenic peptides, particularly modified kringle 5 peptides are capable of forming a conjugate with a blood protein. Conjugates are prepared from anti-angiogenic peptides, particularly kringle 5 peptides, by combining the peptide...

20060135426 - Long lasting synthetic glucagon like peptide (glp-1): Modified insulinotropic peptides are disclosed. The modified insulinotropic peptides are capable of forming a peptidase stabilized insulinotropic peptide. The modified insulinotropic peptides are capable of forming covalent bonds with one or more blood components to form a conjugate. The conjugates may be formed in vivo or ex vivo. The modified...

20060135420 - Method of diagnosing non-alcoholic steatohepatitis (nash) using molecular markers: The invention relates to a method of diagnosing non-alcoholic steatohepatitis (NASH) using molecular markers. The inventive method consists in detecting and quantifying, in vitro in a hepatic tissue sample, the levels of a protein which can be used as a NASH molecular marker and which is selected from apolipoprotein A1,...

20060135416 - Multifunctional context-activated protides and methods of use: This invention is directed to multifunctional, context-activated protides that have two or more effectors with individually distinct biological functions and one or more corresponding activator sites that can each initiate or amplify the biological function of one or more effectors upon context-activation. The context-activated protides of the invention are useful...

20060135419 - Proteins involved in the regulation of energy homeostasis: The prevent invention discloses PRL-1 homologous proteins regulating the energy homeostasis and the metabolism of triglycerides, and polynucleotides, which identify and encode the proteins disclosed in this invention. The invention also relates to the use of these sequences in the diagnosis, study, prevention, and treatment of metabolic diseases and disorders....

20060135418 - Receptors: A multivalent T cell receptor (TCR) complex comprising at least two TCRs, linked by a non-peptidic polymer chain or a peptidic linker sequence. Preferably the TCR complex comprises TCR heterodimers having a non-native disulfide bond between constant domain residues, said TCRs being linked via an optionally substituted, polyalkylene glycol linker....

20060135424 - Treatment of short bowel syndrome patients with colon-in-continuity: Intestinal absorption is enhanced in short bowel syndrome patients presenting with colon-in-continuity by treatment with a GLP-2 receptor agonist, such as teduglutide....

20060135421 - Unitary combination of fsh and hcg: A novel ovulatory induction paradigm entails administration of hCG in combination with FSH during all stages of treatment, where the ratio of FSH to hCG is adjusted to optimize ovulatory stimulation and minimize complications. The use of compositions characterized by various FSH:hCG ratios enables the practitioner readily to tailor the...

20060135422 - Use of angiotensin receptor blockers (arbs) to treat diseases associated with excess ace: Disclosed are methods of treating neuropsychiatric diseases, neuromuscular diseases, viral infections, neurodegenerative diseases and ricin poisoning using angiotensin II receptor blockers....

20060135417 - Use of the crh (corticotropin releasing hormone)-ucn (urocortin) system in the treatment of inflammatory diseases: The invention relates to the use of corticotropin-releasing hormone (CRH) receptor-1 (R1) antagonists and/or CRH-R2 receptor agonists for the treatment of inflammatory diseases via regulation of monocyte/macrophage cell activation, proliferation, differentiation, apoptosis, and inflammatory cytokine production. As CRH system we define natural and synthetic CRH and urocortin (UCN) agonists and...

20060135423 - Vegf-a as an inhibitor of angiogenesis and methods of using same: The invention relates to methods and compositions for the treatment or prevention of ocular angiogenesis and neovascularization associated with neovascular disease. Administration of vascular endothelial growth factor (VEGF)-A into the eye when macrophage infiltration is reduced inhibits ocular angiogenesis....

20060135430 - Bly antagonists and uses thereof: The present invention relates to polypeptides that block BLyS signaling, nucleic acid molecules encoding the polypeptides, and compositions comprising the polypeptides. The present invention also relates to methods for treating an immune-related disease or cancer using the polypeptides and compositions of the invention. The present invention also relates to methods...

20060135431 - Peptides and related molecules that bind to tall-1: wherein V1 is a vehicle that is covalently attached to one or more of the above TALL-1 modulating compositions of matter. The vehicle and the TALL-1 modulating composition of matter may be linked through the N- or C-terminus of the TALL-1 modulating portion. The preferred vehicle is an Fc domain,...

20060135435 - Agent that retards transformation of hormone-dependent cancer to non-hormone-dependent cancer: The present invention relates to a composition that retards the transformation of a hormone-dependent cancer to a non-hormone-dependent cancer, which contains a hormonal agent. The composition of the present invention that retards the transformation of a hormone-dependent cancer to a non-hormone-dependent cancer, which contains a hormonal agent, is capable of...

20060135432 - Agonists and antagonists of conadotropin-releasing hormone-2, and use thereof: The present invention relates to agonists and antagonists of gonadotropin-releasing hormone-2 (GnRH-2), which regulates the activity of GnRH-2 by specifically binding to GnRH-2 receptors, and uses thereof The pharmaceutical compositions comprising the GnRH-2 agonists and antagonists according to the present invention are useful for the treatment of reproductive physiology diseases...

20060135434 - New peptides: The present invention relates to new peptides for targeting to vascular endothelial growth factor receptor 2, VEGFR-2. The invention further relates to their use in therapeutically effective treatment as well as for diagnostic imaging techniques....

20060135433 - Phenolic binding peptides: The present application relates to peptides which bind to tannin, polyphenolic or anthocyanin compounds, and particularly to tea and wine stains on a fabric or other surface. The invention also concerns binding peptide conjugates which includes a binding peptide coupled to an agent and the use of the binding peptide...

20060135436 - Peptides and methods for the control of obesity: e

20060135437 - Novel use of peptide compounds for treating pain in trigeminal neuralgia: The present invention is directed to the use of a class of peptide compounds for treating pain in trigeminal neuralgia....

20060135438 - Peptidyl prodrugs that resist p-glycoprotein mediated drug efflux: Amino acid ester, dipeptide, and tripeptide ester derivatives of bioactive agents are provided wherein said parent agents are substrates effluxed by the P-gp transporter. The derivatives are useful in treating the same condition as the bioactve agent. Also disclosed is a method for preparing a bioactive agent for targeted delivery...

20060135439 - Remedy for nerve damage: The present invention provides a therapeutic agent for nerve damages such as those caused by spinal cord injury or nerve trauma, which comprises, as an active ingredient, a low-molecular-weight saccharide composed of at least glucuronic acid and/or N-acetylglucosamine or a pharmaceutically acceptable salt thereof. The present invention also provides a...

20060135440 - Use of ribose to alleviate rhabdomyolysis and the side effects of statin drugs: A method of alleviating the symptoms of rhabdomyolysis or the side effects of statin DRUG administration is disclosed. The method comprises the administration of D-ribose in doses of three to ten grams at least twice a day until the symptoms or side effects are alleviated....

20060135441 - Combinatorial chemotherapy treatment using na+/k+ atpase inhibitors: The reagent, pharmaceutical formulation, kit, and methods of the invention provides a new approach to alleviate or eliminate certain negative effects associated with the use of certain cancer treatment agents (e.g. chemotherapy therapeutics, etc.) or regimens (e.g. radio therapies, etc.), including stimulation of the hypoxic stress response in tumor cells....

20060135442 - Pancreatic cancer treatment using na+/k+ atpase inhibitors: The reagent, pharmaceutical formulation, kit, and methods of the invention provides a new approach for treating pancreatic cancers. The invention provides the use of Na+/K+-ATPase inhibitors, such as cardiac glycosides (e.g. ouabain and proscillaridin, etc.), either alone or in combination with other standard therapeutic agents (chemo- or radio-therapies, etc.) for...

20060135443 - Use of na*/k*-atpase inhibitors and antagonists thereof: The reagent, pharmaceutical formulation, kit, and methods of the invention provides a new approach for treating hypoxia-related pathological conditions, such as Alzheimer's Disease, and those involving excessive angiogenesis, especially those non-cancer pathological conditions. The invention provides the use of Na+/K+-ATPase inhibitors, such as cardiac glycosides (e.g. ouabain and proscillaridin, etc.),...

20060135445 - Breast cancer-resistant protein inhibitor: e

20060135444 - Combination of flavonoid and procyanidin for the reduction of the mammalian appetite: A nutritional composition suitable for reducing appetite, a method for the treatment and/or prevention of overweight and a method for the reduction of a mammalian appetite. The weight reduction and/or appetite reduction is achieved by administration of procyanidin and a flavonoid selected from the group consisting of chrysin, flavone, precursors...

20060135446 - Composition for improving blood fluidity: The present invention provides a composition for improving blood fluidity that comprises proanthocyanidins and an antioxidant (which is a substance other than proanthocyanidins, ascorbic acid and its derivatives) as active components. The composition for improving blood fluidity of the present invention improves blood flow in the body and further improves...

20060135447 - Macrolides: e

20060135448 - Hydroxypyridinones for the local treatment of skin microcirculatroy disorders: The application of hydroxypyridonone in effective amounts as external agent for patients suffering from skin micro-circulatory disorders (SMD) provides for a significant amelioration of subject conditions. Accordingly, the new use of hydroxypyridonones as external anti-inflammatory agent thereby combined with the depletion of hemosiderin residues offers a suitable treatment to SMD...

20060135458 - Antiviral oligonucleotides: Random sequence oligonucleotides that have antiviral activity are described, along with their use as antiviral agents. In many cases, the oligonucleotides are greater than 40 nucleotides in length and include chemical modifications, such as modified internucleotidic linkages and modifications at the 2′-position of the ribose moieties. Also described are methods...

20060135450 - Combinations of antisense oligonucleotides directed against thymidylate synthase mrna and uses thereof: Effective combinations of antisense oligonucleotides directed against thymidylate synthase mRNA are provided for use in cancer therapies. Combinations of antisense oligonucleotides have enhanced activity compared to the activity of the individual antisense oligonucleotides when used alone. The combinations may be used in conjunction with one or more chemotherapeutic agents to...

20060135449 - Decoy compositions for treating and preventing brain diseases and disorders: The present invention provides introduction of NF-κB decoy oligodeoxynucleotide into rat cranial nerve through a carotid artery during global brain ischemia. Polymerase chain reaction demonstrated that one hour after global brain ischemia, transfected NF-κB decoy oligodeoxynucleotide effectively suppressed expression of tumor necrosis factor α, interleukin 1β and intracellular adhesion molecule...

20060135453 - Down-regulation of target-gene with pei/single-stranded oligoribonucleotide complexes: The present invention provides methods for the downregulation of target genes by an RNA interference mechanism using short single stranded RNA and a cationic polymer, such as linear PEI....

20060135456 - Methods and compositions for rna interference: The present invention provides methods for attenuating gene expression in a cell, especially in a mammalian cell, using gene-targeted double stranded RNA (dsRNA), such as a hairpin RNA. The dsRNA contains a nucleotide sequence that hybridizes under physiologic conditions of the cell to the nucleotide sequence of at least a...

20060135455 - Methods and compositions for the inhibition of gene expression: The present invention relates to methods and compositions for the inhibition of gene expression. In particular, the present invention provides oligonucleotide-based therapeutics for the inhibition of oncogenes involved in cancers....

20060135457 - Methods for constructing antibiotic resistance free vaccines: The present invention provides DNA vaccines comprising an antibiotic resistance gene-free plasmid, methods of generating same, and methods for treating a disease agent, comprising same....

20060135452 - Methods for treating or preventing angiogenesis-dependent symptoms: A method for enhancing the transfection efficiency of naked plasmid DNA in treating and/or preventing angiogenesis-dependent symptoms is provided by the present inventions. According to the present method, a suitable naked plasmid DNA is subjected for intramuscular injection under increased pressure inside the muscle or hyperbaric oxygen. Angiogenesis-dependent symptoms, including...

20060135460 - Methods, assays and compositions for treating retinol-related diseases: Described herein are methods and compositions for treating certain retinol-related diseases and conditions by modulation of transthyretin (TTR) and retinol binding protein (RBP) availability in the subject. For example, the methods and compositions provide for therapeutic agents for the treatment and/or prevention of age-related macular degeneration and/or dystrophies, metabolic disorders,...

20060135454 - Modulation of immunostimulatory activity of immunostimulatory oligonucleotide analogs by positional chemical changes: The invention relates to the therapeutic use of oligonucleotides or oligonucleotide analogs as immunostimulatory agents in immunotherapy applications. The invention provides methods for enhancing the immune response caused by immunostimulatory oligonucleotide compounds....

20060135462 - N8- and c8-linked purine bases and structurally related heterocycles as universal nucleosides used for oligonucleotides hybridization: The present invention is directed to a nucleic acid binding compound comprising N8- or C8-linked purine bases or structurally related heterocycles, a compound useful for the preparation of such compound, a binding product of this nucleic acid binding compound with a nucleic acid, a method for the determination of a...

20060135461 - Reduction of hair growth: Mammalian hair growth is reduced by topically applying a composition including a survivin inhibitor....

20060135459 - Targeted innate immunity: Provided is a cancer therapeutic agent comprising a cancer targeting molecule linked to a CpG oligodeoxynucleotide. Also provided are methods of reducing the size of a tumor or inhibiting the growth of cancer cells in an individual or inhibiting the development of metastatic cancer, comprising administering an effective amount of...

20060135451 - Vaccine: The present invention relates to methods and compositions useful in the treatment and prevention of Hepatitis C virus (HCV) infections and the symptoms and diseases associated therewith. In particular the present invention relates to DNA vaccines that encode the HCV Core protein and a polynucleotide sequence that encodes at least...

20060135464 - Anti-infective compositions, methods and systems for treating pathogen-induced disordered tissues: Compositions, methods and systems for treating disordered epithelial tissues, such as is caused by pathogens and/or by toxins produced thereby. The invention relates to the use of an anti-infective and/or antimicrobial active agent in a carrier, with vigorous agitation of the disordered epithelial tissue for topical treatment thereof under such...

20060135463 - Methods and compositions for the treatment of lupus using clofarabine: This invention relates to methods of treating or preventing lupus comprising the administration of clofarabine or a pharmaceutically acceptable salt, hydrate, solvate or clathrate thereof to a patient in need of such treatment. The invention further relates to methods of treating or preventing lupus comprising the administration of clofarabine or...

20060135467 - Partial and full agonists of a1 adenosine receptors: Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular the supraventricular tachycardias, emesis, angina, myocardial infarction and hyperlipidemia....

20060135465 - Synthesis and use of 2'-substituted-n6-modified nucleosides: An improved method of preparing a sugar modified nucleoside analog includes a protocol in which a hydroxy group of a sugar is selectively deprotected and oxidized prior to nucleophilic modification of the corresponding carbonyl group. The modified sugar is then coupled to a heterocyclic base that is modified with a...

20060135466 - Synthesis of 2-aralkyloxyadenosines, 2-alkoxyadenosines, and their analogs: Provided is a method for the synthesis of an aralkyloxyadenosine or an alkoxyadenosine. The method includes protecting the hydroxyl sugar groups with a protecting group to produce a protected halogenated adenosine. The protected halogenated adenosine is alkoxylated, and the hydroxyl sugar groups of the protected halogenated adenosine are deprotected to...

20060135468 - Treatment of refractory cancers using na+/k+ atpase inhibitors: The reagent, pharmaceutical formulation, kit, and methods of the invention provides a new approach to treat refractory cancers using Na+/K+-ATPase inhibitors, such as cardiac glycosides (e.g. ouabain or proscillaridin, etc.)....

20060135471 - Anti-obesity compositions: The present invention relates to compositions and methods for treating obesity. More particularly, the invention relates to a composition comprising a lipase inhibitor such as orlistat, and glucomannan such as konjac as well as methods for utilizing such compositions and kits for carrying out this method....

20060135470 - Composition and method for treatment and prevention of traumatic synovitis and damage to articular cartilage: The invention provides compositions useful for the treatment and/or prevention of damage to diarthrodial (synovial) joints and, in particular, traumatic synovitis, inflammation of the synovial membrane, and damage to the articular cartilage of the joint. Specifically, provided are compositions specially formulated for intra-articular and/or parenteral use in the treatment and/or...

20060135469 - Separate type medical material: A separate type medical material containing a hyaluronic acid ester derivative, which satisfies the storage stability of a hyaluronic acid ester derivative and avoidance of irritation and pain at the time of injecting a therapeutic agent for joints, is provided. A separate type medical material comprising liquid (A) which is...

20060135472 - Use of water-soluble polymers to improve stability of diiodomethyl-para-tolylsulfone in complex matrices: The invention is a method comprising the use of diiodomethyl-para-tolylsulfone with water-soluble polymers, resulting in improved stability of diiodomethyl-para-tolylsulfone in various compositions with complex matrices. In a preferred embodiment of the invention, diiodomethyl-para-tolylsulfone is premixed with a solution of cationic polymer prior to addition to a formulation containing a complex...

20060135474 - Methods for the preparation, isolation and purification of epothilone b, and x-ray crystal structures of epothilone b: The present invention relates to improved methods for the production, isolation and purification of epothilone B. These methods include, for example, a fermentation process for the production of epothilone B, isolation via adsorption onto a resin, and subsequent purification....

20060135475 - Process for preparing an alpha-lipoic acid/cyclodextrin complex and product prepared: The invention relates to a process for the preparation of a cyclodextrin/alpha-lipoic acid complex, wherein in a first step, an alpha-lipoic acid and a cyclodextrin are dissolved in an aqueous alkaline solution having a pH above pH 7, and in a second step an acid is added to lower the...

20060135473 - Process for the preparation of piroxicam: b-cyclodextrin inclusion compounds: The present invention relates to a process for the preparation of inclusion compounds of piroxicam with β-cyclodextrin. More particularly, according to the process of the invention, the aqueous solution of two components is subjected, before drying, to a freezing process at very high rate. The resulting products have physico-chemical characteristics...

20060135476 - Medical device with coating that promotes endothelial cell adherence and differentiation: Compositions and methods are provided for producing a medical device such as a stent, a stent graft, a synthetic vascular graft, heart valves, coated with a biocompatible matrix which incorporates antibodies, antibody fragments, or small molecules, which recognize, bind to and/or interact with a progenitor cell surface antigen to immobilize...

20060135477 - Compositions for injectable ophthalmic lenses: Injectable ophthalmic compositions suitable for forming an intraocular lens in the capsular bag of an eye comprise linear non-functional polysiloxane, linear terminally functional polysiloxane, and at least one crosslinker. The linear terminally functional polysiloxane may comprise a mixture of linear terminally monofunctional polysiloxane and linear terminally di-functional polysiloxane....

20060135478 - Boronated metal-phthalocyanines, process for their preparation, pharmaceutical compositions comprising them and use thereof: The present invention relates to meta 1-phthalocyanines bearing at least a group containing boron isotopes 11B or 10B, covalently bound to the peripheral positions of meta 1-phthalocyanine nucleus; moreover it refers to the processes for their preparation, the pharmaceutical compositions comprising them and their use for the treatment of neoplastic...

20060135479 - Phosphono-carboxylate compounds for treating amyloidosis: Therapeutic compounds and methods for modulating amyloid deposition in a subject, whatever its clinical setting, are described. Amyloid deposition is modulated by the administration to a subject of an effective amount of a therapeutic compound comprising a phosphonate group and a carboxylate group, a congener thereof, or a pharmaceutically acceptable...

20060135480 - Derivatives of succinic and glutaric acids and analogs thereof useful as inhibitors of phex: The present invention relates to derivatives of succinic and glutaric acids and analogues thereof, having the following general formula (I), useful as inhibitors of PHEX. These derivatives are useful for promoting generation of bone mass and treating or preventing diseases or conditions associated with a phosphate metabolism defect. Methods for...

20060135481 - Narcistatin prodrugs: The present invention provides prodrugs derived from the sparingly soluble anticancer isocarbostyril narciclasine, a component of various Narcissus species, said prodrugs having potential for use against animal and human cancers. Also disclosed is an efficient procedure for the synthetic conversion of narciclasine to several more soluble cyclic phosphate compounds, including...

20060135482 - Use of fosinopril to reduce cardiovascular events in disalysis patients: The invention relates to the use of fosinopril or a pharmaceutically acceptable salt thereof, to reduce the risk of occurrence of a cardiovascular event in dialysis patients, in particular blood dialysis patients, especially patients presenting left-ventricular hypertrophy....

20060135483 - Oxygen/nitrogen heterocycle inhibitors of tyrosine phosphatases: Compounds, pharmaceutical compositions, and methods for treating, preventing, or ameliorating symptoms associated with diseases such as diabetes, cancer, neurodegenerative diseases, and obesity are provided. The compounds and compositions inhibit protein tyrosine phosphatase enzymes, e.g., PTP-1B....

20060135484 - Vesicant treatment with phenyl-thiophene type vitamin d receptor modulators: The present invention relates to a method of treating or preventing damage to human skin cells by chemical vesicants by administering a non-secosteroidal, phenylthiophene compound with vitamin D receptor (VDR) modulating activity....

20060135485 - Microbicidal compositions and their use: A composition comprising a potassium salt of N′-hydroxy-N-cyclohexyldiazenium oxide (KHDO) and a diluent is useful for killing fungi. Such a composition but which additionally includes at least one of certain other fungicidally active components is useful for combating microorganisms in general. Such other fungicidally active component is selected from: alcohols,...

20060135487 - Piperazine derivatives and their use as anti-inflammatory agents: This invention is directed to acyl piperazine derivatives which are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans....

20060135488 - Ptp1b inhibitors: This invention relates to modulating (e.g., inhibiting) protein tyrosine phosphatase 1B (PTP1B)....

20060135486 - Use of sulfonamide-including compounds in combination with angiogenesis inhibitors: The present invention relates to pharmaceutical compositions comprising a sulfonamide-including compound in combination with an angiogenesis inhibitor....

20060135489 - Chemical compounds containing tocopherol and at least one additional pharmaceutical active substrate: and R′, R″ and R′″ are equal to H or methyl stands for tocopherol and A stands for C═X, SOm, X or CH2, whereby X is equal to 0, S or NR1 (when n≧1) or S or NR1 (when n=0), and B means a grouping X—R2—Y with Y equal to...

20060135490 - Targeting mpges-1 as a treatment for inflammation which avoids cardiovascular risk: The present invention relates to methods for the treatment of inflammation and pain without increasing cardiovascular risk by administration of an inhibitor of mPGES-1. The invention further is related to identifying inhibitors of mPGES-1 that do not increase cardiovascular risk when administered to an individual....

20060135492 - Use of 2-methylene-19-nor-20(s)-1alpha,25-dihydroxyvitamin d3 to increase bone strength: This invention provides pharmaceutical-uses for 2-methylene-19-nor-20(S)-1α,25-dihydroxyvitamin D3. This compound is characterized by high bone calcium mobilization activity demonstrating preferential activity on bone. This results in a novel therapeutic agent for the treatment of diseases where bone formation is desired, particularly osteoporosis. This compound also exhibits pronounced activity in arresting the...

20060135493 - Use of 2-methylene-19-nor-20(s)-1alpha,25-dihydroxyvitamin d3 to increase bone strength: This invention provides pharmaceutical uses for 2-methylene-19-nor-20(S)-1α,25-dihydroxyvitamin D3. This compound is characterized by high bone calcium mobilization activity demonstrating preferential activity on bone. This results in a novel therapeutic agent for the treatment of diseases where bone formation is desired, particularly osteoporosis. This compound also exhibits pronounced activity in arresting...

20060135491 - Vitamin d3 analog useful for the treatment of osteoporosis: The present invention relates to the vitamin D3 analog (1R,3R)-5-{(E)-(2R, 5R)-2-[2-(4-hydroxy-4-methylpentyl)-spiro[4.5]dec-7-ylidene]-ethylidene}-cyclohexane-1,3-diol which is useful in the treatment of osteoporosis....

20060135495 - Anti-hiv agents with dual sites of action: e

20060135494 - Methods of treating injuries of the nervous system associated with hemorrhage: Methods for treating injuries of the nervous system associated with hermorrhage by administering a hydrophilic bile acid, such as ursodeoxycholic acid (UDCA), salts thereof, and analogs thereof (e.g., glyco-, tauro-ursodeoxycholic acid, and other conjugated derivative)....

20060135496 - Methods of hormonal treatment utilizing ascending-dose extended cycle regimens: The present invention provides ascending-dose extended cycle regimens in which a female is administered an estrogen and a progestin for a period of greater than 30 or 31 consecutive days, optionally followed by a hormone-free period or by a period of administration of estrogen. The disclosed regimens can be administered...

20060135497 - Combination therapy for treating heart disease: A combination therapy and co-therapy method for administering therapeutic doses of an aldosterone antagonist agent and a metolazone-related compound to a subject in need of treatment for hypertension, congestive heart failure, and chronic kidney disease are provided. A pharmaceutical composition comprising these therapeutic agents is also provided....

20060135498 - Compositions useful for the treatment of microbial infections: The present invention is based on the discovery that certain chemical compounds isolated from Chinese medicinal herbs are useful as anti-microbial agents, e.g., anti-bacterial agents, anti-fungal agents, and the like. In particular, the present invention provides compositions useful for treating microbial infections such as, for example, oral microbial infections, including...

20060135499 - Method of achieving accelerated weight loss by administration of a weight loss accelerating agent to a dieting mammal: Accelerating weight loss by admtinistering to a dieting mammal the weight loss accelerating agent 7-oxo DHEA or a pro-drug thereof incapable of in vivo conversion to testosterone....

20060135500 - Novel oral pharmaceutical suspension of cefdinir crystal: The present invention relates to a novel oral pharmaceutical suspension of Cefdinir crystal. More specifically, the present invention relates to a novel kit for preparation of an oral pharmaceutical suspension containing crystal forrn C Cefdinir....

20060135504 - N-(substituted arylmethyl)-4-(disubstituted methyl) piperidines and pyridines: It has now been found that certain novel N-(substituted aryl)-4(disubstituted methyl)piperidine and pyridine derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): wherein m, n, q, r, and s are independently selected from 0 or 1; and p is 0, 1, 2, or 3; A is...

20060135505 - Tetrahydro-naphthalene derivatives as vanilloid receptor antagonists: in which the variable groups are as defined in the specification and claims, and tautomeric and stereoisomeric forms and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have an excellent activity as VR1 antagonists and are useful for the prophylaxis...

20060135502 - Cyclic derivatives as modulators of chemokine receptor activity:

20060135503 - Cyclic derivatives as modulators of chemokine receptors activity:

20060135501 - Piperidinyl-thiazole carboxylic acid derivatives as angiogenesis inhibitors: This invention relates to compounds of formula (I) and (II) that are useful in treating vascular endothelial growth factor (VEGF)-mediated disorders, particularly endometriosis and acute macular degenerative disorder. The invention also relates to a topical system for the treatment of acute macular degenerative disorder comprising a VEGF inhibitor....

20060135506 - Compositions of a cyclooxygenase-2 selective inhibitor and a calcium modulating agent for the treatment of pain, inflammation or inflammation mediated disorders: The present invention provides compositions and methods for the treatment of pain, inflammation or inflammation mediated disorders in a subject. More particularly, the invention provides a combination therapy for the treatment of pain, inflammation or inflammation mediated disorders comprising the administration to a subject of a calcium modulating agent in...

20060135507 - Therapeutic agent for overactive bladder involved in aging: A method for treating overactive bladder involved in aging, comprising administrating a compound having a cholinesterase inhibitory activity, a pharmacologically acceptable salt or a solvate thereof to a patient with the overactive bladder involved in aging....

20060135508 - Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them: The present invention provides a method for treating diseases caused by and/or associated with an altered protein kinase activity which comprises administering to a mammal in need thereof an effective amount of a pyrrolo-pyrazole or pyrazolo-azepine. The invention also provides specific pyrrolo-pyrazoles and pyrazolo-azepines, useful intermediates, a library comprising at...

20060135509 - Method of treating neurological diseases and disorders: The present invention provides methods for treating neurological diseases and disorders. Compounds that replace or enhance the function of SMN or alleviate or reduce a phenotype of cells with low SMN protein levels are provided. Screening methods and kits for identifying such compounds also are provided....

20060135510 - Use of amprenavir as a radiation sensitizer: The present invention relates to the sensitization of a cell to radiation. In particular, the present invention relates to the use of a protease inhibitor to sensitize a cancer cell to radiation....

20060135511 - Benzodiazepine cgrp receptor antagonists: The present invention is directed to compounds of Formula I: I (where variables R1?, R/ 2?, R3?, R 4?, R6?, R7?, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases...

20060135512 - Aminocycloalkanes as dpp-iv inhibitors: e

20060135513 - Methods of treating tumors: The invention provides a method of inhibiting tumor growth in a mammal, by administering to the mammal composition containing taurolidine, taurultam, or a biologically active derivative thereof. The composition is administered to directly contact a tumor cell at a dose sufficient to induce cell death by apoptosis....

20060135514 - Pyrazolo[1,5-a]pyrimidine derivatives: The Pyrazolo[1,5-a]pyrimidine derivatives represented by formula I and their pharmaceutically acceptable salts exhibit excellent MAPKAP-K2 inhibiting activity. Drugs comprising the compounds as effective ingredients are therefore expected to be useful as therapeutic or prophylactic agents for MAPKAP-K2 mediated disorder, such as inflammatory disease, autoimmune disease, destructive bone disorder, cancer and/or...

20060135515 - Heterocyclic amides and their use treating thromboembolic diseases and tumors: Novel compounds of the formula (I), in which D, W, X, Y, T and R1 have the meaning indicated in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours...

20060135516 - 3-(carbonyl) 1h-indazole compounds as cyclin dependent kinases (cdk) inhibitors: The invention provides a compound of the formula (I): wherein E is O, S, or NH; G is selected from hydrogen; carbocyclic and heterocyclic groups having from 3 to 12 ring members; and acyclic C1-8 hydrocarbyl groups optionally substituted; provided that E—G is not OH or SH and further provided...

20060135517 - Imidazolopyridines and methods of making and using the same: Compounds of formula I possess unexpectedly high affinity for Alk 5 and/or Alk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders. In one embodiment, the invention features a compound of formula I:...

20060135518 - Pyrimidine compounds and uses thereof: m

20060135519 - 5-aryltetrazole compounds and compositions thereof:

20060135521 - Method of treating chronic fatigue syndrome: Methods and compositions for treating humans suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or a condition where inhibiting reuptake of norepinephrine is a benefit are disclosed. The compositions comprise a compound having a pharmacological selectivity of serotonin (Ki)/norepinephrine (Ki) of at least about...

20060135520 - Method of treating peripheral neuropathy: Methods and compositions for treating humans suffering from or preventing a human from suffering, a physiological or psychiatric disease, disorder, or a condition where inhibiting reuptake of norepinephrine is a benefit are disclosed. The compositions comprise a compound having a pharmacological selectivity of serotonin (Ki)/norepinephrine (Ki) of at least about...

20060135522 - Tricyclic delta-opioid modulators: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic δ-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described....

20060135523 - 2-substituted 5,6-diaryl-pyrazine derivatives as cb1 modulator: The present invention relates to 2-substituted-5,6-diarylpyrazine compounds and their compositions, processes for their preparation, and their use in the treatment of obesity and psychiatric and neurological disorders....

20060135524 - Tricyclic delta-opioid modulators: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic δ-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described....

20060135526 - Pyrazolo [1,5-a] pyrimidine adenosine a2a receptor antagonists: R7 is alkyl, optionally substituted phenyl, optionally substituted heteroaryl, cycloalkyl, halo, morpholinyl, optionally substituted piperazinyl, or optionally substituted azacycloalkyl. Also disclosed is the use of the compounds in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, pharmaceutical compositions comprising them and kits...

20060135525 - Pyrazolopyrimidine compound and a process for preparing the same: The present invention provides a novel pyrazolopyrimidine compound of the formula [I]: wherein R′ is (A) a substituted aryl group, (B) an optionally substituted nitrogen-containing aliphatic heteromonocyclic group, (C) a substituted cyclo-lower alkyl group, (D) an optionally substituted amino group, or (E) a substituted heteroaryl group, R2 is (a) an...

20060135527 - Use of imatinib (glivec,sti-571) to inhibit breast cancer resistance protein (bcrp)-mediated resistance to therapeutic agents: e

20060135528 - Piperazinyl-pyridine derivatives: wherein R1, R2, X, Y, Z and m are as defined in the description and claims, and pharmaceutically acceptable salts thereof as well as to pharmaceutical composition comprising these compounds and to methods for their preparation. The compounds are useful for the treatment and/or prevention of diseases which are associated...

20060135529 - Pharmaceutical compositions comprising thieno[2,3-c]pyridine derivatives and use thereof: The present invention provides thieno[2,3-C]pyridine derivatives, pharmaceutical compositions comprising the thieno[2,3-C]pyridine derivatives, and methods of use thereof. The compounds capable of inhibiting glycosaminoglycan (GAG) interactions with effector cell adhesion molecules (ECAM) are useful for treating diseases and disorders mediated by GAG-ECAMs interactions, particularly inflammatory and autoimmune diseases, viral diseases, cancer,...

20060135530 - Fused heterocyclic compounds: A compound represented by the formula wherein ring A is an optionally substituted 5- to 10-membered aromatic ring; R1 and R2 are the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X and Y are the same or different and each...

20060135531 - Modulators of dopamine neurotransmission: wherein R1 is selected from the group consisting of OSO2CF3, OSO2CH3, SO2R3, COCF3, COCH3 and COCH2CH3, wherein R3 is as defined hereafter; R2 is selected from the group consisting of C1-C4 alkyls, allyl, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl and 4,4,4-trifluorobutyl; R3 is selected from the group consisting of C1-C3 alkyls, CF3, and...

20060135532 - Platelet adenosine diphosphate receptor antagonists: e

20060135533 - Compound preparation for dizziness: The use of cinnarizine and dimenhydrinate or their physiologically compatible salts in combination is described for the treatment of vertigo of any genesis....

20060135535 - Phosphodiesterase 4 inhibitors: e

20060135534 - Pyrazine based inhibitors of glycogen synthase kinase 3: New bicyclic based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in...

20060135536 - Ion channel modulating activity i: Methods, compositions, dosing regimes, and routes of administration for the treatment or prevention of arrhythmias. In these methods, early afterdepolarizations and prolongation of QT interval may be reduced or eliminated by administering ion channel modulating compounds to a subject in need thereof. The ion channel modulating compounds may be cycloalkylamine...

20060135537 - Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing the compounds of the invention....

20060135538 - 7-(r)-aminotriazolopyrimidines, their preparation and their use for controlling phytopathogenic fungi: e

20060135539 - Thienopyridazinones and their use in modulation of autoimmune disease: The invention relates to thienopyridazinones compound of formula (I) wherein: R1, R2 and Q are as defined in the specification, and Ar and Ar2 are selected from certain aromatic ring systems which may be optionally substituted, as defined in the specification. Processes for the preparation of compounds of formula (I),...

20060135540 - Ppar active compounds: Compounds are described that are active on at least one of PPARα, PPARδ, and PPARγ, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPARα, PPARδ, and PPARγ....

20060135541 - (3-((quinazolin-4-yl) amino)-1h-pyrazol-1-yl)acetamide derivatives and related compounds as aurora kinase inhibitors for the treatment of proliferative diseases such as cancer: Quinazoline derivatives of formula (I) for use in the treatment of proliferative diseases such as cancer and in the preparation of medicaments for use in the treatment of proliferative diseases, and to processes for their preparation, as well as pharmaceutical compositions containing, them as active ingredient. X is O or...

20060135543 - 2,4-pyrimidinediamine compounds and their uses: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized...

20060135542 - Gtpase inhibitors and use thereof for controlling platelet hyperactivity: The preferred embodiments generally relate to methods and compositions that affect the GTP-binding activity of members of the Rho family GTPases, preferably Rac (Rac1, Rac2 and/or Rac3), such compositions include compounds that modulate the GTP/GDP exchange activity, along with uses for the compounds including screening for compounds which recognize Rac...

20060135544 - Novel synthesis of irbesartan: Provided are a method of making irbesartan via a Suzuki coupling reaction and a novel intermediate, 2-butyl-3-(4′-bromobenzyl)-1,3-diazaspiro[4.4]non-1-ene-4-one, for such process. The novel process includes the step of reacting such intermediate with a protected imidazolephenylboronic acid....

20060135545 - Benzo[b]pyrano[3,2-h]acridin-7-one cinnamate compounds: R5 represents hydrogen, ORc, NRcRd, W1—C(W2)—U—V, W1—C(W2)—W3-T1 or Z-CO—CH═CHAr wherein Rc, Rd, W1, W2, W3, U, V, T, Z and Ar are as defined in the description, its isomers, and addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful in...

20060135546 - Methods for the purification of 20(s)- camptothecin: The invention features scalable methods for the purification of (20S)-camptothecin....

20060135547 - Stable pharmaceutical compositions of desloratadine and processes for preparation of polymorphic forms of desloratadine: Provided are stable pharmaceutical compositions of desloratadine. Also provided are processes for preparing polymorphs of desloratadine...

20060135548 - Processes for producing crystalline macrolides: The present invention provides processes for crystallization of macrolides, specifically pimecrolimus and tacrolimus....

20060135549 - Rapamycin analogues and the uses thereof in the treatment of neurological, proliferative,and inflammatory disorders: e

20060135550 - Rapamycin derivatives and the uses thereof in the treatment of neurological disorders:

20060135551 - Novel heterocyclic compounds and their pharmaceutical compositions: The present invention provides, among other things, new bicyclic heterocyclic compounds, compositions comprising these heterocyclic compounds, methods of making the heterocyclic compounds, and methods of using these heterocyclic compounds for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism....

20060135552 - Thieno-pyridine derivatives as allosteric enhancers of the gabab receptors: wherein R1, R2, R3, R4, and R5 are as defined in the specification. Compounds of the invention are active on the GABAB receptor and are useful for treating a variety of CNS disorders, including anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity-and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic...

20060135553 - Imidazole derivatives: Certain imidazole-containing compounds are useful for treating and/or preventing of various disease conditions, by way of methodology for modulating tyrosine kinases and angiogenesis. Illustrative of such conditions are inflammatory diseases and diseases characterized by abnormal cellular proliferation....

20060135554 - Novel compounds: r

20060135555 - Ring fused pyrazole derivatives as crf antagonists: wherein Ar is optionally substituted aryl or heteroaryl, R1-R4 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts thereof. The invention further relates to processes for preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for their...

20060135556 - Non-nucleoside reverse transcriptase inhibitors: Various carbonyl amides are employed in vitro and in vivo as non-nucleoside inhibitors of a reverse transcriptase, and particularly of HIV reverse transcriptase. Therefore, contemplated compounds may be employed in the treatment of HIV infected patients. Further contemplated aspects include pharmaceutical compositions comprising therapeutically effective amounts of contemplated compounds....

20060135557 - Isoquinoline-1,3,4-trione compounds, the synthetic method and the use thereof: The invention relates to various substituted isoquinoline-1,3,4-trione, the synthetic method thereof and the use for treating neurodegenerative diseases, especially as the medicine for Alzheimer's disease, apoplexy and brain ischemic injuries....

20060135558 - Aroyl-piperidine derivatives: The invention relates to novel N-(3,5-bis-trifluoromethyl-benzoyl)-2-benzyl-4-(quinoloylamino)-piperidines of the formula . . . wherein Y and R each are as defined above and the ring A is unsubstituted or mono- or polysubstituted by substituents selected from the group consisting of lower alkyl, lower alkoxy, halogen, nitro and trifluoromethyl; and the salts...

20060135559 - Novel imidazoline compounds: and R2 and R3are each hydrogen, lower cycloalkyl, lower alkenyl, or optionally substituted lower alkyl (with the proviso that when R2 and R3 are simultaneously hydrogen, Ar1, Ar2 and R1 do not simultaneously represent unsubstituted phenyl). The compounds are useful as treating agents for various NPY-related diseases, for example, circulatory...

20060135561 - 4-aminopiperidine derivatives: wherein R1 and R2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP-IV, such as diabetes, non-insulin dependent diabetes mellitus and/or impaired glucose tolerance, obesity, and/or metabolic syndrome or β-cell...

20060135560 - Prevention and treatment of cardiovascular pathologies with tamoxifen analogues: wherein Z is C═O or a covalent bond; Y is H or O(C1-C4)alkyl, R1 and R2 are individually (C1-C4)alkyl or together with N are a saturated heterocyclic group, R3 is ethyl or chloroethyl, R4 is H, R5 is I, O(C1-C4)alkyl or H and R6 is I, O(C1-C4)alkyl or H with...

20060135562 - Method for treating hiv infection through co-administration of tipranavir and darunavir: A method for treating HIV infection through co-administration of tipranavir and darunavir....

20060135563 - Method for treating hiv infection through co-administration of tipranavir and sch-417690: A method for treating HIV infection through co-administration of tipranavir and SCH-417690....

20060135564 - Insecticidal compositions comprising compounds having inhibitory activity versus acyl coa: cholesterol acyltransferase or salts thereof as effective ingredients: The present invention relates to insecticidal compositions comprising compounds having an inhibitory activity versus acyl CoA:cholesterol acyltransferase (ACAT) or salts thereof as effective ingredients. The compounds having inhibitory activity versus ACAT have an excellent insecticidal effect by inhibiting sterol metabolism in noxious insects. Therefore, the compounds of the present invention...

20060135565 - Crystalline form of rabeprazole sodium: Rabeprazole sodium in crystalline hydrate forms, a pharmaceutical composition containing them, their use in therapy, a process for their preparation, and the use thereof for the purification of rabeprazole sodium....

20060135566 - 5-pyridyl-1,3-azole compounds, process for producing the same and use thereof: wherein R1 represents hydrogen, hydrocarbon, heterocycle, amino, acyl, R2 represents an aromatic group, R3 represents hydrogen, pyridyl, aromatic hydrocarbon, X represents oxygen, optionally oxidized sulfur, Y represents a bond, an oxygen, optionally oxidized sulfur, a group represented by the formula NR4 (R4 represents hydrogen, hydrocarbon or acyl) and Z represents...

20060135567 - Comprehensive pharmacologic therapy for treatment of obesity: The comprehensive pharmacologic therapy for treatment of obesity is a procedure which involves the administration of a desired therapeutic range of Diethylpropion and/or Phentermine in combination with a SSRI medication and nutritional supplementation for brief and long durations which may be 12 months or more. The preferred procedure involves the...

20060135568 - Methods of treating microbial infections in humans and animals: A method of treating a subject with a microbially-based infection, comprising the administration of a compound to the subject. The compound is able to decrease ATP levels in the microbe by at least 10% compared to controls after 24 hours in an in vitro test, without killing mammalian cells during...

20060135569 - Use of benzisoselenazolone compounds against ischemic myocardial damage: The invention discloses use of benzisoselenazolones, particularly compounds represented by the general formula (I) against ischemic myocardial injury. The compounds are characterized by selectively inhibiting Na+/Ca2+ exchange, dilating coronary artery and decreasing myocardial oxygen consumption, which possess the advantages of high activity, potent specificity and low toxicity....

20060135570 - Cyclic sulfamides for inhibiton of gamma-secretase: e

20060135571 - Imidazo(2,1-b)-1,3,4-thiadiazole sulfoxides and sulfones: This invention relates to novel imidazo[2,1-b]-1,3,4-thiadiazole sulfoxide and sulfone compounds of Formula (I) and the use of compounds of Formula (I) in the treatment of neuronal disorders of the central and peripheral nervous systems and for the treatment of proliferative diseases such as cancer....

20060135572 - Casr antagonist: i

20060135573 - Benzothiazole-4,7-diones and benzoxazole-4,7-diones with substituents in position 5 or 6 and method for production thereof: A subject of the invention is a selective process for the preparation of derivatives of benzothiazole-4,7-diones and benzoxazole-4,7-diones monosubstituted in position 5 or in position 6 by an amino group itself optionally substituted. Said derivatives are inhibitors of the Cdc25 phosphatases and can be used for preparing medicaments intended to...

20060135574 - Novel uses for estrogen beta agonists: This invention provides methods for treating cognitive diseases or disorders and symptoms thereof with estrogen beta selective agonists....

20060135575 - 2-acylamino-4-phenylthiazole derivatives, preparation thereof and therapeutic application thereof: i

20060135576 - Heterocyclic inhibitors of kinases: and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth...

20060135577 - Remedy for chronic disease: A remedy and/or a preventive for a chronic disease which contains an EDG-2 antagonist. Because of binding to a subtype EDG-2 of LPA receptor, an EDG-2 antagonist is useful in treating and/or preventing chronic diseases (for example, diseases caused by the progress of chronic asthma, glomerular nephritis, obesity, arteriosclerosis, rheumatoid...

20060135578 - Five-membered heterocyclic compounds: wherein R1 is an optionally substituted 5-membered heterocyclic group; X, Y and V are the same or different and each is a bond, an oxygen atom, a sulfur atom and the like; Q is a divalent hydrocarbon group having 1 to 20 carbon atoms; ring A is an aromatic ring...

20060135579 - Compositions that bind antiterminator rna and assay for screening for such compositions: Compounds that are selective binding agents specific for RNA secondary and tertiary structures and a fluorescence assay for detecting the binding of small molecules to T-box antiterminator model mRNAs. The compounds include novel tri-substituted oxazolidinones and amino alcohols. The assay provides fluorescently labeled model mRNAs that include conserved sequence information...

20060135580 - Novel method for preparing styryl pyrazole, isoxazole and isothiazole derivatives: The invention concerns a method for synthesizing styryl isoxazole, styryl pyrazole and styryl isothazole derivatives in a synthesis step followed by a recrystallization in a basic alcohol medium....

20060135581 - Oxime derivative substituted hydroxyethylamine aspartyl protease inhibitors: The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein....

20060135582 - Process for the preparation of benzo [d] isoxazol-3-yl-methanesulfonic acid and the intermediates thereof: A process for the preparation of benzo[d]isoxazol-3-yl-methanesulfonic acid of formula (I), or a salt thereof, and the intermediates thereof, useful as an intermediate in the preparation of zonisamide....

20060135583 - Imidazolidine derivatives: wherein n is an integer selected from 1 to 20, and R1 and R2, which may be the same or different, each represent a hydrogen atom, or a linear or branched C1-C6 alkyl group, or a salt, a prodrug or a solvate thereof, as well as a drug, a pharmaceutical...

20060135585 - Compounds and methods for thiol-containing compound efflux and cancer treatment: Methods for therapy of cystic fibrosis and other conditions such as cancer are provided. The methods comprise one or more agents capable of increasing thiol-containing compound transport via a transporter system (i.e. ABC transporters such as MDR-1 or MRP-2) in cells. Other embodiments include the use of agents to modulate...

20060135584 - Novel imidazole alcohol compound, process for producing the same, and surface-treating agent comprising the same: (In general formula (1), R1, R2 and R3 are each hydrogen, a vinyl group or an alkyl group with 1 to 20 carbon atoms, an aromatic ring may be formed by R2 and R3, X indicates hydrogen, an alkyl group with 1 to 6 carbon atoms, or a substituent group...

20060135586 - Stabilized polymeric thiol reagents: Disclosed are water soluble polymeric reagents comprising the structure POLY-[Y—S—W]x, where POLY is a water soluble polymer; Y is a hydrocarbon-based spacer group, x is 1 to 25, and S—W is a thiol, protected thiol, or thiol-reactive derivative. Preferably, the water soluble polymer is a PEG polymer. Also disclosed are...

20060135587 - Method and compounds for promoting healing and reducing inflammation: This invention relates to methods of promoting healing and reducing inflammation, and compositions therefore. In particular, the invention relates to the use of 1,3-dialkyl-4,5-bis(N-methylcarbamoyl)imidazolium salts to promote wound healing and to reduce inflammation. Novel compounds and compositions are also provided. In one preferred embodiment the invention provides a method of...

20060135588 - Preventive and/or therapeutic drugs for inflammatory intestinal diseases: wherein R1 represents a hydrogen atom, an aryl group, an alkyl group, or an alkoxycarbonylalkyl group; R2 represents a hydrogen atom, an aryloxy group, an arylmercapto group, an alkyl group or a hydroxyalkyl group; or R1 and R2 are combined with each other to represent an alkylene group; and R3...

20060135589 - 1h-indazole-3-carboxamide compounds as cyclin dependent kinase (cdk) inhibitors: e

20060135590 - Selected fused pyrrolocarbazoles: The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles....

20060135592 - Indolinones and their use as antiproliferative agents: e

20060135591 - Modulators of crth2 activity: Modulators of the CRTH2 receptor and their use in the treatment of various disorders, including asthma are described....

20060135593 - N-acyl nitrogen heterocyles as ligands of peroxisome proliferator-activated receptors: provide pharmacological agents which bind to Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity,...

20060135596 - Amorphous form of a drug: Substantially amorphous atrasentan hydrochloride, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed....

20060135595 - Bis(thio-hydrazide amide) salts for treatment of cancers: Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group. R1-R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded,...

20060135594 - Prodrugs of mitotic kinesin inhibitors: The present invention relates to phosphate ester prodrugs of dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer...

20060135597 - Large conductance calcium-activated k channel opener: R1 is aryl, heterocyclic or heterocycle-substituted carbonyl; R2 is hydrogen, halogen, carboxy, amino, alkyl, alkoxycarbonyl, alkenyl or cycloalkyl; R3 is aryl, heterocyclic or alkyl; and R4 is hydrogen or alkyl, each of substituents may be substituted, or a pharmaceutically acceptable salt thereof as an active ingredient....

20060135598 - Anti-first-pass effect compounds: Safe, effective first-pass inhibiting compounds and citrus-derived substances are provided. Formulations containing the compounds are also provided as are methods for inhibiting the first pass effect....

20060135599 - Use for pharmaceutical composition: The invention relates to the use of one or more cannabinoids in the treatment of neuropathic or chronic pain....

20060135600 - Method for inhibition of necrosis induced by neurotrophin: Disclosed is a method for inhibition of necrosis induced by neurotrophin, and more specifically a method for inhibition of necrosis by administrating oxidative stress inhibitor and a method for simultaneous inhibition of necrosis and apoptosis by administrating oxidative stress inhibitor and neurotrophin. The oxidative stress inhibitor of the present invention...

20060135601 - Novel hexafluoroisopropanol substituted cyclohexane derivatives: s

20060135602 - Novel derivatives of 4,4'-dithiobis-(3-aminobutane-1-sulfphonates) and compositions containing same: The invention relates to the bis-hydrochloride of 4,4′-dithiobis-(3-aminobutane-1-sodium sulphonate) and the bis-trifluoracetate of 4,4′-dithiobis-(3-aminobutane-1-sulphonate of 2,2-dimethylpropyl). The invention also relates to a pharmaceutical composition comprising one of said compounds and to the use of one of said compounds for the production of a medicament. The invention is suitable for use...

20060135603 - Methods for identifying and using ikk inhibitors: The present invention provides methods and compositions for inhibiting IKK, as well as methods and compositions for identifying compounds with activity as inhibitors of IKK, and methods and compositions for the treatment of diseases and/or conditions wherein IKK is implicated and inhibition of its activity is desired. In addition, the...

20060135604 - Pharmaceutical compositions of isolated orthorhombic crystalline 4-[6-acetyl-3-[3-(4-acetyl-3-hydroxy-2-propylphenylthio)propoxy]-2-propylphenoxy]butyric acid and methods of use: e

20060135605 - Intermediates in producing phenoxyacetic acid derivatives and method of using the same: The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has β3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary...

20060135607 - Drug for improving prognosis for subarachnoid hemorrhage: It is intended to provide a drug for improving prognosis for subarachnoid hemorrhage which contains, as the active ingredient, at least one member selected from the group consisting of eicosapentaenoic acid (EPA) and pharmaceutically acceptable salts and esters thereof, and a method of improving prognosis for subarachnoid hemorrhage which comprises...

20060135606 - Use of carnitines for the prevention and/or treatment of disorders caused by the andropause: The use of propionyl L-carnitine in combination with acetyl L-carnitine, or one of their pharmaceutically acceptable salts, is disclosed for the preparation of a medicament, or of a nutritional supplement, for the prevention and/or treatment of the disorders of the male andropause caused by ageing or by chemical or surgical...

20060135608 - Eicosapentaenoic acid (epa) for treating anorexia nervosa (an) and bulimia: Eicosapentaenoic acid (EPA) is used in the treatment of anorexia nervosa, bulimia and related clinical syndromes....

20060135609 - Ophthamological drugs: The present invention relates generally to ophthamological drugs. More specifically, the inventon relates to a method of modifying (derivatizing) ophthamological drugs so as to increase their penetration through the cornea. The invention also relates to drugs modified (derivatized) in accordance with the instant method and to the use of same...

20060135610 - Cardiovascular compositions: Compositions that promote and/or maintain cardiovascular health through the treatment of one or more cardiovascular diseases are provided. Also provided are methods for using compositions that promote and/or maintain cardiovascular health through the prevention, stabilization, reversal and/or treatment of coronary artery disease and/or cerebrovascular disease. Such compositions may be used...

20060135611 - Use of 2,5-dihydroxybenzenesulfonic compounds for the treatment of disorders based on an impairment of no production and/or of regulation of edhf function: The present invention relates to the use of 2,5-dihydroxybenzenesulfonic compounds for the manufacture of a medicament for the regulation of nitric oxide (NO) synthesis and/or the regulation of EDHF (Endothelium-Derived-Hyperpolarizing-Factor) in the endothelium of diabetic patients, whereby the medicament is administered in a daily dose of the 2,5-dihydroxybenzenesulfonic compounds of...

20060135612 - Method of ameliorating or abrogating the effects of a neurodegenerative disorder, such as amyotrophic lateral sclerosis (als), by using a hdac inhibiting agent: A method of ameliorating or abrogating the effects of a neurodegenerative disorder, such as amyotrophic lateral sclerosis (ALS), includes administering a histone deacetylase (HDAC) inhibitor in a subject in need thereof. The HDAC inhibitor includes sodium butyrate or sodium phenylbutyrate....

20060135613 - Carboxamides derivatives: The present invention relates to carboxamides which are useful as an active ingredient of pharmaceutical preparations. The carboxamides of the present invention have IP receptor antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with IP receptor antagonistic activity. Such diseases include urological diseases or...

20060135614 - Novel compounds: This invention relates to novel compounds, which are thyroid receptor ligands, and to methods of preparing such compounds. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a...

20060135615 - Deuterated catecholamine derivatives and medicaments comprising said compounds: The present invention concerns deuterated catecholamine derivatives as well as pharmaceuticals containing these compounds. In addition, the invention concerns the use of deuterated catecholamine derivatives as well as physiologically compatible salts thereof, and also pharmaceutical compositions, which contain these compounds, also in combination with enzyme inhibitors, for the treatment of...

20060135616 - Aromatic compositions for the inhibition of exoprotein production from gram positive bacteria: and salts thereof; R5 is a monovalent saturated or unsaturated aliphatic hydrocarbyl moiety; R6 is a divalent saturated or unsaturated aliphatic hydrocarbyl moiety; R7 is a trivalent saturated or unsaturated aliphatic hydrocarbyl moiety; R8 is a monovalent substituted or unsubstituted saturated or unsaturated aliphatic hydrocarbyl moiety which may or may...

20060135617 - Process for producing optically active flurbiprofen: The present invention provides a method for producing optically active flurbiprofen. The method of the present invention includes mixing racemic flurbiprofen and (S)- or (R)-3-methyl-2-phenylbutylamine in an organic solvent to produce a diastereomeric salt; and treating the diastereomeric salt with an acid in a second solvent. In the method of...

20060135618 - Medicine comprising a thiourea for use as depigmenting agent or anti-mutagenic and anti-carcinogenic agent: The invention concerns a medicine or a cosmetic composition comprising at least one thiourea of general formula (I), or at least one of its monooxide or dioxide derivatives of general formulae (IIa), (IIb) and (III), or mixtures thereof. This medicine is advantageously used for inhibiting tyrosinase, inhibiting melanin synthesis, for...

20060135619 - Anthranilic acid derivatives as inhibitors of 17beta-hydroxysteroid dehydrogenase 3: Anthranilic acid drivatives, methods of using such compounds in the treatment of hormone sensitive diseases such as prostate cancer, and pharmaceutical compositions containing such compounds....

20060135620 - Novel compounds for use in the treatment of autoimmune diseases, immuno-allergical diseases and organ or tissue transplantation rejection: The present invention provides compounds, pharmaceutical compositions and methods for treating, immuno-allergical diseases, autoimmune diseases, and organ or tissue rejection following transplantation....

20060135621 - Method for the production of crystalline forms and crystalline forms of optical enantiomers of modafinil: The invention relates to a process for the preparation of crystalline forms of the optical enantiomers of modafinil, comprising stages comprising: i) dissolving one of the optical enantiomers of modafinil in a solvent other than ethanol, ii) crystallising the modafinil enantiomer, iii) recovering the crystalline form of the modafinil enantiomer...

20060135622 - Amino alcohol derivative, addition salt thereof, and immunosuppressant: An amino alcohol derivative represented by the following general formula (1) (for example, (±)-2-amino-5-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-2-methylpentane-1-ol) exhibits strong immunosuppressive effect while causing less side effects:...

20060135623 - Decrease in oxidative stress status through the administration of natural products and pharmaceutical drugs: The present invention provides compositions, methods, and kits for reducing oxidative stress thereby extending life span. The compositions, methods, and kits of the present invention can also be used be used to treat diseases of aging resulting from oxidative stress....

20060135624 - Natural compound useful for treating diabetes, its preparation and use: The present invention relates to a process for preparing an antidiabetic natural compound and pharmaceutical use of said compound. An antidiabetic Sequoyitol powder is obtained by extracting a medicinal plant, such as Taxus spp, etc., with a solvent, and separating by diphase extraction and chromatography, and it is further purified...

20060135625 - Method of administering split doses of a vascular targeting agent: The present invention is directed to the use of vascular targeting agents or pharmaceutically acceptable salts thereof for administration in divided doses to a warm-blooded animal, such as a human. Also disclosed is a medicament comprising two or more fraction of doses of a vascular targeting agent, or a pharmaceutically...

20060128605 - Preventives/remedies for snore or respiratory disturbances during sleep: Compounds which have an agonist action on a glycine receptor and compounds capable of being present as glycine in living organisms are effective for the prophylaxis or treatment of snoring or respiratory disorders during sleep. Foods and diets which contain such a compound are also effective for the prophylaxis or...

20060128606 - Fibrils: An amyloid fibril substantially free of other protein is disclosed. Also disclosed are processes for preparing the fibril, and methods and uses of the fibril particularly in connection with treating diabetes, blood clotting disorders, cancer and/or heart disease....

20060128611 - Composition for enzyme inhibition: Compositions comprising one or more practically insoluble proteasome inhibitors and a cyclodextrin, particularly a substituted cyclodextrin, substantially increase the solubility of these proteasome inhibitors and facilitate their administration. Such compositions optionally comprise a buffer. Methods of treatment using such compositions are also disclosed....

20060128612 - Cross-linked glycopeptide-cephalosporin antibiotics: This invention provides cross-linked glycopeptide—cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds....

20060128607 - Method for inhibiting \"melanoma inhibitory activity\" mia: The present invention is directed to peptides, antibodies and antibody fragments inhibiting activity of “Melanoma Inhibitory Activity” (MIA)....

20060128610 - Methods of treatment: The inventions relate generally to methods for the prevention and treatment of conditions, diseases and disorders that would be improved, eased, or lessened by the administration of, for example, a composition comprising a therapeutically effective amount a glyponectin polypeptide, agonist, and/or nucleic acid constructs of the invention....

20060128609 - N¹- modified glycopeptides: Described herein are N′-acylated derivatives of desleucylA82846B. The compounds are useful as antibacterial agents....

20060128608 - Novel chemical compounds and their use: The present invention relates to prodrugs of pharmaceutical moieties, more specifically antimicrobial agents, methods for their preparation, pharmaceutical formulations containing them and their use in the treatment of microbial infections....

20060128614 - Antimicrobial peptides with reduced hemolysis and methods of their use: The present invention provides novel cyclic and linear short peptides containing one of the following amino acid residue sequences: Xa1-Naa-Xa1-Xa1-Naa-Xa2 or Xa1-Naa-Xa2-Xa1-Naa-Xa1 wherein: Xa1 represents lysine, arginine, or histidine; Naa represents an unnatural hydrophobic aromatic amino acid moiety selected from the group consisting of (naphtha-1-yl)alanine (1-Nal), (naphtha-2-yl)alanine (2-Nal), (benzothien-3-yl)alanine (Bal),...

20060128613 - Melanocortin receptor ligands: wherein R2, R4, R4′, R5, R6, R6′, R7, R8, R8′, R9, R9′, R10, Ar, Z1, Z2, Z3, X, B, D, p, q, r and s are as described in the specification and claims, and optical isomers, diastereomers or enantiomers thereof; pharmaceutically-acceptable salts, hydrates, and biohydrolyzable esters, amides or imides thereof....

20060128620 - Adrenocorticotropic hormone analogs and related methods: ACTH analog compounds of the present invention include compounds comprising an ACTH peptide sequence with one or more structural modifications that can have one or more of the following preferred ACTH analog biological functions: (1) reduction of corticosteroid secretion by adrenal membrane in the presence of the ACTH analog compared...

20060128615 - Ghrh analogues: The present invention relates to growth hormone-releasing hormone (GHRH) analogues. More particularly, the invention relates to synthetic GHRH analogues of 29 amino acids or more, exhibiting concomitantly an increased resistance to proteolysis and high binding affinity to human GHRH receptor in in vitro studies, in comparison with human native GHRH...

20060128623 - Granulysin peptides and methods of use thereof: Granulysin peptides are small antimicrobial agents with potent activity against bacteria and inflammation. A pharmaceutical composition comprising granulysin peptides as an active agent is administered therapeutically to a patient suffering from a microbial infection....

20060128627 - Human appetite control by glucagon-like peptide receptor binding compounds: A composition including a compound which binds to a receptor for glucagon-like peptide-1 and a pharmaceutical carrier. The amount of the compound present is effective to control appetite in a human. Also disclosed is a method for controlling appetite and for reducing food intake in a human by administering to...

20060128626 - Method of use of peptide antagonists of zonulin to prevent or delay the onset of diabetes: A method for preventing or delaying the onset of autoimmune diseases is disclosed....

20060128618 - Molecules which promote hematopoiesis: Peptides, methods for the preparation thereof, medicaments containing the peptides, and their use in selected indications, such as the treatment of various forms of anemia and stroke....

20060128617 - Oligoribonucleotide or peptidic nucleic acid inhibiting function of hepatitis c virus: A method of inhibiting the replication ability of a hepatitis C virus (HCV) is provided. An oligoribonucleotide or a peptide nucleic acid which sequence-specifically binds to the HCV-RNA, and a therapeutic agent for hepatitis C which contains any of these components as an active ingredient are provided....

20060128621 - Pharmaceutical composition of hydrophobically modified hedgehog proteins and their use: The object of the invention is to provide a pharmaceutical composition of a hydrophobically modified hedgehog protein containing a biocompatible carrier, wherein the carrier binds the hedgehog protein as an active folded structure and can release it locally in vivo in an active form in a delayed manner. Such formulations...

20060128624 - Pharmacokinetic and pharmacodynamic modeling of erythropoietin administration: The present invention relates to systems and methods for obtaining optimized EPO dosage regimens for a desired pharmacodynamic/pharmacokinetic response. The system includes choosing one or more EPO dosage regimens, then using a PK/PD model to determine the pharmacodynamic/pharmacokinetic profile of one or more EPO dosage regimens, and finally selecting one...

20060128625 - Povidone-containing carriers for polypeptide growth factors: A liquid carrier medium is provided which is suitable for solubilizing growth factors, such as mixtures of bone morphogenetic proteins, that are found to induce an angiogenic response in ischemic tissues. The liquid medium comprises an aqueous solution of polyvinyl pyrrolidone....

20060128616 - Process for the purification of tnf-binding proteins using imac: A new purification process for Tumor Necrosis Factor-binding proteins is described. In particular this process is characterized by the use as capture step of an Immobilized Metal Affinity Chromatography (IMAC) using copper as metal. This brings advantages in terms of process yields, purity of the final product and applicability to...

20060128622 - Therapeutic formulations of keratinocyte growth factor: The present invention provides long-term stable formulations of lyophilized keratinocyte growth factor and methods for making a lyophilized composition comprising keratinocyte growth factor....

20060128619 - Therapeutic use of modulators of notch: Provided is a method for modifying IL-4 expression in a cell using a modulator of Notch signalling. Also provided are methods for generating immune modulatory cytokine profiles with increased IL-4 expression and/or increased IL-10 expression and/or reduced IL-5, IL-13 and TNFα expression. In addition, a method for increasing a TH2...

20060128628 - Human tissue antigen-binding peptides and their amino acid sequences: The invention relates to a peptide that has epitopes with amino acid sequences selected from the S protein of SARS virus. Such peptides can bind human tissue antigen to form a complex, and can induce cytotoxicity. The invention relates further to a vaccine or diagnostic agent formed by combining said...

20060128629 - Partial peptide mimetics and methods: Partial peptide mimetics and methods of making and using, wherein the partial peptide mimetics have a first amino acid sequence comprising ANIKLSVQMKL (SEQ ID NO:8), a homolog thereof, or a segment of SEQ ID NO:8 or a homolog thereof, a second amino acid sequence comprising IIVKLND (SEQ ID NO:2), a...

20060128630 - At4 receptor ligands as angiogenic, anti-angiogenic, and anti-tumor agents: AT4 receptor agonists are potent activators of angiogenesis and can be used to treat diseases that are characterized by vascular insufficiency. AT4 receptor antagonists, which are potent inhibitors of angiogenesis, and can be used as anti-angiogenic agents for the treatment of cancer, diabetic retinopathy, rheumatoid arthritis, psoriasis, atherosclerotic plaque formation,...

20060128631 - Peptides and derivatives thereof showing cell attachment, spreading and detachment activity: The present invention relates to peptides and derivatives thereof showing cell attachment, spreading and detachment activity. Particularly, the present invention relates to the peptide NKDIL and EPDIM and derivatives thereof which promote the cell attachment activity through interaction with α3β1 integrin as a functional cell receptor and include aspartic acid...

20060128633 - Colchinol derivatives as vascular damaging agents: wherein X is —C(O)—, —C(S)—, —C═NOH, or —CH(R7)— wherein R7 is hydrogen, hydroxy, C1-7alkoxy, —OR8 or —NR8R9 (wherein R8 is a group —Y1R10 (wherein Y1 is a direct bond, —C(O)—, —C(S)—, —S—, —C(O)O—, —C(O)NR11—, —SO2— or —SO2NR12— (wherein R11 and R12, which may be the same or different, each independently...

20060128632 - Peptide inhibitors of smac protein binding to inhibitor of apoptosis proteins (iap): e

20060128634 - Alpha, alpha-disubstituted benzylglycine derivatives as hiv protease inhibitors: or a stereoisomeric form, a mixture of stereoisomeric forms, or a pharmaceutically acceptable salt thereof, which are useful as HIV protease inhibitors, pharmaceutical compositions and diagnostic kits including the same, methods for using the same for treating viral infection or an assay standards or reagents, and intermediates and processes for...

20060128636 - Breast cancer resistance protein (bcrp) inhibitor: [wherein, each of 8 R's, which are the same or different from one another, represents a hydrogen atom, a hydroxyl group, a nitro group, an amino group, an acetylamino group (—NHCOCH3 group); a cyano group (—CN group); a formyl group (—CHO group), —COOR1 (R1 is hydrogen or C1-C4 alkyl), —O(CH2)nCOOR2...

20060128637 - Phenolic acid complexes of hyoscyamine and process for preparing the same: The present invention provides a novel tannate complex of hyoscyamine for human and veterinary pharmaceutical use. Tannate complexes of active pharmaceutical ingredients are used in sustained release applications and to improve certain organoleptic properties such as taste. A process for preparing the tannate complex of hyoscyamine is provided....

20060128635 - Pyrazole derivative, medicinal composition containing the same, medicinal use thereof and intermediate in producing the same: and the other represents —(CH2)n—Ar wherein Ar represents an optionally substituted C6-10 aryl group or an optionally substituted C1-9 heteroaryl group; and n represents an integral number from 0 to 2, an optionally substituted C1-6 alkoxyl group, an optionally substituted amino group, an optionally substituted C2-9 heterocycloalkyl group or an...

20060128638 - Texaphyrin coordination compounds and uses thereof: Novel coordination polymers, their pharmaceutical formulations, useful for treating atheroma, tumors and other neoplastic tissue, as well as other conditions that are responsive to the induction of targeted oxidative stress, are disclosed....

20060128639 - Regulators of the hedgehog pathway, compositions and uses related thereto: The present invention makes available, inter alia, methods and reagents for modulating smoothened-dependent pathway activation. In certain embodiments, the subject methods can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function mutations....

20060128640 - Combination of a taxane and a cyclin-dependent kinase: The invention relates to a pharmaceutical combination comprised of paclitaxel (Taxol®), docetaxel (Taxotere®), or derivatives of them, and a cyclin-dependent kinase inhibitor. It also relates to a method of administration of such a combination, where the taxane is given intermittently and the cyclin-dependent kinase is given repeatedly within the same...

20060128642 - 9-ketospinosyn derivatives: The present invention relates to derivatives of 9-keto spinosyns, which are substituted by a ═N—(O, NH or NRx)—Ry moiety in the C-9 position, to methods for their manufacture, and to their use for controlling animal pests....

20060128641 - Levamisole, avermectins or similar in pyrrolidone solvent: A stable formulation which is suitable for administration to animals is claimed. The formulation includes at least one active selected from the group comprising avermectins and milbemycins and levamisole. Both of the actives are dissolved in a pyrrolidone solvent....

20060128643 - Compositions containing a combination of a creatine compound and a second agent: The present invention relates to the use of creatine compound and neuroprotective combinations including creatine, creatine phosphate or analogs of creatine, such as cyclocreatine, for treating diseases of the nervous system. Creatine compounds in combination with neuroprotective agents can be used as therapeutically effective compositions against a variety of diseases...

20060128650 - Allele-specific rna interference: Human diseases caused by dominant, gain-of-function mutations develop in heterozygotes bearing one mutant and one wild-type copy of a gene. Because the wild-type gene often performs important functions, whereas the mutant gene is toxic, any therapeutic strategy must selectively inhibit the mutant while retaining wild-type gene expression. The present invention...

20060128646 - Antisense design: A novel class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. These novel oligonucleotides have improved antisense properties. The novel oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or...

20060128649 - Aptamer-mediated regulation of gene expression: This invention provides methods of regulating gene expression. An aptamer is positioned in a nucleic acid molecule along with a sequence encoding a transcriptional regulatory polypeptide. The aptamer disrupts translation of the transcriptional regulatory polypeptide when contacted with an aptamer-binding ligand. Gene expression levels can be either increased or decreased...

20060128648 - Genetic suppression and replacement: A strategy for suppressing specifically or partially specifically an endogenous gene and introducing a replacement gene, said strategy comprising the steps of: 1. providing suppressing nucleic acids or other suppression effectors able to bind to an endogenous gene, gene transcript or gene product to be suppressed and 2. providing genomic...

20060128645 - Inhibition of proliferation and infiltration of brain tumor cells caused by expression of ampa-type glutamate receptor subunit: The present invention is to provide a method of treatment which inhibits proliferation and invasion of brain tumor cells in developing animal brain tumor cells, and a method for measuring proliferation/invasion activity of brain tumor cells, in the brain tumor cells, preferably, in glioblastoma. Proliferation and invasion of brain tumor...

20060128651 - Methods and compositions for modulating drug activity through telomere damage: The invention provides methods and compositions for modulating the activity of therapeutic agents for the treatment of a cancer by administering one or more agents that (either alone or in combination) induces telomere damage and inhibits telomerase activity in the cancer cell. The method initially uses, e.g., a telomere damage-inducing...

20060128647 - Novel oligonucleotides and treating cardiac disorders by using the same: Novel oligonucleotides and methods of treating a cardiac disease or disorder using the same are provided. The oligonucleotides are useful in modulating the expression of the connexin 43 protein and may be combined with other biologically active agents and compositions to treat cardiac disease. Methods of modulating connexin expression include...

20060128644 - Use of mob-5 in pain: The invention discloses Mob-5 as a suitable target for the development of new therapeutics to treat or ameliorate chronic pain. The invention relates to methods to treat and/or ameliorate chronic pain and pharmaceutical compositions therefor comprising modulators with inhibitory or stimulatory effect on Mob-5 activity and/or Mob-5 gene expression. The...

20060128652 - Purine derivatives and methods of use thereof: The invention relates to Purine Derivatives; compositions comprising an effective amount of a Purine Derivative; and methods for treating or preventing an ischemic condition, reperfusion injury, a cellular proliferative disorder, a cardiovascular disease, a neurological disorder, a skin disorder, a radiation-induced injury, a wound, or an inflammatory disease comprising administering...

20060128654 - Pharmaceutical formulation of cytidine analogs and derivatives: The present invention provides pharmaceutical formulations of cytidine analogs and derivatives, such as 5-azacytidine, 5-aza-2′-deoxy-2′,2′-difluorocytidine, 5-aza-2′-deoxy-2′-fluorocytidine, 2′-deoxy-2′,2′-difluorocytidine, and cytosine 1-β-D-arabinofuranoside, as well as methods of manufacturing the formulations. In particular, the cytidine analog or derivative is formulated with a cyclodextrin compound to stabilize and/or enhance solubility of the drug. Kits...

20060128653 - Pharmaceutical formulation of decitabine: The present invention provides pharmaceutical formulations of decitabine or 5-aza-2′-deoxycytidine as well as methods of manufacturing the formulations. In particular, decitabine is formulated with a cyclodextrin compound to stabilize and/or enhance solubility of the drug. Kits and methods for using the pharmaceutical formulations are also provided, including methods of administering...

20060128656 - Charged phospholipid compositions and methods for their use: The invention provides a pharmaceutical composition comprising a synthetic or naturally occurring charged phospholipid, which is formulated into a dosage form for administration to a subject or which is administered as a food additive. Negatively charged phospholipid composition increase the net negative charge on intravascular lipoproteins, enhance the clearance of...

20060128655 - Use of hyaluronic acid or its derivatives to enhance delivery of antineoplastic agents: A combination for administration to a mammal which combination employs a therapeutically effective amount of a medicinal and/or therapeutic agent to treat a disease or condition and an amount of hyaluronic acid and/or salts thereof and/or homologues, analogues, derivatives, complexes, esters, fragments and subunits of hyaluronic acid sufficient to facilitate...

20060128657 - Selected betaines and their uses: A physiologically acceptable, sterile and pyrogen-free solution of betaine dissolved in a physiologically acceptable solvent, having a pH adjusted to from 5.0 to 8.0 with a betaine concentration of from 5 to 500 mg/ml....

20060128658 - Biocompatible dialysis fluids containing icodextrins: Icodextrin-based solutions and methods of making same that can be used during medical therapy, such as dialysis therapy are provided. The icodextrin-based solution at least includes a first solution containing icodextrin at a pH ranging from about 1.5 to about 5.0 and a buffer solution at a pH ranging from...

20060128659 - Sulfotransferase inhibitors: wherein R1, R2 and R5 each independently represents SO3− or H, and at least one of them represents SO3−; R3 represents H, acetyl or SO3−; R4 represents H, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group, a substituted or unsubstituted...

20060128660 - Fk228 analogs and methods of making and using the same: The present invention provides FK228 analogs and methods of making and using the same. Such analogs are potent inhibitors of histone deacetylase and, in certain embodiments, are capable of specifically targeting cancerous cells and tissues. In preferred embodiments, these analogs are characterized by a cyclic disulfide design....

20060128661 - Novel substituted 1h-pyrrolo[2,3-b]pyridines and preparation thereof: e

20060128663 - Aryl boronate functionalized polymers for treating obesity: Ar in Structural Formulas (I) and (II) is substituted or unsubstituted; and each Z is —O—, —NH— or —S— and is independently selected. Pharmaceutically acceptable salts of the polymer are also included. The aryl boronate ester, boronamide or boronate thioester can be cleaved to release the corresponding aryl boronic acid....

20060128664 - Aryl boronic acids for treating obesity:

20060128662 - Novel compounds for treatment of obesity:

20060128665 - Marine lipid compositions: There is described marine phospholipids (MPL) compositions suitable for human, aquaculture applications comprising a dry composition comprising nutritional components selected from the group consisting of marine phospholipids, marine proteins and amino acid blends obtainable by fluid extraction of a dried marine raw material. The compositions have low amounts of neutral...

20060128666 - Use of sphingomyelin and lyso-sphingomyelin as absorption enhancers: The invention relates to agents to improve the uptake of nutrients and medicines, and more in particular to sphingomyelin and/or lysosphingomyelin for use in a pharmaceutical preparation to improve the uptake of certain nutrients and pharmaceutically active substances. The present invention provides a pharmaceutical preparation in which sphingomyelin and/or lysosphingomyelin...

20060128667 - Hydroxyphosphonates and phosphonophosphates as apolipoprotein e modulators: The present invention relates to the novel hydroxyphosphonates and phosphonophosphates and the methods of their use to modulate apolipoprotein E levels and the use of such compounds in therapy, including cardiovascular and neurological disease states....

20060128668 - Pancratistatin cyclic phosphate prodrugs an phenpanstatin cyclic phosphate prodrugs: Selective phosphorylation of phenpanstatin (3a) with tetrabutylammonium dihydrogen phosphate and dicyclohexyl-carbodiimide in pyridine followed by cation exchange chromatographic procedures was found to provide an efficient route to a new series (3b-3d) of promising 3,4-O-cyclic phosphate prodrugs designated phenpanstatin phosphates. Application of analogous reaction conditions to pancratistatin (1a) led to a...

20060128669 - Heterocyclic compounds having inhibitory activity against hiv integrase: l

20060128670 - Pesticidally active ketone and oxime derivatives: Compounds of formula (I), wherein A0, A1, and A2 are each independently of the others a bond or a C1-C6alkylene bridge; A3 is a C1-C6alkylene bridge which is unsubstituted or substituted by from one to six identical or different substituents selected from halogen and C3-C8cycloalkyl; Y is, for example, 0,...

20060128671 - Compositions containing a combination of a creatine compound and a second agent: The present invention relates to the use of creatine compound and neuroprotective combinations including creatine, creatine phosphate or analogs of creatine, such as cyclocreatine, for treating diseases of the nervous system. Creatine compounds in combination with neuroprotective agents can be used as therapeutically effective compositions against a variety of diseases...

20060128672 - Methods for the administration of amifostine and related compounds: The present invention provides methods of administering amifostine, WR-1065, or a combination thereof, to patients receiving radiation therapy or chemotherapy in a manner that significantly reduces or decreases the adverse or undesirable side-effects of the compounds as compared with conventional intravenous administration....

20060128673 - Pharmaceutical compositions comprising cb1 cannabinoid receptor antagonists and potassium channel openers for the treatment of obesity and related conditions: Described is a novel combination therapy for diabetes mellitus type I and/or for obesity and its concomitant and/or secondary diseases or conditions, in particular the metabolic syndrome and/or syndrome X, and/or diabetes mellitus type II, by administering a combination of at least one KATP channel opener as a first active...

20060128674 - Intermediates for imidazonaphthyridines: Imidazonaphthyridine and tetrahydroimidazonaphthyridine compounds induce the biosynthesis of cytokines such as interferon and tumor necrosis factor. The compounds exhibit antiviral and antitumor properties. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are disclosed....

20060128675 - Method for monitoring the effectiveness of teracycline in the treatment of asthma: The present invention is directed to a method of lowering excess IgE levels in a mammal suffering from a disease where IgE is pathogenic which method comprises administering to said mammal an IgE lowering effective amount of a tetracycline such as minocycline or doxycline. It is also directed to a...

20060128676 - Compositions of nicotinic agonists and therapeutic agents and methods for treating or preventing diseases or pain: Disclosed herein are compositions of nicotinic agonists, salts, hydrates, solvates or prodrugs thereof and therapeutic agents salts, hydrates, solvates or prodrugs thereof, pharmaceutical compositions thereof and methods of using these compositions and pharmaceutical compositions thereof to treat or prevent disease or pain in a subject. Also disclosed are methods of...

20060128677 - Compounds, compositions and methods for preventing neurodegeneration in acute and chronic injuries in the central nervous system: The present invention provides compositions and methods for prevention and prophylaxis of neurological diseases accompanied by neuronal death. The invention includes synthesis of 5-benzylamino salicylic acid (BAS) and its derivatives. BAS and its derivatives protect cortical neurons from toxic insults by N-methyl-D-aspartate, Zn2+, and reactive oxygen species. Thus, the present...

20060128678 - Manganese based organometallic complexes, pharmaceutical compositions and dietetic products: The invention relates to compounds and their uses, particularly in the pharmaceutical and dietetic industries. The invention discloses complexes having Mn-SOD like activities, as well as methods for treating various diseases associated with oxidative stress, including cancer and inflammatory conditions, by administering said compounds. It further deals with pharmaceutical compositions...

20060128679 - Method for treatment of dysmenorrhea: A method of treatment of dysmenorrhea in the context of oral contraception characterized by daily administration of ethinylestradiol and drospirenone in an extended regimen....

20060128680 - Macrocyclic module compositions: Macrocyclic module compositions are made from cyclic synthons. The macrocyclic module structures are prepared by stepwise or concerted schemes which couple synthons in a closed ring. The macrocyclic module structures may have a pore of nanometer dimensions....

20060128682 - Compounds and methods for the treatment of cancer: The present invention provides organic arsenicals. Many of these compounds have potent in vitro cytotoxic activity against numerous human tumor cell lines, both of solid and hematological origin, as well as against malignant blood cells from patients with leukemia....

20060128681 - Novel rho inhibitors: Rho is an enzyme essential for the growth and survival of Escherichia coli, and bicyclomycin is its only known selective inhibitor. The site and pathway of rho inhibition by the putative metal thiol chelates are disclosed. Additionally compositions and methods of divalent metals and compounds containing a thiol group are...

20060128683 - Novel use of porphyrin derivatives: The present invention is related to novel use of photopyrin compounds useful as an anticancer agent by way of reproducing singlet state oxygen radical and the inventive compounds showed potent inhibition effect on colon cancer, cervical cancer, gastric cancer, cystic cancer or lung cancer. Accordingly, the porphyrin compound of the...

20060128684 - Anthranilic acid amide derivatives and their pharmaceutical use: The present invention relates to new anthranilic acid amide derivatives, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof—alone or in combination with one or more other pharmaceutically active compounds....

20060128685 - Pyrazole derivative: The present invention provides compounds represented by formula (I) or formula (II), salts of the compounds, and solvates of the compounds or the salts. Also provided are medicaments containing any of the compounds, salts, or solvates and preventive and/or therapeutic agents for ischemic diseases, containing any of the compounds, salts,...

20060128686 - Preparation of pyridonecarboxylic acid antibacterials: A process for making 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid, and therapeutically acceptable salts thereof, and intermediates used in the process are disclosed....

20060128687 - Lactam glycogen phosphorylase inhibitors and method of use: p

20060128688 - Asenapine for the treatment of schizophrenia in a patient with overweight or predisposition for overweight: The invention provides means for the treatment of schizophrenia with an antipsychotic agent administered to a patient with overweight, or to a patient that was having weight gain due to an antipsychotic agent, or to a patient that needs to be protected against weight increase due to the presence of...

20060128689 - Chromanylurea compounds that inhibit vanilloid receptor subtype 1 (vr1) receptor and uses thereof: e

20060128690 - Amine derivative: provided that when the nitrogen-containing heterocycle formed by R1 and R2 together with the adjacent nitrogen atom is a piperazine, or when R is a C1-4 alkyl, Ar1 is a cyclic group having substituent(s), or a salt thereof, having a melanin-concentrating hormone antagonistic action and useful as an agent for...

20060128691 - Substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives: o

20060128694 - Adenosine a2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders: There is disclosed a method for the treatment or prevention of Extra Pyramidal syndrome (EPS), dystonia, restless legs syndrome (RLS) or periodic leg movement in sleep (PLMS) comprising the administration of an adenosine A2a receptor antagonist, alone or in combination with other agents useful for treating EPS, dystonia, RLS or...

20060128692 - Non nucleoside reverse transcriptase inhibitors: Phosphorus-substituted imidazole compounds with anti-HIV properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit reverse transcriptase activity and are useful therapeutically for the inhibition of such enzymes, as well as in assays for the detection of such enzymes....

20060128693 - Pyrrolobenzodiazepines: Compounds of formula (I): formula (I) and salts, solvates, chemically protected forms, and prodrugs thereof, are C disclosed wherein R2 is selected from: an optionally substituted napthyl group; an optionally substituted thiophenyl or furanyl group; and a phenyl group substituted by: one or more chloro or fluoro groups; an ethyl...

20060128695 - Cyclic nucleotide phosphodiesterase inhibitors, preparation and uses: The invention concerns the use of PDE2 inhibitors for treating disorders of the central and peripheral nervous system, a method for therapeutic treatment by administering to an animal said inhibitors. More specifically, the invention concerns novel benzodiazepinone derivatives and their uses in therapeutics more particularly for treating pathologies involving activity...

20060128696 - Treating seizures using ice inhibitors: This invention relates to methods and compositions for treating or preventing seizures....

20060128697 - New benzothiazine and benzothiadiazine compounds: i

20060128698 - Fungicidal combinations comprising glyoxalic acid methyl ester-o-methy-loxime derivatives: The present invention relates to a method of combating phytopathogenic disease on crop plants by applying to the crop plants and/or the locus thereof an effective amount of a combination of a) 2-[α-{[(α-methyl-3-trifluoromethyl-benzyl)imino]-oxy}-o-tolyl]-glyoxalic acid methyl ester-O methyloxime (I) and b) one or more other plant fungicides. These combinations exhibit synergistic...

20060128699 - Novel pharmacophore for the discovery and testing of na,k-atpase inhibitor compositions and methods for their use in treating cardiovascular diseases and conditions: Disclosed is a novel pharmacophore and novel inotropic compositions created from the novel pharmacophore. Also disclosed are methods of making and using the novel pharmacophore and method of use of novel compositions to treat heart diseases by inhibiting Na, K-ATPase....

20060128701 - Benzoxazinone-derived compounds, their preparation and use as medicaments: The present invention relates to Benzoxazinone-derived compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans or animals....

20060128700 - Morpoline-bridged indazole derivatives: The present invention relates to novel morpholine-bridged indazole derivatives which stimulate soluble guanylate cyclase, to processes for the preparation thereof, and to the use thereof for producing medicaments, in particular medicaments for the treatment of disorders of the central nervous system....

20060128702 - Heterocyclic and bicyclic compounds, compositions and methods: The present invention provides, among other things, new bicyclo heterocyclic compounds, compositions comprising these heterocyclic compounds, methods of making the heterocyclic compounds, and methods of using these heterocyclic compounds for treating a variety of conditions and disease states associated with, for example, cellular proliferation, inflammation, glycosidase expression, or the low...

20060128703 - Novel crystalline form of linezolid: The present invention relates to a novel crystalline form of linezolid, to processes for its preparation and to a pharmaceutical composition containing it....

20060128705 - Method of treating chronic fatigue syndrome: Methods and compositions for treating humans suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or a condition where inhibiting reuptake of norepinephrine is a benefit are disclosed. The compositions comprise a compound having a pharmacological selectivity of serotonin (Ki)/norepinephrine (Ki) of at least about...

20060128704 - Tetrahydro-naphthalene derivatives: in which R1 represents hydrogen or C1-6 alkyl, and X represents —N(H)Y1, —N(H)—C1-6 alkylene Y1, biphenyl or C1-6 alkyl substituted by biphenyl, and the group Y1 is an optionally substituted biphenyl. The tetrahydro-naphthalene derivatives of the present invention have excellent activity as VR1 antagonists and are useful for the prophylaxis...

20060128706 - Apoptosis promoters: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member....

20060128708 - Antagonizing an adenosine a2a receptor to ameliorate one or more components of addictive behavior: This invention provides a method of mitigating/ameliorating one or more components of addictive behavior associated with chronic consumption of a substance of abuse, or withdrawal therefrom. The method typically involves administering to a subject in need thereof an adenosine A2A receptor antagonist in an amount sufficient to ameliorate said one...

20060128707 - Imidazotriazinone derivatives as pde 7 (phosphodiesterase 7) inhibitors: The present invention provides the compounds inhibiting PDE 7 selectively, and therefore, enhances cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic disease, inflammatory disease or immunologic disease. The compound is imidazotirazinone compound represented by the following formula (IA) or (IB): especially,...

20060128709 - Pyrrolotriazine inhibitors of kinases: and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, PDGFR, HER-1, HER-2, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways...

20060128710 - Antagonists to the vanilloid receptor subtype 1 (vr1) and uses thereof: d

20060128711 - Antitumoral analogs: Derivatives of ecteinascidin 736 of general formula (I) wherein the groups R1, R2, R3, R4 and R5 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO2R′, C(═O)R′, C(═O)OR′, NO2, NH2, NHR′, N(R′)2, NHC(O)R′, CN, halogen, ═O, substituted or unsubstituted C1-C25 alkyl, substituted or...

20060128712 - Phenyl-piperazine methanone derivatives, substituted by heterocyclic groups: r

20060128713 - Bi- and tricyclic substituted phenyl methanones:

20060128714 - Maternal multi-nutrient against diabetes-related birth defects: The present invention provides uses of multi-nutrient supplements to rescue aberrant biochemical pathways and reduce birth defect caused by maternal diabetes. Choice of supplements is based on the ability of each supplement to correct the following hyperglycemia-associated abnormalities: increased reactive oxygen species generation, abnormal membrane phospholipid metabolism, and decreased glutathione...

20060128717 - Therapeutic agents useful for treating pain: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Tetrahydropiperidyl Compound”); compositions comprising an effective amount of a Tetrahydropiperidyl Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke,...

20060128716 - Use of 4-pyridylmethyl-phthalazine derivatives for the manufacture of a medicament for the treatment of myelodysplastic syndromes: The present invention relates to a method of treating myelodysplastic syndromes comprising administering a therapeutically effective amount of a 4-pyridylmethyl-phthalazine derivative to a warm-blooded animal in need thereof....

20060128718 - Tetrahydropyridazine derivatives having a pesticidal effect: e

20060128715 - Oxime derivative hydroxyethylamine aspartyl-protease inhibitors: The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein....

20060128719 - Use of alpha-adrenergic blockers for the treatment of dysmenorrhea: A method of treating primary dysmenorrhea which comprises administering to a human female suffering from the same a therapeutically effective amount of alpha-adrenergic blocker. Exemplary alpha-adrenergic blockers are phenoxybenzamine, alfuzosin, doxazosin, terazosin, prazosin, and tamsulosin, or a pharmaceutically acceptable salt or ester thereof. Tamsulosin HCl is preferred....

20060128720 - Inhibition of cell death responses induced by oxidative stress: The invention provides methods of reducing or preventing oxidative stress-induced cell death by contacting a cell with a compound that inhibits the kinase activity and/or the mitochondrial translocation of c-Abl. The methods of the invention can be used to treat individuals individual diagnosed as having or being at risk of...

20060128721 - Novel formulations of opioid-based treatments of pain comprising substituted 1,4-di-piperidin-4-yl-piperazine derivatives: the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1. The pharmaceutical composition according to the invention reduces to a large extent a number of unwanted side-effects associated with opioid...

20060128722 - Indoles useful in the treatment of androgen-receptor related diseases: e

20060128724 - Pyrazole-substituted aminoheteroaryl compounds as protein kinase inhibitors:

20060128723 - Sulptionamide compounds that modulate chemokine receptor activity (ccr4): The invention provides thienylsulphonamides for use in therapy....

20060128725 - Novel pyrazolopyrimidines as cyclin dependent kinase inhibitors: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition,...

20060128726 - Process for preparing novel crystalline forms of (2s)-1-[[(7r)-7-(3,4-dichlorophenyl)-4,7-dihydro-5-methylpyrazolo[1,5]pyrimidine-6-yl]carbonyl]-2-(4-fluorophenyl)pyrrolidine, novel stable forms produced therein and formulations: A process is provided for preparing novel crystalline forms, namely selectively and consistently preparing the H2-1 dihydrate crystalline form, the H2-2 dihydrate crystalline form, the N-3 anhydrate crystalline form and the MTBE solvate crystalline form of the IKur compound (2S)-1-[[(7R)-7-(3,4-dichlorophenyl)-4,7-dihydro-5-methylpyrazolo[1,5]pyrimidine-6-yl]carbonyl]-2-(4-fluorophenyl)pyrrolidine. The process includes preparation of the H2-1 and H2-2 forms...

20060128727 - Fungicidal mixtures based on a triazolopyrimidine derivative: in which R is methyl, cyclopropyl or 1-propynyl, in a synergistically effective amount, methods for controlling harmful fungi from the class of the Oomycetes using mixtures of the compound I with one of the compounds II, and the use of the compound I with one of the compounds II for...

20060128729 - Novel bicyclic heterocyclic compounds, process for their preparation and compositions containing them: The present invention provides, among other things, new bicyclo heterocyclic compounds, compositions comprising these heterocyclic compounds, methods of making the heterocyclic compounds, and methods of using these heterocyclic compounds for treating a variety of conditions and disease states associated with, for example, cellular proliferation, inflammation, glycosidase expression, or the low...

20060128728 - Pyridinylpyrazolopyrimidinone derivatives as pde 7 inhibitors: To provide the compounds inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic disease, inflammatory disease or immunologic disease. The compound is pyridinylpyrazolopyrimidinone compound represented by the following formula (IA) or (IB): especially, R1 is...

20060128730 - Use of radical-scavenging compounds for treatment and prevention of no-dependent microcirculation disorders: A method of treatment of the human or non-human animal body for treating NO-dependent microcirculation disorders is disclosed, for example microcirculation disorders caused by metabolic diseases, such as elevated levels of homocystin-homocystein inflammatory reactions or autoimmune diseases, furthermore peripheral microcirculation disorders or microcirculation disorders associated with increased cell fragmentation, which...

20060128731 - Pyrrolo [2,3-d] pyrimidine and their use as purinergic receptor antagonists: Use of a compound of the formula (I) wherein R1 is selected from alkyl, alkoxy, aryloxy, alkylthio, arylthio, aryl, halogen, CN, NR7R8, NR6COR7, NR6CO2R9 and NR6SO2R9; R2 is selected from aryl attached via an unsaturated carbon; R3 and R4 are independently selected from H, alkyl, halogen, alkoxy, alkylthio, CN and...

20060128732 - Fused azole-pyrimidine derivatives: The present invention relates to hovel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with...

20060128733 - Method for treating hiv infection through co-administration of tipranavir and reverset: A method for treating HIV infection through co-administration of tipranavir and reverset....

20060128734 - Diaryl urea derivatives useful for the treatment of protein kinase dependent diseases: The invention relates to the use of diaryl urea derivatives in the treatment of protein kinase dependent diseases or for the manufacture of pharmaceutical compositions for use in the treatment of said diseases, methods of use of diaryl urea derivatives in the treatment of said diseases, pharmaceutical preparations comprising diaryl...

20060128735 - Substituted thiophenes with antibacterial activity: Novel substituted thiophenes that are inhibitors of bacterial methionyl t-RNA synthetase (MRS) are disclosed. Also disclosed are method for their preparation and their use in therapy as anti-bacterial agents....

20060128736 - Camptothecin-carboxylate formulations: The present invention relates to compositions, particularly colloidal nanoaggregates comprising the carboxylate form of a campothecin drug or a derivative thereof associated with at least one organic cationic molecule, which has a positive net charge. The composition or nanoaggregate may be present as an emulsion, droplet, mincelle, liposome, nanoparticle or...

20060128737 - Androgen receptor agonists: (R1, R2, X, Y, Z and m are as defined in claim 1) which show no excessive action on the prostate but show a particularly potent androgen receptor agonistic action on skeletal muscle tissue and bone tissue, as well as pharmaceuticals comprising such derivatives or their salts as active ingredients....

20060128738 - Treatment of interstitial cystitis using cannabinoid analogs: The present invention relates to non-psychoactive derivatives of tetrahydrocannabinol, which are useful in treating interstitial cystitis and relieving symptoms thereof. The invention uses cannabinol analogs, which are preferably analogs of (6aR,10aR)-Δ8-tetrahydrocannabinol-11-oic acids [hereinafter referred to as (6aR,10aR)-Δ8-THC-11-oic acid], as well as pharmaceutical compositions containing the cannabinol analogs and analogs of...

20060128739 - Solvent free amorphous rapamycin: An improved process for coating implantable medical devices utilizes a number of techniques for improving the stability of therapeutic agents contained within the coating. The stability of the therapeutic agents may be improved by creating substantially solvent-free, amorphous forms of the therapeutic agents....

20060128740 - Tricyclic androgen receptor modulator compounds and methods: This invention relates to non-steroidal tricyclic compounds that are modulators of androgen receptors and to methods for making and using such compounds....

20060128741 - 8h-imidazo[4,5-d]thiazolo[4,5-b]pyridine based tricyclic compounds and pharmaceutical compositions comprising same: i

20060128742 - Cell migration inhibiting compositions and methods and compositions for treating cancer: Methods for treating an individual having cancer are provided. The method may include administering a cell migration inhibitor and a chemotherapeutic agent to the individual to inhibit migration of cancer cell. Inhibiting cell migration may increase cell division. In this manner, the cell migration inhibitor and the chemotherapeutic agent in...

20060128743 - Method of improving bioavailability of orally administered drugs, a method of screening for enhancers of such bioavailability and novel pharmaceutical compositions for oral delivery of drugs: A method for increasing the systemic exposure of cells selected from tumor cells and normal cells to an orally administered pharmaceutically active compound, wherein a bioenhancer comprising an inhibitor of BCRP is orally administered concomitantly with said orally administered pharmaceutically active compound, and in which method the inhibitor is administered...

20060128745 - Chemical compounds: The present invention is related to aza-oxindole derivatives, compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition...

20060128746 - Methods, kits and compositions for using pyrrole derivatives: e

20060128744 - Use of 5-ht6 agonist for the treatment and prevention of neurodegenerative disorders: The present invention provides method for the treatment, amelioration or prevention of a neurodegenerative disorder in a patient in need thereof which comprises administering to said patient an effective amount of a 5-hydroxytryptamine-6 agonist....

20060128747 - Biaryl compounds having anti-infective activity: Aromatic compounds exemplified by exhibit antimicrobial activity....

20060128748 - Bicyclic triazole alpha4 integrin inhibitors: The compounds of the present invention are novel bicyclic triazole amino acid-derivatives useful as α4 integrin receptor antagonists. The invention is further directed to methods for treating integrin mediated disorders including, but not limited to, inflammatory, autoimmune and cell-proliferative disorders, methods for preparing the compounds and methods for preparing the...

20060128749 - Compounds: e

20060128750 - Chemokine receptor binding heterocyclic compounds: Tertiary amine compounds that bind chemokine receptors such as CXCR4 and CCR5 are disclosed....

20060128751 - Cetp inhibitors in combination with antihypertensive agents and uses thereof: This invention relates to pharmaceutical combinations of a cholesteryl ester transfer protein (CETP) inhibitor or a pharmaceutically acceptable salt thereof; and an antihypertensive agent or a pharmaceutically acceptable salt thereof, optionally in combination with an HMG CoA reductase inhibitor or a pharmaceutically acceptable salt thereof, kits containing such combinations and...

20060128753 - 4-aminopiperidine derivatives, processes for their preparation and their use as medicaments: The present invention relates to 4-aminopiperidine derivatives, to processes for their preparation, to their use in therapy and to pharmaceutical compositions containing them. More particularly these compounds are useful for treatment of disorders of the central and/or peripheral nervous system. Of particular interest, is the potent antidepressant activity shown by...

20060128752 - Chemical compounds: provided that when m is 0, p is 2, q , r and n represent 1, R1, R2,R3, R4, R5 and R7 are hydrogen and R is chlorine, R5 is not iodine; and pharmaceutically acceptable salts and solvates thereof; process for their preparation and their use in the treatment of...

20060128754 - Tubulysins, method for producing the same and tubulysin preparations: o

20060128755 - Amide derivative: wherein: A is a cycloalkyl group, an aryl group or a heteroaryl group; X is a nitrogen atom or CR17; Y is —NRa—, —(CRbRb′)m—, and the like; m is 0 to 4; and R1 to R17 may be the same or different and each is a hydrogen atom, a halogen...

20060128756 - Heteroaryl-substituted pyrrole derivatives, their preparation and their therapeutic uses: m′ is 1; E′ is nitrogen; D′ is >C(R5′), R5′ is hydrogen, Substituent α′ or Substituent β′; B′ is nitrogen-containing 5-membered heterocyclic; R4′ is 1 to 3 substituents from Substituent α′, Substituent β′ and Substituent γ′; R1′ and R3′ are bonded to two atoms of the pyrrole adjacent to the...

20060128757 - Pyridine derivatives useful as cyclooxygenase inhibitor: #

20060128758 - 4-,6- or 7-hydroxyindoles with n-oxide groups and the use thereof as therapeutic agents: The invention relates to substituted 4-, 6- or 7-hydroxyindoles with N-oxide groups, process for their preparation, pharmaceutical preparations which comprise these compounds, and the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 4, as active ingredients for the treatment of disorders which can be influenced by inhibition of...

20060128759 - Substituted isoxazole derivatives and their use in pharmaceutics: The invention relates to substituted isoxazole derivatives of formula (I), wherein the radicals R1, R2 and R3 have the meanings as cited in the description. The inventive compounds comprise an immunomodulatory action and/or an action that inhibits the release of cytokines and are thus suited for treating diseases associated with...

20060128761 - Novel triazole compounds as transforming growth factor (tgf) inhibitors: Novel triazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-β signaling pathway. They are useful in the treatment of various TGF-related disease states...

20060128760 - Use of mglur5 antagonists for the treatment of gerd: The present invention relates to the use of metabotropic glutamate receptor 5 antagonists for the inhibition of transient lower esophageal sphincter relaxations. A further aspects of the invention is directed to the use of metabotropic glutamate receptor 5 antagonists for the treatment of gastro, esophageal reflux disease, as well as...

20060128762 - Medicinal composition and method for treating malignant tumor and utilization thereof: The present invention provides an excellent method and a pharmaceutical composition for treating a malignant tumor, and use thereof. Specifically, the present invention is related to a pharmaceutical composition for treating malignant tumor comprising a specific aminostilbazole derivative or a pharmaceutically acceptable salt thereof, which is administered in combination with...

20060128763 - Stable amorphous amlodipine camsylate, process for preparing same and composition for oral administration thereof: This invention relates to a stable, amorphous form of amlodipine camsylate having a high solubility which can be efficiently used in treating cardiovascular diseases....

20060128765 - 2-(bicyclo)alkylamino-derivatives as mediators of chronic pain and inflammation: Compounds disclosed herein are bradykinin B1 antagonist compounds useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway....

20060128764 - Non-steroidal farnesoid x receptor modulators and methods for the use thereof: The efficient regulation of cholesterol synthesis, metabolism, acquisition, and transport is an essential component of lipid homeostasis. The farnesoid X receptor (FXR) is a transcriptional sensor for bile acids, the primary product of cholesterol metabolism. Accordingly, the development of potent, selective, small molecule agonists, partial agonists, and antagonists of FXR...

20060128766 - Triazole substituted aminobenzophenone compounds: e

20060128767 - Methods of preparing sulfinamides and sulfoxides: This invention encompasses novel methods of preparing sulfinamides and sulfoxides, particularly stereomerically pure sulfinamides and sulfoxides. The invention further encompasses novel compounds from which sulfinamides and sulfoxides can be prepared....

20060128768 - Furanthiazole derivatives as heparanase inhibitors: The invention provides a compound of formula (I) or a pharmaceutically acceptable salt or prodrug thereof. (I) wherein the groups Q, R2, R3, R4 and R5 represent various substituent groups, and their use as inhibitors of heparanase....

20060128770 - Thiazole derivatives: A compound of the formula (I): R1—NH—X—Y-Z (I) wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof useful as a vascular adhesion protein-1 (VAP-1) inhibitor, a pharmaceutical composition, a method for preventing or treating a VAP-1 associated disease, especially macular edema, which method includes...

20060128769 - Thiazoyl biphenyl amides: c

20060128771 - Method of treating acne: A method of selectively enhancing photothermal sebaceous gland disruption and treatment of acne is disclosed. The method provides for alleviation of the acne symptoms as well as preventing acne recurrence and new acne from occurring....

20060128772 - Novel 1,2,4-thiadiazole derivatives as melanocortin receptor modulators: The present invention is directed to novel 1,2,4-thiadiazole derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II...

20060128773 - Wood preservatives and waterproofing compositions and processes: An alkyl dimethyl benzyl ammonium saccharinate is put into solution with a water soluble alcohol, such as ethanol, and subsequently mixed with water to form a aqueous solution for the treatment of wood to protect it from attacks by fungus, insects and other pests or to waterproof the wood. Preferably...

20060128774 - (meth)acrylate amide acetals: The present invention relates to the composition and process for making (meth)acrylate amide acetals....

20060128776 - Opioid receptor active compounds: wherein R1 to R4 and n have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods...

20060128775 - Regiospecific process for the preparation of 4-[1- (4-cyanophenyl)-1-(1,2,4-triazol-1-yl) methyl] benzonitrile: A regiospecific process for the preparation of 4-[1-(4-cyanophenyl)-1-(1,2,4-triazol-1-yl)methyl]benzonitrile comprising reacting 4-halomethylbenzonitrile with 4-amino-1,2,4-triazole followed by deamination and reaction with 4-fluorobenzonitrile....

20060128777 - Cancer treatments: Methods and compositions for treating cancers characterized by death-resistant cancer cells are described. In general, such methods involve administration of a therapeutically effective amount of a compound that induces mitotic catastrophe in the some, and preferably most or all, of the cancerous cells. Methods for assessing the efficacy of such...

20060128778 - Amino acid composition for improving central functions: An amino acid composition or an amino acid solution for improving central functions which contains threonine, proline, glycine, valine, isoleucine, leucine, tyrosine, phenylalanine, lysine, aspartic acid, serine, glutamic acid, alanine, methionine, tryptophan, histidine and arginine; and an amino acid composition or an amino acid solution derived from the above composition...

20060128779 - Control of parasites in animals by the use of parasiticidal 2-phenyl-3-(1h-pyrrol-2-yl)acrylonitrile derivatives: 2-Phenyl-3-(1H-pyrrol-2-yl)acrylonitrile compounds useful for controlling parasites in animals and methods of treatment of parasite infestation in animals using the compounds are disclosed....

20060128780 - Cyclic substituted fused pyrrolocarbazoles and isoindolones: The present invention is directed to cyclic substituted fused pyrrolocarbazoles and isoindolones. The invention also is directed to methods for making and using the cyclic substituted fused pyrrolocarbazoles and isoindolones....

20060128781 - Flavaxate derivatives as muscarinic receptor antagonists: This invention generally relates the derivatives of 3.6-disubstituted azabicyclo[3.1.0]hexanes of the following formula [IA]. The compounds of this invention can function as muscarinic receptor antagonists, and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates...

20060128782 - Pharmaceutical composition based on ketorolac or one of its salts pharmaceutically acceptable and use of ketorolac or its salts in pharmaceutical compositions: The present invention refers to pharmaceutical compositions based on ketorolac or one of its salts pharmaceutically acceptable, as well as the use of ketorolac or one of its salts acceptable from pharmaceutical viewpoint, for preparation of a pharmaceutical composition (tablets) for sublingual administration, with the purpose of accelerating the pharmacological...

20060128785 - Analogs of indole-3-carbinol metabolites as chemotherapeutic and chemopreventive agents: e

20060128784 - Bis-heteroaryl alkanes as therapeutic agents: This invention provides compounds which are useful as inhibitors of protein tyrosine phosphatases (PTPases). As inhibitors of PTPases the compounds of the invention are useful for the management, treatment, control and adjunct treatment of diseases in mammals mediated by PTPase activity. Such diseases include type I diabetes, type II diabetes,...

20060128783 - Tyrosine kinase inhibitors: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises an indole-sulfonamide moiety. The present invention is also related to the pharmaceutically acceptable salts,...

20060128786 - Compounds for the treatment of alzheimer's disease: The invention relates to compounds of formula (I). Useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of...

20060128787 - Novel indoline compound and medicinal use thereof: wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing this indoline compound or a pharmaceutically acceptable salt thereof. The compound of the present invention shows superior ACAT inhibitory effect and superior lipoperoxidation inhibitory effect and is useful as an...

20060128788 - Purification of tegaserod maleate: Provided is a process for the purification of tegaserod maleate. Also provided is an isolated compound and the preparation thereof. This compound may be used as a reference marker and a reference standard, in the analysis of the purity of the tegaserod maleate....

20060128789 - Process for the preparation of substituted pyrrolidine derivatives and intermediates: Two syntheses are provided; one for the preparation of (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol, and other for the preparation of (3S,4R)-4-(hydroxymethyl)pyrrolidin-3-ol. (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol is prepared using the achiral ylide prepared from benzylamine instead of phenethylamine (Scheme 3) which provides a crystalline intermediate. The synthesis of (3S,4R)-4-(hydroxymethyl)pyrrolidin-3-ol is achieved from (S)-diethylmalate as described in Scheme 4....

20060128790 - Spiro derivatives as lipoxygenase inhibitors: The present invention is concerned with certain novel spiro substituted heterocylic ring derivatives. These compounds may be useful in the manufacture of pharmaceutical compositions for treating disorders mediated by lipoxygenases. They may also be useful in the manufacture of pharmaceutical formulations for the treatment of lipoxygenase-mediated disorders....

20060128791 - 3-methylamino-1-(2-thienyl)-1-propanone, production and use thereof: The present invention relates to the preparation of 3-methylamino-1-(2-thienyl)-1-propanone and its use for preparing the pharmaceutical (+)-(S)-N-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine oxalate—(trade name Duloxetine®)....

20060128793 - Analogs of 17-hydroxywortmannin as p13k inhibitors: e

20060128792 - Deguelin as a chemopreventive agent for lung cancer: The present invention provides the chemopreventive agent deguelin, a natural product isolated from Mundulea serica (Leguminosae), and derivatives thereof, for use in combination with a second agent for inhibiting growth premalignant and malignant lung cancer cells by causing G2/M arrest and apoptosis. Thus, the present invention provides deguelin-based combination therapies...

20060128794 - Treatment of interstitial cystitis using (6ar,10ar)-delta8-tetrahydrocannabinol-11-oic acids: The present invention relates to non-psychoactive derivatives of tetrahydrocannabinol, which are useful in treating interstitial cystitis and relieving symptoms thereof. The invention uses (6aR,10aR)-Δ8-tetrahydrocannabinol-11-oic acids (hereinafter referred to as (6aR,10aR)-Δ8-THC-11-oic acid), as well as pharmaceutical compositions containing the (6aR,10aR)-Δ8-THC-11-oic acids, for treatment of interstitial cystitis in a mammal. The invention...

20060128795 - Agents for promoting fattening of animals and method of promoting fattening: Agents for promoting fattening of animals which contain as the active ingredient(s) at least one member selected from among acids originating in hexoses, non-toxic salts thereof and intramolecular esterification products thereof; and a method of promoting fattening by using these agents....

20060128796 - Active substance combinations comprising insecticidal and acaricidal properties: The invention relates to novel active compound combinations of certain cyclic ketoenols and certain insecticidally active compounds that together have very good insecticidal and acaricidal properties....

20060128797 - Method and composition for resuscitation: The key obstacle for current resuscitation is the acutely limited time window. The major reason for the limited time window is that the brain is extremely vulnerable to hypoxic-ischemic insult. The existence of cerebrospinal fluid (CSF) is the major reason why brain and spinal cord is so vulnerable. A method...

20060128798 - Method and composition for resuscitation: The key obstacle for current resuscitation is the acutely limited time window. The major reason for the limited time window is that the brain and spinal cord are extremely vulnerable to hypoxic-ischemic insult. A method and a lymph-like fluid composition for resuscitation of cardiac arrest are provided. The method includes...

20060128799 - Method for preparation of amino acid chelate: The present invention provides methods for preparation of metallic amino acid chelates that are electrically neutral and free of interfering ions, by reacting a metal carbonate and an acidic amino acid in an aqueous solution, and the uses of said metallic amino acid chelates. The metallic amino acid chelates can...

20060128800 - Medium-chain length fatty acids, glycerides and analogues as stimulators of erythropoiesis: Use of a composition comprising a compound of any of formulae I, II, Ila, III and Illa; or a combination thereof wherein each R1 is independently C7-11 alkyl; A and B are independently H or CO—R1; R2 is H or C1-4 alkyl; M is a metal monocation (k=1) or dication...

20060128801 - Organic compounds: The invention relates to compounds of the general formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R8′, R9, W, a, b and n have the significances given in claim 1, and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for...

20060128802 - Methods of treating tardive dyskinesia and other movement disorders: The present invention describes a novel treatment for movement disorders, including tardive dyskinesia, tic disorders, Tourette's syndrome, and blepharospasm, and other focal dystonias. The treatment of the present invention utilizes agents that simultaneously act as NMDA-type glutamate receptor antagonists and GABA-A receptor agonists. Preferably these two activities are characteristic of...

20060128803 - Method of treating dry eye disorders using 13(s)-hode and its analogs: The topical use of 13(S)-HODE and analogs are disclosed for the treatment of dry eye disorders....

20060128804 - Novel approach to antimicrobial host defense with molecular shields with epa and dha analogs: Methods to cause tissue, such as mucosal cells, to express increased amounts of bactericidal permeability increasing protein (BPI) are described. Various BPI inducing agents include icosapentanoic acid (EPA) analogs and docosahexaenoic acid (DHA) analogs....

20060128805 - Methods of treating erythropoietin-resistance: A human having an erythropoietin resistant condition is treated by the administration of an iron chelator. The human can have end-stage renal disease, chronic renal disease, cancer or anemia. Administration of the iron chelator can essentially halt or diminish an erythropoietin resistant condition in a human....

20060128806 - Controlled release arginine alpha-ketoglutarate: An oral formulation of arginine α-ketoglutarate is disclosed which formulation is comprised of arginine α-ketoglutarate and one or more excipient materials. A wide range of different controlled release formulations will be apparent to those skilled in the art upon reading this disclosure. The formulation of arginine α-ketoglutarate and excipient material...

20060128807 - Amino alcohol derivatives, pharmaceutical compositions containing the same, and use thereof: or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen or lower alkyl; R3, R4, R5 and R6 are each hydrogen, halogen, lower alkyl or lower alkoxy; R7 and R8 are each hydrogen, halogen, lower alkyl, halo-lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, cyano, a hydroxyl group, lower...

20060128808 - Method of using adapalene in acne maintenance therapy: The present invention provides for a method of using adapalene for the maintenance theray of acne vulgaris to prevent acne recurrence or reduce the severity of the acne recurrence....

20060128809 - Rapidly absorbed liquid compositions: The present invention provides a method which provides for a faster absorption of pharmaceutically acceptable amines. The method provides a pharmaceutically acceptable amine in combination with a non-steroidal anti-inflammatory drug in a liquid form. A preferred embodiment employs pseudoephedrine and ibuprofen....

20060128810 - Remedies for allergic diseases: The present invention relates to a prophylactic and/or therapeutic agent for an allergic disease which contains a compound having an agonistic activity to EP3 receptor that is one of the prostaglandin E2 receptor subtypes. More specifically, a compound having an agonistic activity to EP3 receptor is effective in therapy of...

20060128811 - Antibacterial agents: Compounds of formula (I) have antibacterial activity; wherein Q represents a radical of formula —N(OH)CH(═O) or formula —C(═O)NH(OH); Y represents —C(═O)—, —C(═S)—, —S(═O)—, or —SO2—; R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of formula —N(OH)CH(═O),...

20060128812 - Process for the preparation of 2-[(diphenylmethyl) thio] acetamide: Process for the preparation of 2-[(diphenylmethyl)thioacetamide, an intermediate for the preparation of Modafinil which is a CNS stimulant and used for the treatment of narcolepsia. The process comprises reacting 2-[(diphenylmethyl)thio]acetic acid with alcohols, in presence of catalytic amount of inorganic acid or organic acid at reflux temperature of alcohol to...

20060128813 - Inhibition of the asexual reproduction of fungi by eugenol and/or derivatives thereof: This invention relates to the use of eugenol and/or eugenol derivatives for inhibiting the asexual propagation of fungi. This invention also relates to filter media, adhesives, building materials, building auxiliaries, textiles, pelts, paper, skins or leather, laundry detergents, cleaning compositions, rinse agents, hand washing preparations, manual dishwashing detergents, machine dishwashing...

20060128814 - Photolytic cross-linkable monomers: Photolytic cross-linkable polymers comprises three domains, a cationic domain, a cross-linkable domain and a photolabile domain. The photolytic cross-linkable polymers according to the current invention are useful in a method to complex and compact DNA and RNA for delivery to a living cell, wherein the DNA or RNA is released...

20060116315 - Method of screening agent for improving memory and learning ability: A screening tool and a screening method of a substance which is useful as an agent for improving the memory, an agent for improving learning ability, and/or an antidementia agent; a polypeptide, a polynucleotide, a vector, and a cell which may be used in the above screening; and a novel...

20060116316 - Heterocyclic inhibitors of ires-mediated translation and methods of use thereof: The present invention provides heterocyclic compounds that exhibits IRES-inhibitory activity. The heterocyclic compounds generally a nine-membered ring of three repeating C—C—N subunits covalently bound through amide bonds, and variable side groups linked to a central carbon of each subunit. Formulations and kits containing the subject compounds are also provided....

20060116317 - Characterization of a membrane estrogen receptor: The present disclosure relates to a process for dyeing keratin materials with compositions comprising, in a medium that is suitable for dyeing, at least one ninhydrin derivative, which may optionally be combined with at least one compound comprising at least one labile hydrogen. Further disclosed herein are dying compositions, multi-component...

20060116322 - Formation of novel erythropoietin conjugates using transglutaminase: The invention provides biologically active erythropoietin (EPO) conjugate compositions wherein a transglutaminase reaction is employed to covalently and site specifically conjugate the EPO molecule to a non-antigenic hydrophilic polymer that can also be covalently linked to an organic molecule either of which modification increases the circulating serum half-life of the...

20060116320 - Growth hormone crystals and a process for production of these gh-crystals: A process for producing cation crystals of growth hormone or growth hormone derivatives, as well as growth hormone and growth derivatives. The process of producing the growth hormone crystals includes the steps of (a) adding cations of inorganic or organic nature and an organic solvent or a mixture of inorganic...

20060116321 - Immunosuppressive exosomes: The present invention relates to methods and compositions for use in mediating an immunosuppressive reaction. The compositions of the invention comprise exosomes having immunosuppressive activity. Such exosomes may be derived from a variety of different cell types, including antigen presenting cells such as dendritic cells and macrophages. Prior to isolation...

20060116319 - Method for identifying and treating photodamaged skin: The present invention relates to modulation of MAP2K2 and DUSP-1 genes and proteins encoded thereby. More specifically, the present invention relates to modulation of MAP2K2 and DUSP-1 genes to detect and condition photo-damaged skin, preferably, chronically photo-damaged skin, as well as to identify active compounds and compositions for skin conditioning....

20060116324 - Novel formulations: The present invention relates to compositions comprising coagulation factor FVIIa....

20060116318 - Preptin methods of use: This invention features a method for treating a bone condition in a patient, e.g., a mammal, a human, a horse, a dog, or a cat. The method includes administering an effective amount of preptin, preptin analog, or a preptin agonist to the patient....

20060116323 - Tumor-inhibiting protein and the use thereof: The invention has disclosed a new tumor suppressor protein HCRP1, the polynucleotide sequences encoding this polypeptides, and methods for production of the polypeptide using the recombinant technology. The tumor suppression protein, HCRP1, is obtained through the positional candidate cloning strategy. It locates in 8p22 region of human chromosome. The full...

20060116325 - Methods and compositions for inhibiting hiv-coreceptor interactions: Novel methods and compositions are provided for inhibiting interactions between human immunodeficiency viruses (HIVs) and viral coreceptors, including CXCR4 and/or CCR5 coreceptors. The anti-coreceptor binding agent includes a novel peptide portion of the gp120 envelope protein of HIV-1, as well as peptide analogs and mimetics of this peptide, that specifically...

20060116327 - Antimicrobial compounds: v

20060116326 - Benzothiophene compounds having antiinfective activity:

20060116328 - Combined use of carnosinase inhibitor with l-carnosines and composition: The present invention provides combined use of a carnosinase inhibitor with L-carnosine and its related substance, and a composition containing the same, which are useful for treatment or prevention of various diseases, improvement of health conditions, improvement of exercise ability, improvement of skin health, prevention of the side effects of...

20060116329 - Halothenoyl-cyclopropane-1-carboxylic acid derivatives: Compounds of formula (I) wherein R is hydroxy, linear or branched C1-C6 alkoxy, phenoxy, benzyloxy, a group —N(R1R2) wherein R1 is hydrogen, linear or branched C1-C4 alkyl, benzyl, phenyl and R2 is hydrogen or linear or branched C1-C4 alkyl, or R is a glycoside residue or a primary alkoxy residue...

20060116330 - Methods of mimicking the metabolic effects of caloric restriction by administration of mannoheptulose: Disclosed herein are methods of using glucose anti-metabolites to alter utilization of glucose or other energy sources and to mimic metabolic effects of caloric restriction. In particular, in one embodiment herein, methods of enhancing longevity in an animal are described, the methods comprising administration of a composition comprising a glucose...

20060116331 - Glycosylceramide analogues: Glycosylceramide analogues are disclosed in which the ceramide moiety and optionally the carbohydrate moiety are modified or replaced. These analogues are useful as immunomodulators, antitumor agents, and as other pharmaceutical agents....

20060116332 - Methods for inhibition of nkt cells: Molecules that interact with the NKT cell antigen receptor and its counterpart antigen presenting molecule, but which inhibit the NKT cell immune function, are administered to a patient. Conditions of particular interest include the treatment of systemic lupus erythematosus (SLE), cancer, atherosclerosis, and allergic disease. In some embodiment of the...

20060116333 - Composition for protecting organ, tissue or cell and utilization thereof: The present invention provides a composition for efficiently protecting and preserving organs, tissues or cells. In particular, the present invention provides a protective composition which can be used during operations. Specifically, the present invention provides a composition for protecting and preserving organs, tissues or cells, comprising a polyphenol. A method...

20060116334 - Folate based composition for treatment of the cardiovascular system: New formulations for the prevention and treatment of cardiovascular diseases arthrosclerosis and risk factors thereof including elevated cholesterol and blood pressure levels comprise phytosterols, flavones and folate, alone or in combination, along with additional compounds chosen to address some or all of the pathways which can result in cardiovascular diseases,...

20060116336 - Lyophilized azithromycin formulation: The invention provides among other things a stable, sterile pharmaceutical formulation comprising lyophilized azithromycin and ethanol. The invention also provides a method of producing a stable, sterile pharmaceutical product comprising lyophilized azithromycin. The invention also provides a pharmaceutical dosage form comprising the pharmaceutical formulation, as well as a method of...

20060116335 - Ready-for-complexation composition: The invention relates to a ready-for-complexation (RFC) composition, comprising a polyene antimycotic and a cyclodextrin or the derivatives thereof. Also disclosed is a method of using the ready-for-complexation (RFC) composition of the invention to improve the solubility of polyene antimycotic....

20060116337 - Use of glycyrrhizin and its derivatives as mcp-1 production inhibitors: The object of the present invention is to provide the use of glycyrrhizin and its derivatives for inhibition of MCP-1 production. The present invention discloses an MCP-1 production inhibition method and pharmaceutical composition for the same comprising administration of glycyrrhizin and its derivatives in an amount effective for said inhibition...

20060116339 - Antisense modulation of purinoreceptor p2x3: The invention relates to antisense oligonucleotides, compositions and methods useful for modulating the expression of P2X3. The compositions comprise antisense oligonucleotides, particularly antisense oligonucleotides targeted to nucleic acids encoding P2X3....

20060116340 - Herpesvirus ribozymes and vectors: Hammerhead ribozymes that target components critical to HSV replication (ICP4, UL20, UL30, and UL54) were synthesized and shown to efficiently cleave target RNA encoding a portion of these components in in vitro assays. Several cloned cell lines stably expressing these ribozymes were established. HSV-mediated plaque formation was dramatically reduced in...

20060116338 - Mammalian early developmental regulator gene: This disclosure encompasses the edr3 polynucleotide, polypeptides encoded by the edr3 gene and fragments thereof. This disclosure also encompasses homologues of the edr3 gene from mammals, in particular from humans. In addition, this disclosure encompasses the use of edr3 polynucleotides, edr3 proteins and polypeptides, and antibodies to the edr3 protein...

20060116341 - Pharmaceutical composition for treating and/or preventing a pathology associated with an obsessional behavior or with obesity: This invention relates to the use of a ligand of the 5-HT4 receptor or of a pharmaceutically acceptable salt of this ligand and to a nucleic acid coding for a 5-HT4 receptor or of a functionally equivalent receptor for a drug for treating and/or preventing a pathology associated with an...

20060116342 - Protective immunity or immunological tolerance induced with rna, particularly total cellular rna: Effective anti-tumor immunity is induced in mice utilizing RNA-pulsed epidermal cells (EC) for in vivo immunization or by injecting RNA intradermally into naïve mice. A vaccine comprising total cell RNA and a pharmaceutically acceptable carrier for inducing an immune response to reduce or prevent the occurrence of a tumor....

20060116344 - Remedy and preventive for diseases caused by nf-kb: Administration of a decoy, i.e. a compound which specifically antagonizes the nucleic acid domain to which NF-κB is bound, is effective in the treatment and prevention of diseases caused by the transcriptional regulatory factor NF-κB, such as ischemic diseases, inflammatory diseases, autoimmune diseases, cancer metastasis and invasion, and cachexia....

20060116343 - Sphingosine kinase-1 mediates gene expression regulation of a monocyte chemoattractant protein-1 gene: The present invention relates to methods of identifying, monitoring, and using compounds that regulate the biological activity of Sphingosine kinase-1....

20060116345 - Antitumor effect potentiator and antitumor agent: The present invention provides an antitumor effect potentiator for enhancing antitumor activity of an antitumor agent comprising tegafur in a therapeutically effective amount, gimeracil in an amount effective for enhancing an antitumor effect, and oteracil potassium in an amount effective for inhibiting a side effect, the antitumor effect potentiator comprising...

20060116349 - Methods and compositions for administration of iron for the treatment of restless leg syndrome: The invention is directed to methods of treating Restless Leg Syndrome by administering iron complexes with specificed iron release rates or specified iron core size....

20060116347 - Methods and compositions to treat glycosaminoglycan-associated molecular interactions: Therapeutic compounds and methods for inhibiting a glycosaminoglycan (GAG)-associated molecular interaction in a subject, whatever its clinical setting, are described....

20060116348 - Polymer grafting by polysaccharide synthases: The present invention relates to methodology for polymer grafting by a polysaccharide synthase and, more particularly, polymer grafting using the hyaluronate synthase from Pasteurella multocida. The present invention also relates to coatings for biomaterials wherein the coatings provide protective properties to the biomaterial and/or act as a bioadhesive. Such coatings...

20060116346 - Taxanes covalently bounded to hyaluronic acid or hyaluronic acid derivatives: The present invention relates to water-soluble taxanes covalently bounded tohyaluronic acid or hyaluronic acid derivatives, and in particular to paclitaxel and docetaxel, useful for the preparation of pharmaceutical compositions to be used in the field of oncology, in the treatment of autoimmune disorders and of restenosis. The invention also relates...

20060116350 - Dopamine 3 receptor agonist and antagonist treatment of gastrointestinal motility disorders: The invention discloses that systemic activation of dopamine 3 receptor (D3R) significantly delays gastric emptying in rat, suggesting that D3R plays an important role in the regulation of gastric motility. Specific D3R antagonist, nafadotride, was shown to partially reverse the effect of dopamine on gastric emptying. The invention also discloses...

20060116351 - 17,20(z)-dehydro vitamin d analogs and their uses: This invention discloses 17,20(Z)-dehydro vitamin D analogs, and specifically 17(Z)-1α,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin D3 and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as...

20060116352 - 2alpha-methyl and 2beta-methyl analogs of 19,26,27-trinor-(20s)-1alpha-hydroxyvitamin d3 and their uses: This invention discloses 2α-methyl and 2β-methyl analogs of 19,26,27-trinor-(20S) -1α-hydroxyvitamin D3 and pharmaceutical uses therefor. These compounds exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as...

20060116353 - Method for removal of unwanted organism from the human body and a treatment for removal of unwanted organism from the human body: A method and treatment for removing an unwanted living organism from a person includes administering topically to the person an effective amount of a solution including a pyrethrin compound and piperonyl butoxide. The term “pyrethrin compound” includes pyrethrin, cinerin, and allethrin. A carrier formulation can be added to said piperonyl...

20060116354 - Antineoplastic ether lipid compounds with modifications at the sn-3 carbon: Ether lipid compounds of formula (I), pharmaceutically-acceptable salts, prodrugs or isomers thereof are provided, where the variables are as defined herein. The compounds of the invention have anti-neoplastic activity, and accordingly have utility in treating cancer and related diseases. Enantiomers of these compounds, pharmaceutical compositions, and methods for treating cancer...

20060116355 - Eye care kit for treating periocular disease: A care compliance kit is revealed to minimize and prevent the spreading of highly contagious bacterial and viral ocular diseases, to improve conditions for healing, to optimize the functioning of topical antibiotics and to advance compliance to a two-step system approach for effective eye hygiene for Blepharitis, Conjunctivitis, and Dry...

20060116356 - Phosphonate analogs of hiv integrase inhibitor compounds: Novel HIV integrase inhibitor compounds having at least one phosphonate group, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed....

20060116357 - Phosphonooxy quinazoline derivatives and their pharmaceutical use: Quinazoline derivatives of formula (I) wherein A is 5-membered heteroaryl containing a nitrogen atom and one or two further nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy....

20060116358 - Inositol pyrophosphates, and methods of use thereof: The present invention comprises compounds, compositions thereof, and methods capable of delivering modified inositol hexaphospahte (IHP) comprising an internal pyrophosphate ring to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to...

20060116359 - 17.beta-(alpha-hydroxy)-esters of androstanes as intermediates for the preparation of 17.beta-fluorinated-androstane esters: Process for the preparation of polyhalogenated steroids, in particular of androstanic fluoro derivatives corticosteroids by means of the formation of new androstanic S-hydroxy alkyl or aralkyl-17-carbothioate intermediates....

20060116360 - Method of administering anti-angiogenic agents and a method of treating disease using same: A method of administering an anti-angiogenic agent to a human or an animal comprising administering the anti-angiogenic agent such that a plasma concentration of the anti-angiogenic agent in the human or animal is substantially continuously maintained above 1 ng/mL....

20060116361 - 5-amidino-2-hydroxybenzenesulfonamide derivatives, pharmaceutical compositions containing the same and intermediates for their preparation: R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally...

20060116362 - Nobel compounds having selective inhibiting effect at gsk3: The present invention relates to new compounds of formula (I) wherein: Z is N and X is CH or N; Y is CONR5; P is phenyl or a 5 or 6 membered heteroaromatic ring containing one or more heteroatoms selected from N, O or S; Q is phenyl or a...

20060116363 - Tricyclic derivatives as ltd4 antagonists: Compounds of formula (I) and their pharmaceutically acceptable salts are provided as well as processes for the manufacture of such compounds. The compounds are useful in the treatment or prevention of inflammatory and allergic diseases....

20060116364 - Selective estrogen receptor modulator: formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a...

20060116365 - Small molecule modulators of cytokine activity: and pharmaceutically acceptable derivatives thereof, wherein m, p, R1, R2, R3 and R4 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of diseases, disorders or conditions associated with...

20060116367 - Novel [1,4]benzodiazepines as vasopressin v2 receptor antagonists: The invention is directed to novel [1,4]benzodiazepine compounds useful as vasopressin receptor antagonists for treating conditions involving increased vascular resistance and cardiac insufficiency. Pharmaceutical compositions comprising [1,4]benzodiazepine compounds of the present invention and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver...

20060116366 - Spirocyclic ureas, compositions containing such compounds and methods of use: The present invention relates to spirocyclic ureas, compositions containing such compounds and methods of treatment The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus....

20060116368 - 4-piperidinecarboxamide modulators of vanilloid vr1 receptor: This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to hetero isonipecotic amides that are potent modulators of VR1 which are useful for the treatment and prevention of disease conditions in mammals....

20060116369 - Certain compounds, compositions, and methods: Compounds useful for treating cellular proliferative diseases are disclosed....

20060116370 - Substituted pteridines for the treatment of inflammatory diseases: The invention relates to new pteridines which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds....

20060116371 - Substituted pteridines for the treatment of inflammatory diseases: The invention relates to new pteridines which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds....

20060116372 - Substituted pteridines for the treatment of inflammatory diseases: The invention relates to new pteridines which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds....

20060116373 - Substituted pteridines for the treatment of inflammatory diseases: The invention relates to new pteridines which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds....

20060116375 - 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-alkoxy-7-ethynyl-3-quinolinecarbonitriles for the treatment of ischemic injury: R′ and R″ are independently alkyl of 1 to 3 carbon atoms, or R′ and R″, taken together with the nitrogen to which they are attached, can form a 5 or 6 membered saturated ring which may optionally contain an additional heteroatom selected from NR′″, O or S(O)n; n is...

20060116374 - Taxol enhancer compounds: R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ═O or ═S. Also disclosed are pharmaceutical compositions...

20060116376 - Therapeutic pyrazolo[3,4-b]pyridines and indazoles: wherein R2, R3, R4, R5, R6, R7, X, and L have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of central nervous disorders and conditions including attention deficit hyperactivity disorder, neuropathic pain, urinary incontinence, anxiety, depression, and...

20060116377 - Dialkylhydroxybenzoic acid derivatives containing metal chelating groups and their therapeutic uses: Novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups are disclosed. The novel compounds are used as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species and/or excess Zn ions, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds have not only low toxicity but...

20060116379 - Compounds exhibiting type x spla2 inhibiting effect: wherein R20 is —CH2COOH and the like; R21 is —COCONH2 and the like; R22 is C4-C6 alkyl; and the like; R23 is —CH2—R18 wherein R18 is aryl and the like; R24 is hydrogen or C1-C6 alkyl and the like; an optical active compound, a prodrug thereof, or a pharmaceutically acceptable...

20060116378 - Fused heterocyclic isoxazoline derivatives and their use as anti-derpressants: The invention concerns fused heterocyclic isoxazoline derivatives of Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof, more in particular, tetrahydropyranoisoxazole, hexahydroisoxazolopyridine, tetrahydrothiopyrano isoxazole and hexahydrobenzoisoxazole derivatives fused to a heterocyclic ring system via the 6-membered ring of...

20060116380 - Novel anthranilamide pyridinureas as vascular endothelial growth factor (vegf) receptor kinase inhibitors: The invention relates to novel anthranilamide pyridinureas as VEGF receptor kinase inhibitors, their production and use as pharmaceutical agents for preventing or treating diseases that are triggered by persistent angiogenesis....

20060116381 - 4-4(methylpiperazin-1-ylmethyl)-n-[4-methyl-3-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-ben-zamide for treating mutated-ret kinase associated diseases: The invention relates to the use of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide or a pharmaceutically acceptable salt thereof for the treatment of mutated-RET kinase associated disease, especially mutated-RET kinase associated thyroid cancer....

20060116382 - Lactam compounds and their use as pharmaceuticals: The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or...

20060116383 - Integrin antagonists useful as anticancer agents: and to pharmaceutically acceptable salts and solvates thereof, wherein A, X2, X4, X5 and X1 are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of Formula 1 and to pharmaceutical compositions for treating such disorders which contain the...

20060116384 - 1-aryl- or 1-alkylsulfonyl-heterocyclylbenzazoles as 5-hydroxytryptamine-6 ligands: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor....

20060116385 - Novel compounds having selective inhibiting effect at gsk3: The present invention relates to new compounds of formula (I) wherein Z is N; Y is CONR5, NR5CO, SO2NR5, NR5SO2, CH2NR5, NR5, NR5CONR5, CH2CO, CO, O or CH2O; X is CH or N; P is phenyl or a 5 or 6 membered heteroaromatic ring containing one or more heteroatoms selected...

20060116386 - Oxazolidinones as antibacterial agents: A compound of the formula (I), or a pharmaceutically-acceptable salt, or in-vivo hydrolysable ester thereof: Wherein C is selected from (D) and (E), R2a, R6a, and R3a are independently selected from for example H, CF3, Me and Et; R2b and R6b are independently selected from for example H, F, CF3,...

20060116387 - Hydrate of n-methyl-n-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-a]-pyrimidin-7-yl}phenyl)acetamide and processes and methods related thereto: A novel hydrate form of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide (“Compound No. 1”) and processes related to the use thereof in the synthesis of a polymorphic form of Compound No. 1....

20060116388 - Cxcr3 antagonists: Compounds, compositions and methods that are useful in the treatment of inflammatory and immune conditions and diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of a chemokine receptor. The subject methods are useful for the treatment of inflammatory and immunoregulatory disorders and...

20060116389 - Antibacterial oxazolidinones: A compound of the formula (I), or a pharmaceutically-acceptable salt, or in-vivo hydrolysable ester thereof: formula (I) wherein C is selected from D and E, formula (II) R2a, R6a, and R3a are independently selected from for example H, CF3, Me and Et; R2b and R6b are independently selected from for...

20060116390 - Hepatitis c virus inhibitors: The present invention relates to new compounds useful for the treatment or prevention of hepatitis C, process for preparing them, and a composition for the treatment or prevention of hepatitis C comprising the compounds as an active ingredient....

20060116391 - Process for preparing the calcium salt of rosuvastatin: An improved process for manufacture of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl)(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid calcium salt, which is useful for the production of a pharmaceutical useful in the treatment of, inter alia, hypercholesterolemia, hyperlipoproteinemia and atherosclerosis, is described....

20060116392 - Methods for treating anxiety disorders and related article of manufacture: This invention provides a method for treating a subject afflicted with an anxiety disorder whose symptoms are exacerbated by the subject's exposure to a predetermined eliciting event, which method comprises administering to the subject a therapeutically effective amount of a protein synthesis inhibitor before, during the time, and/or after the...

20060116393 - Substituted pyrido [2,1-a] isoquinoline derivatives: i

20060116394 - Fab i inhibitors: Compounds are disclosed which are Fab I inhibitors and are useful in the treatment bacterial infections....

20060116395 - 1h-pyrazole and 1h-pyrole-azabicyclic compounds for the treatment of disease: m

20060116396 - 5-substituted quinoline and isoquinoline derivatives, a process for their production and their use as anti-inflammatory agents:

20060116397 - Use of saquinavir as a radiation sensitizer: The present invention relates to the sensitization of a cell to radiation. In particular, the present invention relates to the use of a protease inhibitor to sensitize a cancer cell to radiation....

20060116398 - Compounds having beta2 adrenergic receptor agonist and muscarinic receptor antagonist activity: wherein R1, R2, R3, R4, R5, R6, R7, R8a, R8b, W, a and b are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both β2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Accordingly, such compounds are...

20060116399 - Diarylmethylidene piperidine derivatives, preparations thereof and uses thereof: Compounds of general formula: wherein R1, R2, R3, R4, and R5 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain....

20060116401 - Antibacterial compounds: A compound of the formula (I), or a pharmaceutically-acceptable salt, or in-vivo hydrolysable ester thereof wherein in (I) C is for example formula (D), (E), (H) wherein A and B are independently selected from formulae (i) and (ii) and R2b and R6b, R2b and R6a, R3a and R5a, are for...

20060116400 - Oxazolidinone and/or isoxazoline derivatives as antibacterial agents: A compound of the formula (I), or a pharmaceutically-acceptable salt, or in-vivo hydrolysable ester thereof formula (I) wherein in (I) C is for example formula (D), formula (E), formula (H) wherein A and B are independently selected from (i) formula (J) and (ii) formula (K) m is 1 or 2;...

20060116402 - N-substituted benzimidazolyl c-kit inhibitors and combinatorial benzimidazole library: c

20060116403 - Therapeutic target and uses thereof: The present invention relates to the finding of a novel therapeutic target which is implicated in regulating glycosaminoglycan (GAG) length, and the use of this target particularly for regulating lipoprotein binding. More particularly the invention relates to the use of this target for methods of treating and preventing conditions associated...

20060116404 - Cai-based systems and methods for the localized treatment of ocular and other diseases: The subject invention provides CAI compounds and formulations thereof, and methods for their use in the localized treatment of non-life threatening diseases. Formulations of CAI compounds of the subject invention include CAI free base and CAI prodrug microcrystallines, microparticles, emulsions, and the like. The subject invention further provides methods for...

20060116405 - Indol derivatives and their use as 5-ht ligands: The invention relates to indol derivatives of Formula (I) in which R1, R2, R3, X, A, n, m and p have the meanings indicated above....

20060116406 - 7-(1,3-thiazol-2-yl)thio!-coumarin derivatives and their use as leukotriene biosynthesis inhibitors: The instant invention provides compounds of Formula (I) which are leukotriene biosynthesis inhibitors. Compounds of formula (I) are useful as anti-asthmatic, anti-allergic, anti-inflammatory, cytoprotective and anti-artherosclerotic agents....

20060116407 - Amide derivatives: e

20060116408 - N-substituted benzothiophenesulfonamide derivatives: The present invention relates to an N-substituted benzothiophenesulfonamide derivative or a pharmaceutically acceptable salt thereof and applications thereof. Furthermore, it provides an agent for preventing or treating cardiac or circulatory disease and so on caused by abnormal increase of production of angiotensin II or endothelin I based on chymase activity,...

20060116410 - 4-aminomethyl benzamidine derivatives: e

20060116409 - Phospholipase inhibitors: A novel class of 3-oxo-3H-benzo[d]isoxazole carboxamide compounds is disclosed together with the use of such compounds for inhibiting hepatic lipase and/or endothelial lipase activity for treatment, amelioration or prevention of hepatic lipase and/or endothelial lipase mediated diseases....

20060116411 - Medicinal composition containing triazole compound: A pharmaceutical composition containing a triazole compound which is (2R,3R)-3-[[trans-2-[(1E,3E)-4-(4-cyano-2-fluorophenyl)-1,3-butadien-1-yl]-1,3-dioxan-5-yl]thio]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanol and at least one pharmaceutically acceptable basic substance, wherein a ratio of the triazole compound to the basic substance is 1:0.01 to 1:10; the triazole compound is in an amount of 1 to 2000 mg; and the composition has an...

20060116412 - Novel benzimidazole derivatives useful as selective androgen receptor modulators (sarms): The present invention is directed to novel benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor....

20060116413 - Methods for treating alzheimer's disease using hydroxyethylene compounds containing a heteroyclic amide bond isostere: Disclosed are methods for treating Alzheimer's disease, and other diseases, and/or inhibiting beta-secretase enzyme, and/or inhibiting deposition of A beta peptide in a mammal, by use of compounds of formula (I) wherein X, R1, and R2 are defined herein....

20060116414 - Disubstituted pyrazolyl carboxanilides: s

20060116415 - Novel tetracyclic heteroatom containing derivatives useful as sex steroid hormone receptor modulators: The present invention is directed to novel tetracyclic heteroatom containing derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation....

20060116416 - Ppar active compounds: Compounds are described that are active on at least one of PPARα, PPARδ, and PPARγ, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPARα, PPARδ, and PPARγ....

20060116417 - Thrombopoietin activity modulating compounds and methods: m

20060116418 - Materials and methods for treating hypercholesterolemia: The subject invention provides novel HMG-CoA-reductase inhibitors. In a preferred embodiment, the HMG-CoA reductase inhibitors of the subject invention can be deactivated to a primary inactive metabolite by hydrolytic enzymes. Compounds of the present invention can be advantageously used to treat patients suffering hypercholesterolemia....

20060116419 - Nf-kb inhibitors: The present invention provides a specific compound and methods for treating diseases related to the inhibition of IKK-β phosphorylation of IK....

20060116420 - Crystalline forms of 3'-tert-butyl-3'-n-tert-butyloxycarbonyl-4-deacetyl-3'-dephenyl-3'-n-debenzoyl-4-o-methoxycarbonyl-paclitaxel: e

20060116421 - Tetrahydropyranyl cyclopentyl benzylamide modulators of chemokine receptor activity: The present invention is directed to compounds of the formula (I) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R27, R28, R29, R30, R31, X, m, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these...

20060116422 - Prodrugs built as multiple self-elimination-release spacers: This invention concerns multiple release spacers and spacer systems, which release multiple leaving groups following a single activation. It concerns compounds comprising a specifier linked to two or more of the same or different leaving groups (L in the figure) via a self-eliminating multiple release spacer or spacer system, which...

20060116423 - Methods and compositions for treatment of central nervous system injury with isothiocyanates: Methods and compositions comprising isothiocyanates or derivatives or metabolites thereof, for attenuating or preventing central nervous system tissue damage, and/or improving cognitive function, are disclosed. Treatment of head trauma, spinal cord injury, stroke, aging, neurological diseases, and other insults to the central nervous system that compromise the blood-brain barrier, cause...

20060116424 - Short-acting sedative hypnotic agents for anesthesia and sedation: The invention provides compounds compositions and methods useful for inducing or maintaining general anesthesia or sedation in mammals....

20060116425 - Methods and compositions for the treatment and prevention of lung disease: Methods and compositions for the treatment of lung disease such as emphysema and/or bronchopulmonary dysplasia in a mammal. Also disclosed are methods and compositions promoting the formation of alveolar septa and increasing the gas-exchange surface area of a mammalian lung, and for the prevention and/or treatment of alveolar destruction....

20060116426 - Inhibitor for perioperative blood sugar elevation: An inhibitor for perioperative blood sugar elevation characterized by containing a branched amino acid, a compound which can be converted into a branched amino acid in vivo or a compound to which an amino group has been transferred from a branched amino acid. This inhibitor for perioperative blood sugar elevation...

20060116427 - Adapalene polymorphic forms: Novel adapalene crystalline and amorphous Forms, processes for the preparation thereof, their use for the purification of adapalene, pharmaceutical compositions containing the forms and the use thereof in therapy....

20060116428 - Intravitreally-injectable solution for the treatment of vitreous hemorrhages: The present invention relates to an ophthalmic solution for the clarification of vitreous hemorrhages. More specifically, it relates to a pharmaceutically acceptable intraocular injectable solution, for the treatment of vitreous hemorrhages, whereby the reabsorption of such hemorrhage is encouraged. It enables the clarification of the vitreous hemorrhage in a significantly...