Drug, bio-affecting and body treating compositions inventions 05/06

20060111271 - Active and passive immunization against pharmacologically active hapten molecules using a synthetic carrier compound composed of similar elements: The present invention relates to vaccine conjugates composed of a hapten linked to a carrier compound, which are used for active or passive immunization in order to elicit antibodies against the hapten. The carrier compound used in the present invention is composed of a multitude of typically dozens of similar...

20060111272 - Metabolically inert antifolates for treating disorders of abnormal cellular proliferation and inflammation: The present invention provides compositions and methods for the treatment of disorders of abnormal cell proliferation and/or inflammation, such as psoriasis and inflammatory bowel disease, in a human or other host animals....

20060111274 - Methods and compositions for enhancing transport across biological membranes: Methods and compositions for transporting drugs and macromolecules across biological membranes are disclosed. In one embodiment, the invention pertains to a method for enhancing transport of a selected compound across a biological membrane, wherein a biological membrane is contacted with a conjugate containing a biologically active agent that is covalently...

20060111273 - 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 polyglutamic 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...

20060111275 - Size enhanced hemoglobins: surface decoration and crosslinking of the protein with polyoxy alkylene glycols: Novel modified hemoglobins comprising polyalkylene glycols and novel methods for making those hemoglobins are provided. One group of modified hemoglobins comprise polyalkylene glycols bonded to the hemoglobin with an amide linkage at Glu-43(β). Additional polyalkylene glycols can also be bonded to the Glu-22(β) and/or the Asp-47(β). These hemoglobins are made...

20060111276 - Cidofovir peptide conjugates as prodrugs: Cidofovir-based compounds having an amino acid, dipeptide or tripeptide attached to a cidofovir or cyclic cidofovir framework. The compounds show enhanced oral bioavailability and increased binding to the PepT1 transporter. The present invention also provides compositions and methods for treating virus infections, and a method of preparing cidofovir....

20060111277 - Echinocandin/carbohydrate complexes: A complex of an echinocandin compound with a carbohydrate is described having improved thermal stability and water solubility. A process for making the echinocandin/carbohydrate complex is also described as well as the use of the complex in pharmaceutical formulations and treatments of fungal infections....

20060111279 - Glycopegylated erythropoietin: The present invention provides conjugates between erythropoietin and PEG moieties. The conjugates are linked via an intact glycosyl linking group interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from glycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified...

20060111278 - Tff peptides: A trefoil factor peptide....

20060111281 - Cyclic peptide compositions for treatment of sexual dysfunction: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, m and p are as defined. Further provided are compositions for treatment of sexual dysfunction in mammals, including male sexual dysfunction, such as erectile dysfunction, and female sexual dysfunction, by administration of a cyclic peptide including a...

20060111280 - Novel substance fki-1033 and process for producing the same:

20060111287 - Acetylated protein: An isolated multiply acetylated protein HMGB1; or a variant or fragment thereof, or a polynucleotide encoding therefor....

20060111293 - Antagonists for human prolactin: Modified prolactin molecules wherein the prolactin molecule comprises at least one mutation in a region selected from i) amino acids 41-57, ii) amino acids 94-110, and iii) amino acids 160-173; and wherein the at least one mutation is selected from deletions, replacements, and insertions. The modified prolactins are prolactin antagonists,...

20060111297 - Blood factor domains: The present invention provides methods and compositions for detecting, diagnosing, prognosing and monitoring the progress of diseases. Further provided are methods for screening to identify agonists and antagonists of antigens associated with these diseases....

20060111295 - Cellular receptors utilized as carrier agents for pharmaceutical compounds used in the treatment of arthritis, inflammation and immune disorders: This invention describes a method of utilizing soluble receptors such as tumor necrosis factor receptor or interleukin receptor to carry pharmaceutical compounds to areas of inflammation. Patients with inflammatory disease such as arthritis, or cardiomyopathy or other inflammatory conditions may benefit from this treatment....

20060111289 - Compositions and methods of using alpha-fetoprotein growth inhibitory peptides: This invention describes compositions related to growth inhibitory protein-derived peptide fragments. These fragments can be identified by several methods including homology comparison and amino acid pairing techniques. Certain fragment sequences have been shown to provide homology to various biological activities and are contemplated as potential therapeutic agents. These biological activities...

20060111298 - Compositions and therapeutic methods using morphogenic proteins and stimulatory factors: The present invention provides pharmaceutical compositions comprising a morphogenic protein stimulatory factor (MPSF) for improving the tissue inductive activity of morphogenic proteins, particularly those belonging to the BMP protein family. Methods for improving the tissue inductive activity of a morphogenic protein in a mammal using those compositions are provided. This...

20060111292 - Compositions for mucosal and oral administration comprising hcg fragments: The invention relates to the field of immunology, more specifically to the field of immune-mediated disorders such as allergies, auto-immune disease, transplantation-related disease and other inflammatory diseases. The invention in particular relates to the systemic treatment of inflammatory disease by oral or mucosal administration of a pharmaceutical composition with a...

20060111282 - Factor vii or viia polypeptide variants: The present invention relates to novel polypeptide variants of factor VII (FVII) or factor VIIa (FVIIa) polypeptides, where said variants comprise an amino acid substitution in position 10 and 32 and where said variants further comprise a sugar moiety covalently attached to an introduced in vivo N-glycosylation site located outside...

20060111284 - Method for treating cancer: A method of treating lymphoma, ovarian cancer, colorectal cancer, or gastric cancer by administering an effective amount of Mesna to a patient is provided. A method for treating and reducing the effective dose of an anti-cancer agent by administering Mesna in conjunction with an anti-cancer agent is also provided....

20060111286 - Method of modulating endothelial cell activity: The present invention relates generally to a method of modulating endothelial cell activity and to agents useful for same. More particularly, the present invention relates to a method of modulating intercellular vascular endothelial permeability by modulating an intracellular protein kinase C-dependent signalling mechanism. The method for the present invention is...

20060111288 - Peripheral benzodiazepine receptor independent superoxide generation: A method of treating cancer through the application of a compound that causes the intra-mitochondrial generation of reactive oxygen species in tumor cells by a mechanism that is independent of the peripheral benzodiazepine receptor....

20060111296 - Plasmin-inhibitory therapies: The disclosure features a method of treating cancers, angiogenesis-related disorders and lymphangiogenesis-related disorders with plasmin inhibitors. An exemplary method includes: administering, to a subject, a plasmin inhibitor, such as a protein that includes a Kunitz domain that inhibits plasmin....

20060111283 - Prevention therapy and prognosis/monitoring in sepsis and septic shock: The invention relates to the use of a peptide which binds to lipopolysaccharide (LPS) or lipoteichoic acid (LTA), for manufacturing a pharmaceutical composition for treating sepsis or septic shock, wherein the peptide comprises the amino acid sequence of apolipoprotein CI (apoCI) or a part thereof that comprises at least the...

20060111294 - Use of a polypeptide domain to modulate the tumorigenic and metastatic potential of cancer cells: The present invention relates to the use of a polypeptide domain to modulate the tumorigenic and metastatic potential of cancer cells. More specifically, the present invention relates to a domain of a Secretory Leukocyte Protease Inhibitor (SLPI) to modulate tumor invasiveness and/or metastasis. It further relates to compounds, such as...

20060111285 - Use of granme b as an hsp70/hsp70 peptide dependent inducer of apoptosis in tumor cells: The present invention relates to a method of inducing or enhancing the expression of granzyme B in natural killer (NK) cells. The present invention relates also to a use of said NK cells for the preparation of a pharmaceutical composition for the treatment of tumors, viral or bacterial infections or...

20060111290 - Use of sdf-1 or g-csf to improve myocardial function after ischemic injury: This invention provides methods of improving myocardial function in a subject after ischemic injury comprising administering G-CSF or SDF-1 to the subject....

20060111291 - Uv device for treating osteolysis: Irradiating osteolytic regions with UVB light....

20060111299 - Compositions and methods for treating atherosclerosis: Peptides and mimetics of selected domains of mammalian serum amyloid A isoform 2.1 (SAA2.1) and compounds and compositions thereof are provided that enhance the effect on macrophage cholesterol ester hydrolase activity and/or inhibit acyl CoA:cholesterol acyl transferase activity. Methods of using these compositions in the treatment and/or prevention of atherosclerosis...

20060111300 - Antimicrobial amino acid sequences derived from alpha-melanocyte-stimulating hormone: The presence of the ancient anti-inflammatory peptide α-melanocyte stimulating hormone (α-MSH [1-13], SYSMEHFRWGKPV) in barrier organs such as gut and skin suggests a role in the nonspecific (innate) host defense system. α-MSH and other amino acid sequences derived from α-MSH were determined to have antimicrobial influences, including against two major...

20060111301 - Methods for preventing and treating alzheimer's disease: The invention relates to the use of a compound comprising the following amino acid sequence X1X2X3X4X5X6, wherein X1 is an amino acid, except of C, X2 is an amino acid, except of C, X3 is an amino acid, except of C, X4 is an amino acid, except of C, X5...

20060111302 - Compositions and methods to reduce mutagenesis: The present invention provides methods and compositions for said inhibition of drug resistance. In one embodiment, said invention provides methods and compositions for said inhibition of antibiotic resistance. The invention generally involves said administration of achaogens, agents that inhibit said mutational process, to inhibit said evolution of drug resistance. Also,...

20060111304 - Anthranyl derivatives having an anticholecystokinin activity (anti-cck-1), a process for their preparation, and pharmaceutical use thereof: Anthranylic compounds having anti-CCK activity of general formula (I) in which, n is a whole number lying between 0 and 7; R1 is chosen independently from the groups (II), in which X1 is chosen independently from, S, O, NR2 and X2 is a group chosen from: H, C1-C4 alkyl, F,...

20060111303 - Diketohydrazine derivative compounds and drugs contaiing the compounds as the active ingredient: The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory...

20060111305 - Metabolites of certain [1,4]diazepino[6,7,1-ij]quinoline derivatives and methods of preparation and use thereof: e

20060111306 - Dehydroephiandrosterone and ubiquinone compositions for treating asthma and bronoconstriction: A composition and various formulations comprise preventative or therapeutic amounts of an epiandrosterone, analogue thereof or salt thereof, and/or a ubiquinone or salt thereof, and a pharmaceutically or veterinarily acceptable carrier or diluent. The composition and formulations are useful for treating bronchoconstriction, respiratory tract inflammation and allergies, asthma, and cancer....

20060111308 - Methods and compositions for therapeutic treatment: Methods and compositions are described for the modulation of central nervous system and/or fetal effects of substances. Methods and compositions are described for the modulation of efflux transporter activity to increase the efflux of drugs and other compounds out of a physiological compartment and into an external environment. In particular,...

20060111307 - Methods and compositions for treating pain: Methods and compositions are described for the modulation of central nervous system and/or fetal effects of substances. Methods and compositions are described for the modulation of efflux transporter activity to increase the efflux of drugs and other compounds out of a physiological compartment and into an external environment. In particular,...

20060111309 - Chalcomycin derivatives: The invention relates to novel chalcomycin derivatives, medicaments containing said derivatives or the salts thereof, and the use of chalcomycin derivatives for treating diseases, especially infections. The inventive chalcomycin derivatives are acylated on the sugar esters and derivatives are also acylated on the 9-carbonyl function....

20060111310 - Composition comprising triterpene saponins and compounds with angeloyl functional group, methods for preparing same and uses thereof: This invention provides a compound comprising a triterpenoidal saponin, triterpenoid, triterpenoidal compound or sapongenin, comprising at least two side groups selected from the group consisting of: angeloyl groups, tigloyl groups and senecioyl groups, wherein the side groups are attached to carbon 21, 22 or/and 28 of triterpenoidal saponin, triterpenoid, triterpenoidal...

20060111311 - 5-nitro-nucleoside compounds for treating viral infections: Disclosed are compounds, compositions and methods for treating viral infections caused by a flaviviridae family virus, such as hepatitis C virus....

20060111312 - Antigene locks and therapeutic uses thereof: An oligonucleotide based therapeutic strategy, called anti-gene locks, is described which specifically kills cells based on their genotype. The strategy employs oligonucleotides with arms and a backbone that are complementary to both strands of the gene target. Anti-gene locks bind in vitro in a sequence dependent fashion and inhibit DNA...

20060111315 - Method for inhibition of pathogenic microorganisms: Disclosed is a method for inhibiting the growth of a microorganism by high efficiency transfection of a human host cell with a nucleic acid encoding an antimicrobial agent, such that the host cell expresses the antimicrobial agent effective to inhibit growth of the microorganism....

20060111314 - Method for treating or preventing metastasis of colorectal cancers: Disclosed are methods of detecting metastasis of colorectal cancer using differentially expressed genes. Also disclosed are methods of identifying agents for treating colorectal cancer or preventing metastasis of colorectal cancer....

20060111313 - Nell-1 enhanced bone mineralization: This invention pertains to the discovery that the human NELL-1 gene induces or upregulates bone mineralization. The HELL-1 gene or gene product thus provides a convenient target for screening for modulators of bone mineralization. In addition, HELL-1 can be used to facilitate repair of bone fractures and/or to generally increase...

20060111316 - Treatment of inflammatory, non-infectious, autoimmune, vasculitic, degenerative vascular, host-v-graft diseases, alzheimers disease, and amyloidosis using mammalian, dsdna vaccination: The present invention relates generally to compositions and methods using mammalian, dsDNA (Double Stranded Deoxyribonucleic Acid) vaccination for the induction and maintenance of regulator suppressor T cells resulting in suppression of non infectious, and post infectious, inflammatory, allergic, auto-immune, vasculitic, certain degenerative vascular, and graft versus host diseases, with or...

20060111317 - Rapid two-step synthesis of anti-coagulants: The present invention provides methods for the production of N-deacetylate N-sulfate derivatives of non-sulfated N-acetyl heparosan (HS) polysaccharides, compounds thus obtained and compositions comprising same. This invention also provides applications of N-deacetylate N-sulfate derivatives of non-sulfated N-acetyl heparosan (HS) polysaccharides, and compositions comprising same, for use in controlling coagulation and...

20060111318 - Agent for treating eye diseases: An agent for treating various kinds of diseases which contains at least one selected from the group consisting of sexual steroid hormone such as estrogen or its metabolites, its derivative, structural analogues thereof, estrogen acting substance or SERM non-feminizing estrogen (non-hormonal estrogen), and an activator of sirtuin and has a...

20060111319 - Use of dextran sulfate: The present invention refers to use of dextran sulfate, or a pharmaceutically acceptable derivate thereof, for manufacturing of a medicament for treatment of Instant Blood-Mediated Inflammatory Reaction (IBMIR). In addition, the invention refers to the use of dextran sulfate, or a pharmaceutically acceptable derivate thereof, for manufacturing of a medicament...

20060111321 - 2-methylene-19-nor-1alpha-hydroxy-17-ene-homopregnacalciferol and its uses: This invention discloses 2-methylene-19-nor-17-ene vitamin D analogs, and specifically 2-methylene-19-nor-α-hydroxy-17-ene-homopregnacalciferol 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...

20060111320 - Fungicidal mixtures based on a triazolopyrimidine derivative and azoles: Disclosed are fungicidal mixtures containing A) a triazolopyrimidine derivative of formula (1), and B) an azole derivative or the salts or addition compound thereof selected among bromuconazole, difenoconazole, diniconazole, fenbuconazole, fluquinconazole, flusilazole, hexaconazole, prochloraz, tetraconazole, triflumizole, flutriafol, myclobutanil, penconazole, simeconazole, ipconazole, triticonazole, and prothioconazole as active components in a synergistically...

20060111322 - Indazole compounds, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation: The invention is directed to intermediates useful for making indazole compounds that modulate and/or inhibit cell proliferation....

20060111323 - Use of polysiloxanes having quaternary ammonium groups as formulation auxiliaries, and compositions comprising them: The present invention relates to the use of polysiloxanes containing at least one quaternary ammonium group as formulation auxiliaries in formulations of pharmaceutically and veterinary active compounds, and to compositions comprising a) a pharmaceutically or veterinary active compound and b) a polysiloxane derivative containing at least one quaternary ammonium group...

20060111324 - (+)-ttrans-isomers of (1-phosphonomethoxy-2-alkylcyclopropyl)methyl nucleoside derivatives, process for the preparation of stereoisomers thereof, and use of antiviral agents thereof: The present invention relates to (+)-trans-isomers of (1-phosphonomethoxy-2-alkylcyclopropyl)methyl nucleoside derivatives of the formula (1) which are useful as an antiviral agent (particularly, against hepatitis B virus), pharmaceutically acceptable saltss, hydrates, or solvates thereof, and processes for the preparation of stereoisomers of the compounds of the formula (1), and a composition...

20060111325 - Acyloxyalkyl carbamate prodrugs, methods of synthesis, and use: Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, methods of making prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, methods of using prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof and...

20060111326 - New phosphoramide derivatives: New phosphoramide derivatives of formula (I) and the salts and solvates thereof, wherein the meanings of the various substituents are as disclosed in the description. Said compounds are useful as antiinflammatory and analgesic agents....

20060111327 - Derivatives of triptolide having a high immunosuppressive effect and high water solubility, and uses thereof: The present invention provides water soluble triptolide derivatives of formula I, II, IIIa, and IIIb, which have high immunosuppressive activity and in which R1 and R2 have the same meanings as defined in claims. The present invention also provides chemically synthetic methods of the triptolide derivatives of formula I, II,...

20060111328 - Carbamoyl-and thiocarbamoyl-phosphonates and pharmaceutical compositions comprising them: e

20060111329 - Anticancer agents based on regulation of protein prenylation: Oncoproteins such as Ras and RhoB are known to induce cell division in an unrestrained manner when such proteins are localized at the inner surface of a cancer cell membrane. The localization is effected by the prenylation reaction, whereby a hydrophobic group (e.g. a farnesyl group) is attached to the...

20060111330 - 17,20(e)-dehydro vitamin d analogs and their uses: This invention discloses 17,20(E)-dehydro vitamin D analogs, and specifically 17(E)-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...

20060111331 - Gave10 agonists for treating inflammation: i

20060111334 - Oral solid dosage forms containing a low dose of estradiol: The present invention relates to oral solid dosage forms containing a very low dose of estradiol. The dosage forms are formulated in a manner so as to avoid degradation of the estradiol and to minimise the content of polyvinylpyrrolidone, while still achieving similar fast dissolution of the estradiol. The dosage...

20060111332 - Process and intermediates to prepare17beta-hydroxy-7alpha-methyl-19-nor-17alpha-pregn -5(10)-en-20-yn-3-one: The present invention is a process for the preparation of 17β-hydroxy-7α-methyl-19-nor-17α-pregn-5(10)-en-20-yn-3-one (17α-ethynyl-17β-hydroxy-7α-methyl-5(10)-estren-3-one, tibolone) of formula 1, which comprises hydrolysis of 17α-ethynyl-17β-hydroxy-7α-methyl-5(10)-estrene 3,3-cyclic ketals of formula 2, where groups R1, R2, R3 and R4 are hydrogen atoms or alkyl groups, or R1 and R3, taken together with the carbon atoms within...

20060111333 - Structural, behavioral characterization, and synthesis of attractants for migratory lamprey: Compounds that function as lamprey attractants and methods....

20060111335 - Photoactivated anti-viral and anti-cancer agent: Bisbipyridyl rhodium (III) compound and methods for photo-induced inactivation of pathogenic contaminants in biological materials....

20060111336 - Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes: The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed...

20060111338 - 2-amino-4-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors: e

20060111337 - Substituted biaryl quinolin-4-ylamine analogues: Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat...

20060111339 - Novel oral general anesthetics and metabolitically resistant anticonvulsants: The present invention is directed to novel themisone derivative compounds that have been modified to prevent the formation of the toxic metabolite, 2-phenyl-acrylamide. Compositions comprising such derivative compounds have activity as anesthetics and as neuroprotective agents....

20060111340 - 1-thia-3-aza-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof: The present invention relates to derivatives of 1-thia-3-aza-dibenzoazulene class, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of tumour necrosis factor-α (TNF-α) production and the inhibition of interleukin-1 (IL-1) production as well...

20060111341 - Use of galanthamine and the derivatives thereof in the production of medicaments: The invention relates to the use of galanthamine and the cholinergically active derivatives thereof in the production of medicaments for preventive treatment of postoperative delirium and/or subsyndronal postoperative delirium. Galanthamine, the galathamine derivative(4aS,6R,8aS)-6-hydroxy-3-methoxy-11-methyl-4a,5,9,10-tetrahydro-6H-benzofuro[3a,3,2-ef][2]benzazepinium bromide and analogous salts, hydrates or solvates are advantageously suited for use according to the invention....

20060111342 - Insecticidal tricyclic derivatives: It has now been found that certain tricyclic derivatives have provided unexpected insecticidal activity. These compounds are represented by formula I: wherein R1 through R8, inclusively, and X and Y are fully described. Compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an...

20060111343 - Oxcarbazepine dosage forms: Dosage forms of oxcarbazepine or a pharmaceutically acceptable salt thereof and a pH modifying agent for use in oral administration are provided....

20060111344 - Arylethanolamine beta2-adrenoreceptor agonist compounds: The present invention relates to compounds of formula (I) as defined herein and salts or solvates thereof. Processes for preparing these compounds and pharmaceutical formulations containing them are also disclosed, as well as methods for the prophylaxis of treatment of a clinical condition using such compounds....

20060111345 - Pharmaceutical compositions comprising a selective cox-2 inhibitor and a diuretic: In a first aspect, the present invention includes a pharmaceutical composition comprising a COX-2 inhibitor and a diuretic. Such a composition can be used to treat a patient suffering from, for example, osteoarthritis, rheumatoid arthritis, juvenile rheumatoid arthritis, pain, primary dysmenorrhea, migraine, or colorectal polyps. The disclosure provides methods as...

20060111346 - Methods of modulating high-density lipoprotein cholesterol levels and pharmaceutical formulations for the same: Method of modulating High-Density Lipoprotein Cholesterol (HDL-C) levels in a mammal by administering to the mammal a therapeutically effective amount of a fluphenazine ester derivative. Pharmaceutical formulations for administration of the fluphenazine ester derivative are also disclosed....

20060111347 - Substituted sulfones and methods of use: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject...

20060111348 - Combination therapy using an 11beta-hydroxysteroid dehydrogenase type 1 inhibitor and an antihypertensive agent for the treatment of metabolic syndrome and related diseases and disorders: Combination therapy comprising the administration of an 11β-hydroxysteroid dehydrogenase type 1 inhibitor and an antihypertensive agent useful for treating, preventing and reducing the risk of developing insulin resistance, dyslipidemia, obesity, hypertension and other related diseases and disorders....

20060111349 - (arylamidoaryl)squaramide compounds: or a pharmaceutically acceptable salt or N-oxide thereof, wherein A, Q, Y, R5, m and J are defined herein, are useful in the treatment of tumors and cancers such as mastocytosis/mast cell leukemia, gastrointestinal stromal tumors (GIST), germ cell tumors, small cell lung carcinoma (SCLC), sinonasal natural killer/T-cell lymphoma, testicular...

20060111351 - Aryl sulfonamides: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated...

20060111350 - Solid forms of linezolid and processes for preparation thereof: Novel crystalline forms of Linezolid, designated as Form TIII, Form V, Form VI, Form IX, Form X, Form XII, Form XIV, Form XVII, and Form XVIII, are disclosed. The novel crystalline forms are characterized by powder X-ray diffraction, FTIR and FTRaman spectroscopy, and differential scanning calorimetry. Methods of preparing the...

20060111352 - Acetylenic compounds useful in treating inflammatory disorders: This invention is directed to acetylenic compounds as inhibitors of a nicotinamide adenine dinucleotide oxidase hydride donor useful in treating or ameliorating a reactive oxygen species mediated inflammatory disorder....

20060111353 - Substituted arylcyclopropylacetamides as glucokinase activators: According to the present invention there is provided a compounds of formula (I): and pharmaceutically acceptable salts thereof....

20060111354 - Medicaments containing vardenafil hydrochloride trihydrate: The invention relates to a method for producing medicaments that contain vardenafil hydrochloride, essentially as trihydrate in solid form, and to medicaments that can be obtained according to this method...

20060111355 - Gonadotropin releasing hormone receptor antagonists: The present invention relates to Gonadotropin Releasing Hormone (“GnRH”) (also known as Luteinizing Hormone Releasing Hormone) receptor antagonists....

20060111356 - External preparation for allergic diseases: The invention presents an external preparation for allergic diseases containing 3′-hydroxymethyl-4-hydroxypyrrolido[1,2-f]2′,5′-pipera-zinedione as an active ingredient. This compound has a prophylactic and therapeutic effect of allergic diseases, and the external preparation of the invention can be used in prophylaxis and treatment of various allergic diseases (for example, atopic dermatitis, urticaria, allergic...

20060111357 - Quinoline compounds for use in mch receptor related disorders: The present invention relates to the use of quinoline compounds for the preparation of a pharmaceutical and/or a cosmetic composition for the treatment, prophylaxis and/or diagnosis of a condition caused by or involving a melanin-concentrating hormone. The invention also relates to novel quinoline compounds per se. The quinoline compounds have...

20060111358 - Treatment of aml: wherein the radicals and symbols have the meanings as defined in the specification, together or in combination with a conventional compound or compound mixture useful in AML treatment, in particular a topoisomerase II inhibitor, an antimetabolite, or an antitumor antibiotic, for simultaneous, separate or sequential use; and to a pharmaceutical...

20060111359 - Inhibitors of fatty acid amide hydrolase: Improved competitive inhibitors of FAAH employ an α-keto heterocyclic pharmacophore and a binding subunit having a ?-unsaturation. The α-keto heterocyclic pharmacophore and a binding subunit are attached to one another, preferably by a hydrocarbon chain. The improvement lies in the use of a heterocyclic pharmacophore selected from oxazoles, oxadiazoles, thiazoles,...

20060111360 - Bicyclic compounds as selective melanin concentrating hormone receptor antagonists for the treatment of obesity and related disorders: wherein V, W, Y, Z, R1, R2, R3, R4, d, m, n, p and r are herein defined, said compounds being novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as...

20060111361 - Method of reversing left ventricle remodeling: The present invention relates to method of reversing left ventricle remodeling by combined administration of therapeutically effective amounts ranolazine and at least one co-remodeling agent, which may be an ACE inhibitor, an ARB, or a beta-blocker. The method finds utility in the treatment of heart failure. This invention also relates...

20060111362 - 1,3-dihydroimidazole ring compound: represents a double bond or a single bond; X3 denotes an oxygen atom or a sulfur atom; X1 denotes a C2-6 alkyl group which may have substituents; Z1 denotes a nitrogen atom or the formula —CR3═; Z2 and Z3 each independently denote a nitrogen atom, the formula —CR1═, a carbonyl...

20060111364 - Cathepsin cysteine protease inhibitors and their use: The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F, L and B. Of particular interest are diseases associated with Cathepsin S. In addition this invention also discloses processes for the preparation of...

20060111365 - Combinations comprising n- {5-[4- [4-methy l-piperazino-methyl) -benzoylamido] -2-methylphenyl) -4- (3-pyridyl) -2-pyrimidine-amine and at least one telomerase inhibitor: The invention relates to a method of treating a warm-blooded animal, especially a human, having a proliferative disease comprising administering to the animal a combination which comprises (a) N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine and (b) at least one telomerase inhibitor, to a combination comprising (a) and (b) as defined above and optionally at least...

20060111363 - Treatment of uveal melanoma: e

20060111366 - Pharmaceutical use of substituted amides: The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture...

20060111367 - Sulfur-containing naphthalimide derivatives: The invention discloses novel sulfur-containing naphthalimide derivatives, and the preparation and uses thereof. The conjugated plane of naphthalimide derivatives of the invention is enlarged by incorporating 5-or 6-membered heteroaromatic ring and/or introducing S heteroatom, thus increasing the anti-tumor activity of naphthalimide. The compounds of the invention displays significant inhibiting activities...

20060111368 - Phosphodiesterase inhibitor: [wherein n represents an integer of from 1 to 4, R1 represents substituted or unsubstituted lower alkyl, —C(═Y)R9 or the like, R2 represents a hydrogen atom, substituted or unsubstituted lower alkyl or the like, R3 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, a substituted or unsubstituted heterocyclic...

20060111369 - Synthesis, characterization and biological action of optically active isomers of floxacins: Disclosed herein is the method for synthesis and separation of enantiospecific isomers of floxacins. These isomers can be used to study the antibacterial action, as well as cardiac effects, such as arrhythmogenic activity, QT internal prolongation and dispersion, and Ikr inhibition in humans. A method for the identification of chiral...

20060111370 - Heterocyclic aspartyl protease inhibitors: s

20060111371 - Protein tyrosine kinase inhibitors: wherein R1 and R2 are independently selected from the group consisting of H; alkyl; alkenyl; alkynyl; halogen; aryl; heteroaryl containing N, O, or S; the aryl and heteroaryl may be further substituted with halogen, an alkyl, alkenyl, and alkynyl; NZ1Z2, wherein Z1 and Z2 are independently selected from the group...

20060111372 - Alkyl-substituted pyrazolopyrimidines: The invention relates to novel alkyl-substituted pyrazolopyrimidines, process for their preparation, and the use thereof for producing medicaments for improving perception, concentration, learning and/or memory....

20060111373 - Pyrazolo [3,4-d] pyrimidine derivatives and their use as purinergic receptor antagonists: Use of a compound of formula (I): wherein R1 is selected from alkyl, alkoxy, aryloxy, alkylthio, arylthio, aryl, halogen, CN, NR6R7, NR5COR6, NR5CONR6R7, NR5CO2R8 and NR5SO2R8; R2 is selected from heteroaryl attached via an unsaturated carbon; R3 is selected from H, alkyl, halogen, OR5, SR5 and NR6R7; R4 is selected...

20060111374 - Compounds, compositions, and methods: Compounds, compositions and methods useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed....

20060111375 - Compound having tgfß inhibitory activity and medicinal composition containing the same: wherein X represents CH or N; Z represents —O—, —NH— or —C(═O)—; R and R′ represent a hydrogen atom, hydroxyl, a halogen atom, optionally substituted alkyl, optionally substituted alkenyl optionally substituted alkoxy, amino, aminocarbonyl, or an optionally substituted heterocyclic group; and A represents an optionally substituted specific carbocyclic or heterocyclic...

20060111376 - 2,4-diamino quinazoline and pyridopyrimidine ester derivatives as dihydrofolate reductase inhibitors: The invention provides novel compounds or the formula II: wherein R1, R2, R3 and R4 are independently hydrogen of a group that liberates the free amine in vivo, for example —CO-alkyl, preferably —CO—C1-C3 alkyl or pivalate; or —COhaloalkyl, preferably —CO—C1-C3 haloalkyl, most preferably —CO—C1-C3 chloroalkyl; wherein W is: and @...

20060111377 - Heterocyclic derivatives: The invention relates to novel heterocyclic derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development....

20060111378 - Substituted 2-anilinopyrimidines as cell-cycle-kinase or receptor-tyrosine-kinase inhibitors, their production and use as pharmaceutical agents: e

20060111379 - Substituted 2-anilinopyrimidines as cell-cycle-kinase or receptor-tyrosine-kinase inhibitors, their production and use as pharmaceutical agents: The present invention relates to a pharmaceutical composition comprising as active ingredient the hydrochloric acid salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile and to processes for their preparation....

20060111380 - Novel azole derivatives: wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted by a substituent, and at least two of T, U, V and W are...

20060111381 - Amidine compounds: Amidine derivatives of opioids of the formula YN—X—(NH)n-C(═NR)—R′ in which YN is a morphine-like opioid radical; X is a direct bond, a substituted or unsubstituted, branched, straight-chained or cyclic alkylene having from 1 to 6 carbon atoms, optionally containing one or two heteroatoms in the alkyl chain, or an optionally...

20060111382 - Compositions and methods for treating or preventing pain: Disclosed herein are compositions and methods which treat or prevent pain in a subject. More specifically, disclosed herein are compositions of nicotinic agonists, salts, hydrates, solvates, prodrugs or metabolites thereof and opioid agonists salts, hydrates, solvates, prodrugs or metabolites thereof, pharmaceutical compositions thereof and methods of using these compositions and...

20060111383 - Preparation of oxycodone: A process for preparing oxycodone or an oxycodone salt, wherein the oxycodone or oxycodone salt has low levels of impurities (especially 14-hydroxycodeinone) is disclosed. The process comprises the steps of: a) preparing a mixture comprising oxycodone and a solvent and adjusting the pH of the mixture to less than 6;...

20060111384 - 4-hydroxybenzomorphans: 4-Hydroxybenzomorphans containing carboxamide or thiocarboxamide at the 3-position are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications....

20060111385 - Novel 4-phenyl substituted tetrahydroisoquinolines and therapeutic use thereof: The present invention relates to a method of treating disorders including cognition impairment, generalized anxiety disorder, acute stress disorder, social phobia, simple phobias, pre-menstrual dysphoric disorder, social anxiety disorder, major depressive disorder, eating disorders, obesity, anorexia nervosa, bulimia nervosa, binge eating disorder, substance abuse disorders, chemical dependencies, nicotine addiction, cocaine...

20060111386 - Novel 4-phenyl substituted tetrahydroisoquinolines and therapeutic use thereof: The present invention relates to a method of treating disorders including cognition impairment, generalized anxiety disorder, acute stress disorder, social phobia, simple phobias, pre-menstrual dysphoric disorder, social anxiety disorder, major depressive disorder, eating disorders, obesity, anorexia nervosa, bulimia nervosa, binge eating disorder, substance abuse disorders, chemical dependencies, nicotine addiction, cocaine...

20060111387 - Aryl substituted imidazoquinolines: Aryl substituted imidazoquinoline compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed....

20060111388 - Phenanthroline and derivatives thereof used to lower intraocular pressure in an affected eye: Methods and compositions used for lowering intraocular pressure. More particularly, the methods and compositions for lowering intraocular pressure pertain to the use of at least a phenanthroline derivative in an ophthalmic delivery solution....

20060111389 - Therapeutic acridone and acridine compounds: The present invention pertains to acridone and acridine compounds of formula (I), wherein either: (a) K is ═O, L is —H, alpha is a single bond, beta is a double bond, gamma is a single bond (acridones): or, (b) K is a 9-substituent. L is absent, alpha is a double...

20060111390 - Azaindoles as inhibitors of c-jun n-terminal kinases: The present invention relates to novel 5-substituted 7-azaindole compounds of formula (I), their use in the inhibition of c-Jun N-terminal kinases, their use in medicine and particularly in the prevention and/or treatment of neurodegenerative disorders related to apoptosis and/or inflammation. The invention also provides processes for manufacture of said compounds,...

20060111391 - Pyridine imidazoles and aza-indoles as progesterone receptor modulators: The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders mediated by one or more estrogen receptors. The compounds of the invention are useful in the treatment of disorders associated with the depletion of estrogen such as...

20060111392 - Substituted biaryl-carboxylate derivatives: Substituted biaryl-carboyxlate derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway....

20060111393 - 4-phenyl substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine and serotonin: b

20060111396 - 4-phenyl substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine and serotonin:

20060111394 - Aryl-and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine and serotonin:

20060111395 - Aryl-and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine and serotonin:

20060111397 - Methods and compositions for treating diseases associated with excesses in ace: Over 40 common diseases, in addition to congestive heart failure (CHF) due to hypertension (HTN) or non-insulin dependent diabetes mellitus (type II diabetes mellitus) (NIDDM), atherosclerotic peripheral vascular disease (ASPVD) due to HTN or NIDDM, and chronic obstructive pulmonary disease; emphysema (COPD), are associated with the ACE D/D genotype and...

20060111398 - Therapeutic use of farnesyltransferase inhibitors and methods of monitoring the efficacy thereof: The therapeutic use of farnesyltransferase inhibitors (e.g., tipifarnib) for the treatment of sepsis is described. Methods useful to monitor the effectiveness of such treatment are also described....

20060111399 - Salts of n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and their preparation: Disclosed herein are salts of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide including the citrate, fumarate, maleate, malate, phosphate, succinate, sulphate, and edisylate salts....

20060111400 - Piperidinetriol derivatives as inhibitors of glycosylceramidsynthase: Compounds of formula (I); wherein R represents various substituent groups, are useful as inhibitors of glucosylceramide synthase....

20060111401 - Taxanes having a c10 carbonate substituent: Taxanes having a methylcarbonate or ethylcarbonate substituent at C(10), a hydroxy substituent at C(7), and a range of C(13) side chain substituents....

20060111402 - 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....

20060111403 - Cyano anthranilamide insecticides: This invention provides compounds of Formula (I), N-oxides and suitable salts thereof INSERT FORMULA I HERE wherein R1 is Me, Cl, Br or F; R2 is F, Cl, Br, C1-C4 haloalkyl or C1-C4 haloalkoxy; R3 is F, Cl or Br; R4 is H or C1-C4 alkyl, C3-C4 alkenyl, C3-C4 alkynyl,...

20060111404 - Salts of n-[2-({(3r)-1-[trans-4-hydroxy-4-(6-methoxypyridin-3-yl)-cyclohexyl]pyrrolidin-3-yl}amino)-2-oxoethyl]-3-(trifluoromethyl)benzamide: The present invention pertains to bis(methanesulfonic acid), bis(ethanesulfonic acid), and camphoric acid salts of chemokine receptor inhibitor N-[2-({(3R)-1-[trans-4-hydroxy-4-(6-methoxypyridin-3-yl)-cyclohexyl]-pyrrolidin-3-yl}amino)-2-oxoethyl]-3-(trifluoromethyl)-benzamide, methods of preparing the same, and methods of using the same....

20060111405 - O-pyridinequinone derivatives, the composition containing the derivatives, the process for preparation of the derivatives and the use of the derivatives: The present invention relates to the o-pyridinequinone disubstituted derivatives, the composition containing the derivatives, the process for preparation of the derivatives and the use of the derivatives. The o-pyridinequinone disubstituted derivatives of the present invention have action of selectivity inhibiting COX-2 and they can be made into pharmaceuticals. The o-pyridinequinone...

20060111406 - Amide linker peroxisome proliferator activated receptor modulators: The present invention is directed to compounds, compositions, and use of compounds the structural Formula (I)....

20060111407 - Association between a heterocyclic compound stimulating lipid and carbohydrate metabolisms and an antioxidant agent for treating obesity: The invention relates to a combination comprising a compound favouring lipid and carbohydrate metabolisms and an antioxidant agent and to pharmaceutical compositioins comprising the combination....

20060111408 - Therapeutic benzothiazole compounds: e

20060111409 - Medicament for treatment of diabetes: wherein X represents a connecting group whose number of atoms in the main chain is 2 to 5 (said connecting group may be substituted), A represents hydrogen atom or acetyl group, E represents an aryl group which may be substituted or a hetero aryl group which may be substituted, ring...

20060111410 - Microbicide substances: The invention relates to antimicrobial, synergistically active mixtures of 1,2-benzisothiazolinone (BIT) and tetramethylolacetylenediurea (TMAD)....

20060111411 - Substituted 5-carboxyamide pyrazoles and [1,2,4]triazoles as antiviral agents: The present invention provides compounds of formula I wherein X, Y, R1-R7 are as defined herein. Compositions containing these compounds, and methods for inhibiting HCV RNA-dependent RNA polymerase and treating hepatitis C and related disorders using these compounds and compositions are also provided....

20060111412 - Substituted 5-oxo pyrazoles and [1,2,4]triazoles as antiviral agents: The present invention provides compounds of formula I wherein X and R1-R7 are as defined herein. Compositions containing these compounds, and methods for inhibiting HCV RNA-dependent RNA polymerase and treating hepatitis C and related disorders using these compounds and compositions are also provided....

20060111414 - 2-amino-1-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors: e

20060111413 - 2-amino-3-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors:

20060111415 - 2-aminonaphthalene derivatives and related glycogen phosphorylase inhibitors:

20060111417 - Amorphous telmisartan: Amorphous telmisartan and combinations of amorphous telmisartan with one or more pharmaceutical carriers....

20060111416 - Octahydropyrrolo[3,4-c]pyrrole derivatives: o

20060111418 - Blood-brain barrier disruption inhibitor: 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...

20060111421 - Method of treating or preventing myocardial ischemia-reperfusion injury using nf-kb inhibitors: The present invention concerns a method of treatment or prevention of myocardial ischemia-reperfusion injury by diagnosing that a person is in need of treatment or prevention of myocardial ischemia-reperfusion injury and administering a therapeutically effective amount of a ligand which modulates NF-kB transcription factor by interaction with estrogen receptor ER-α,...

20060111419 - Novel fused indazole compounds: represents a double bond or a single bond; R1a represents a hydrogen atom, etc.; the ring A represents a benzene ring, a naphthalene ring or a 5- to 10-membered aromatic heterocyclic ring, etc.; and R2a, R2b and R2c each independently represent (1) a hydrogen atom, (2) a halogen atom, (3)...

20060111422 - Novel pyrazole-based hmg coa reductase inhibitors: Novel compounds and pharmaceutical compositions useful as hypocholesterolemic and hypolipidemic agents are described. More specifically, potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (“HMG CoA reductase”) are described. Methods of using such compounds and compositions to treat subjects, including humans, suffering from hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, Alzheimer's Disease, benign prostatic...

20060111420 - Sorbicillactone-a derivatives for the treatment of tumour and viral diseases: v

20060111423 - Use of diindolylmethane-related indoles and growth factor receptor inhibitors for the treatment of human cytomegalovirus-associated disease: The present invention includes compositions and methods for the treatment and prevention of conditions associated with Human Cytomegalovirus (HCMV) infection. HCMV-associated conditions include infections (active and latent), benign cell-proliferative conditions, pre-cancerous cell-proliferative conditions, and cancerous conditions. In particular, the present invention describes new therapeutic and preventative uses for 3,3′-diindolylmethane (DIM),...

20060111424 - Fused cyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function: Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds....

20060111425 - Azabicyclo derivatives as muscarinic receptor antagonists: This invention generally relates to muscarinic receptor antagonists which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. Specifically, the invention relates to derivatives of azabicyclo compounds, including, for example, 6-substituted azabicyclo[3.1.0] hexanes, and 2,4,6-trisubstituted derivatives. The...

20060111427 - Indole derivatives useful as progesterone receptor modulators: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment or prevention of disorders and diseases mediated by agonists and antagonists of the progesterone receptor. The clinical uses of these compounds are related to contraception, the treatment and/or prevention of secondary...

20060111426 - Indole-3-sulphur derivaties: The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders. (I)...

20060111428 - Combination of an dpp-iv inhibitor and a ppar-alpha compound: The invention relates to a combination which comprises a DPP-IV inhibitor and at least one further PPARα compound, preferably selected from the group consisting of fenofibrate, micronized fenofibrate, bezafibrate, gemfibrazil and ciprofibrate for simultaneous, separate or sequential use in the prevention, delay of progression or treatment of conditions mediated by...

20060111429 - Novel compounds: het is a non-aromatic 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6-membered carbocyclic group or a second 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, wherein the het group...

20060111430 - 2,3,4-substituted cyclopentanones as therapeutic agents: t

20060111431 - Thiophene carboxanmides as inhibitors of the enzyme ikk-2: The invention relates to thiophene carboxamides of formula (I) wherein Ar, R1, R2, R3, R4, R5, m and n are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy....

20060111432 - Paclitaxel aqueous injection solution and methods for preparing the same: The present invention provides an injectable pharmaceutical composition containing, as an active ingredient, paclitaxel, an anti-cancer agent. The injectable pharmaceutical composition comprises an effective amount of paclitaxel, which is dissolved in polyoxyethylated castor oil, alcohol, and an injectable aqueous solution. A sufficient amount of CO2 is added to stabilize paclitaxel...

20060111433 - Use of angelicin and of its structural analogues for the treatment of thalassemia: The use of angelicin and its structural analogues for the preparation of a medicament for the therapeutic treatment of beta-thalassaemia is described. A structural analogue which is particularly preferred for this purpose is bergapten....

20060111435 - Compositions for treating or preventing obesity and insulin resistance disorders: Provided herein are methods and compositions for modulating the activity or level of a sirtuin, thereby treating or preventing obesity or an insulin resistance disorder, such as diabetes in a subject. Exemplary methods comprise contacting a cell with a sirtuin activating compound or an inhibitory compound to thereby increase or...

20060111434 - Method for preparing derivatives of fungicidal iodochromones: This invention relates to new methods for preparing chemical compounds, in particular fungicidal compounds, especially iodinated derivatives of chromones, preferably compounds of formula (I), and intermediate compounds useful for these methods....

20060111436 - Compositions and treatments for modulating kinase and/or hmg-coa reductase: The present invention provides compositions of matter, kits and methods for their use in the treatment of kinase-related conditions and/or HMG-CoA reductase-related conditions. In particular, the invention provides compositions for treating immuno-compromised and/or cardiovascular conditions in an animal subject by modulating one or more MAP kinase(s) and/or HMG-CoA reductase, as...

20060111437 - Hyperlipemia therapeutic agent: The present invention relates to a hyperlipemia therapeutic agent comprising pitavastatins and eicosapentaenoic acid or an ester derivative thereof as effective ingredients. According to the present invention, a type IIb and type IV hyperlipemia therapeutic agent having an excellent effect of lowering the cholesterol and triglyceride in blood is provided....

20060111438 - Asymmetric synthesis of substituted dihydrobenzofurans: e

20060111439 - Acyloxyalkyl carbamate prodrugs of sulfinic acids, methods of synthesis, and use: Acyloxyalkyl carbamate prodrugs of 3-aminopropylsulfinic acid and analogs thereof, pharmaceutical compositions of 3-aminopropylsulfinic acid and analogs thereof, methods of making prodrugs of 3-aminopropylsulfinic acid and analogs thereof, methods of using prodrugs of 3-aminopropylsulfinic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing diseases or disorders such as...

20060111440 - Cathepsin cysteine protease inhibitors: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis....

20060111441 - Treating wasting disorders with selective androgen receptor modulators: This invention provides: 1) a method of treating a subject suffering from a muscle wasting disorder; 2) a method of preventing a muscle wasting disorder in a subject; 3) a method of treating, preventing, suppressing, inhibiting or reducing muscle loss in a subject suffering from a muscle wasting disorder; 4)...

20060111442 - Use of methyl pyruvate to increase cellular energy production downstream of glycolysis for the parp-1 ablation of hiv without necrotic cell death caused by continuous, chronic parp-1 activation through the concomitant depletion of atp and nad.: The present invention relates to the use of methyl pyruvic acid (a methyl ester of pyruvic acid) and/or methyl pyruvate (methyl pyruvate is the ionized form of methyl pyruvic acid) for the purpose of increasing cellular energy production thereby providing energy for the continuous activation of PARP-1 and up-regulation of...

20060111443 - Preventive therapeutic composition for muscular fatigue, pulled muscle and disease attributed thereto: The present invention provides a composition for the inhibition of and promotion of recovery from muscular fatigue or muscular damage and diseases associated therewith, in particular, muscular fatigue or muscular damage caused by exercise stress and diseases associated therewith, and a composition for the prevention or treatment of myofibrosis during...

20060111444 - Novel halogen-substituted aminodicarboxylic acid derivatives: e

20060111445 - Novel carboxylic acids and derivatives for the treatment of and preventing diabetes and dyslipidaemia: The present invention relates to a compound of the formula ((I): in which: n is an integer chosen from 1, 2 and 3; Y represents O; N—OR9, in which R9 represents H or a saturated hydrocarbon-based aliphatic group; CR10R11, in which R10 and R11, which may be identical or different,...

20060111446 - 5-amidino-n-(2-aminophenethyl)-2-hydroxybenzenesulfonamide derivative, medicinal composition containing the same, pharmaceutical use thereof, and intermediate therefor: R3 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom or a hydroxy group, etc., or a pharmaceutically acceptable salt thereof, which exerts a potent and selective activated...

20060111447 - Inhibiting progressive cognitive impairment: The present invention provides compositions and methods for inhibiting progressive cognitive impairment in persons at risk of developing dementia, for example patients suffering from MCI. It is based, at least in part, on the discovery that nimesulide, at extremely low concentrations, has a number of anti-amyloid effects, including decreasing the...

20060111448 - Methods for treating cognitive impairment in humans with multiple sclerosis: Cognitive impairments in humans with multiple sclerosis are treated and cognition is improved with an amphetamine compound. In one embodiment, the method includes administering an l-amphetamine compound. In another embodiment, the method includes administering an l-methamphetamine compound....

20060111449 - Use of long-chain alcohols for effectively lowering elevated cholesterol levels: The invention relates to the use of long-chain alcohols for effectively lowering elevated cholesterol levels, wherein the long-chain alcohols are obtained from montan wax alcohols and Guerbet alcohols and their beeswax analogs....

20060111450 - Compositions and methods for treating alzheimer's disease and related disorders and promoting a healthy nervous system: The present invention relates generally to methods of inhibiting the onset and progression of Alzheimer's disease (AD), mild cognitive impairment (MCI), and related neurodegenerative disorders involving amyloidosis. The methods involve administering a composition comprising a therapeutically effective amount of D-pinitol to individuals who are at risk of developing the disease...

20060111451 - 1-chloro-2,4-dinitrobenzene gel compositions and methods for using the same: Gel compositions that contain 1-dichloro-2,4-dinitrobenzene (DNCB) are provided. Embodiments of the subject gel compositions include DNCB, an organic solvent and a viscosity agent, wherein the organic solvent and viscosity agent are inert with respect to the DNCB. Also provided are methods for using the subject compositions and kits for use...

20060105938 - Method of treating or preventing obeisity and lipid metabolism disorders and compositions for use therein: The present invention provides a method of preventing or treating human obesity, said method comprising ingesting a composition containing, calculated on dry matter: 10-100 wt. % protein hydrolysate; 0-90 wt. % intact protein; 0-50 wt. % carbohydrate; and wherein hydrolysed protein and intact protein together are present in a concentration...

20060105939 - Treatment of autism and similar disorders: Methods of treating certain behavioral characteristics associated with autism are provided. Additionally, methods of treating disorders associated with repetitive behaviors, social deficits and/or cognitive deficits are also provided. A therapeutic amount of oxytocin or oxytocin analogs, either alone or in combination, are administered to individuals demonstrating behavioral characteristics associated with...

20060105940 - Compound useful in the treatment or prevention of cognitive disorders associated with diabetes and associated methods: Described is the efficient synthesis of an easy to manipulate and utilize, soluble tartrate salt of a potent, reversible butyrylcholinesterase inhibitor, (−)-(3aS)-3a-methyl-1,2,3,3a,8,8a-hexahydropyrrolo-[2,3-b]indol-5-yl N—4′-isopropylphenylcarbamate (“MHI tartrate”), for use in altering the enzymatic activity of butyrylcholinesterase and/or acetylcholinesterase in a subject exhibiting or predicted to exhibit cognitive disorders associated with diabetes. Subjects...

20060105941 - Mixed antibiotic codrugs: Novel compounds which degrade in vivo into two or more different active antibiotics are disclosed herein. Methods, compositions, and medicaments related thereto are also disclosed....

20060105943 - Cyclic peptidomimetic urokinase receptor antagonists: The present invention relates to cyclic peptides as inhibitors of urokinase binding to the urokinase receptor. Said cyclic peptides are suitable as pharmaceutical active substances for disorders mediated by urokinase and its receptor....

20060105942 - Inhibition of cell division based use of analogs of neuropeptide y: We describe peptides with cell-cycle inhibitory and anti-angiogenic activity and their use in the treatment of diseases which would benefit from the inhibition of cell division and/or angiogenesis, for example cancer....

20060105944 - Methods for the therapeutic use of cyclosporine components: Methods of treating humans or animals having various conditions are disclosed which include administering a cyclosporine component. Among the conditions treated are dry mouth syndrome, verruciform xanthoma, achlorhydria, mucous cysts, oral submucous fibrosis, oral nevi, cancer of the oral mucosa, maloplakia of the genito-urinary tract, vulvovaginitis, helicobacter plylori infection, duodenal...

20060105945 - Therapeutic methods using cyclosporine components: Methods of treating humans or animals having various conditions are disclosed which include administering a cyclosporine component. Among the conditions treated are dry mouth syndrome, verruciform xanthoma, achlorhydria, mucous cysts, oral submucous fibrosis, oral nevi, cancer of the oral mucosa, maloplakia of the genito-urinary tract, vulvovaginitis, helicobacter plylori infection, duodenal...

20060105948 - Glp-2 derivatives: The present invention relates to novel derivatives of human glucagon-like peptide-2 (GLP-2) peptides, which have a protracted profile of action, as well as pharmaceutical compositions, uses and methods of treatment....

20060105954 - Glucagon-like peptide-2 and its therapeutic use: Glucagon-like peptide 2, a product of glucagon gene expression, and analogs of glucagon-like peptide 2, have been identified as gastrointestinal tissue growth factors. Their effects on the growth of small bowel and pancreatic islets are described. Their formulation as a pharmaceutical, and their therapeutic use in treating disorders of the...

20060105951 - Melanocortin receptor binding mimetibodies, compositions, methods and uses: Melanocortin receptor binding mimetibody polypeptides are disclosed. Polynucleotides encoding these polypeptides, cells comprising these polynucleotides or expressing the mimetibodies, and methods of making and using the forgoing are also disclosed....

20060105946 - Method for treating the central nervous system by administration of igf structural analogs: This invention is directed to a method for treating a disease or disorder of the brain or spinal cord in a mammal, including human, comprising the administration of an effective amount of an insulin-like growth factor (IGF) structural analog at a site outside of the blood-brain, blood-central nervous system, or...

20060105952 - Modified annexin proteins and methods for their use in organ transplantation: Modified annexin proteins, including a homodimer of human annexin V, are provided. Methods for their use, such as to prevent thrombosis without increasing hemorrhage and to attenuate ischemia-reperfusion injury (IPI), are also provided. The modified annexins bind phosphatidylserine (PS) on cell surfaces, thereby preventing the assembly of the prothromkinase complex....

20060105950 - Morphogen compositions and use thereof to treat wounds: Disclosed are compositions and methods for promoting or accelerating wound healing and preventing, treating, or reducing symptoms associated with wounds or wounding disorders such as diabetic ulcers and burns. In one embodiment, the method includes administering a therapeutically effective amount of a nucleic acid encoding at least one morphogen, or...

20060105947 - Novel chimeric analgesic peptides: The present invention provides a novel chimeric peptide containing an opioid peptide moiety and a nociceptive peptide moiety for producing analgesia...

20060105949 - Pharmaceutical preparations and methods for inhibiting tumors: The invention provides pharmaceutical compositions and method for inhibiting growth of prostatic adenocarcinoma, stomach cancer, breast cancer, endometrial, ovarian or other cancers of epithelial secretion, or benign prostate hyperplasia (BPH) In one embodiment the pharmaceutical composition includes human rHuPSP94, antigenic portions thereof, and functionally equivalent polypeptides thereof. In another embodiment,...

20060105953 - System for protease mediated protein expression: The present invention provides methods and materials that can be used to detect, examine and exploit protease mediated protein expression. An illustrative embodiment of the invention is a polynucleotide encoding a polypeptide having a plurality of operatively linked elements comprising a polypeptide degradation signal that functions as a proteosome substrate;...

20060105955 - Topical drug delivery using phosphatidylcholine: The present invention relates to compositions and methods for transdermal drug delivery comprising formulating a phosphatidylcholine carrier composition containing the drug and applying the composition to the skin....

20060105956 - Phenotypic reversion of pancreatic carcinoma cells: The present invention provides peptides (including analogs and derivatives thereof) corresponding to residues 96-110 and 35-47 of ras-p21, which peptides have attached thereto a membrane-penetrating leader sequence. The subject peptides, analogs and derivatives thereof are useful in treatment of cancers and have been shown to induce phenotypic reversion of pancreatic...

20060105957 - Loop peptide and tgfalpha for stimulating stem cell proliferation and migration: There is disclosed a novel genus of small peptides, much smaller than human TGFα, was discovered as having TGFα biological activity and therefore are useful as pharmacologic agents for the same indications as full length TGFα polypeptide. There is further disclosed that TGFα and consequently the genus of small peptides...

20060105958 - Pheromones and the luteinizing hormone for inducing proliferation of neural stem cells and neurogenesis: The present invention provides a method of increasing neural stem cell numbers or neurogenesis by using a pheromone, a luteinizing hormone (LH) and/or a human chorionic gonadotrophin (hCG). The method can be practiced in vivo to obtain more neural stem cells in situ, which can in turn produce more neurons...

20060105959 - Organic compounds with biological action as thrombin inhibitors and use thereof: The invention relates to biologically active molecules, which interact with thrombin and inhibit the same. The invention particularly relates to molecules of general fomula (I): Y1—(NH—X1—C═O)—(NH—X2—C═O)—(NH—X3—C═O)—(NH—X4—C═O)—(NH—X6—C═O) (NH—X6—C═O)—Y2, wherein Y1, Y2 and X1-6 have the meanings given in the description and N- or C-terminal abbreviated variations of said compounds and the...

20060105960 - New selenohydroxy acids and their derivatives, applications in nutrition, cosmetics and pharmaceutics: e

20060105965 - Method for enhancing energy levels and reducing the effects of stress using nutraceutical formulations: The present invention provides compositions and methods related to enhancing energy levels in an individual. The invention also provides methods for reducing the effects of stress in an individual. Certain embodiments of this invention include a composition comprising niacin bound chromium, D-ribose, a withanolide and an amine selected from the...

20060105961 - Method of using a cox-2 inhibitor and a topoisomerase ii inhibitor as a combination therapy in the treatment of neoplasia: The present invention provides compositions and methods to treat, prevent or inhibit a neoplasia or a neoplasia-related disorder in a mammal using a combination of a COX-2 inhibitor and a topoisomerase II inhibitor....

20060105966 - Novel anticonvulsant derivative salts: The invention relates to novel pharmaceutically acceptable salts of anticonvulsant derivatives, processes for preparation of and pharmaceutical compositions containing said salts, useful in the treatment of epilepsy....

20060105964 - Piperazine derivatives useful as ccr5 antagonists: R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists...

20060105963 - Therapeutic agents for inhibiting and/or treating vaginal infection: A vaginal treatment composition that employs a therapeutic agent to inhibit and/or treat vaginal infection is provided. The therapeutic agent is capable of inhibiting and/or killing Gardnerella (e.g., Gardnerella vaginalis), Candida (e.g., Candida albicans), and/or Trichomonas (e.g., Trichomonas vaginalis) pathogens. Desirably, such antimicrobial efficacy is achieved without substantially inhibiting the...

20060105962 - Tonic to maintain intestinal flora: An orally-administered pre-biotic composition for promoting the growth of normal, healthy intestinal flora while preventing the proliferation of unhealthy and toxic intestinal flora. When ingested, the composition improves the natural biological protection of the human body against toxic substances that are present in foods ingested and those that are produced...

20060105967 - Flavone derivatives as tnfalpha inhibitors or antagonists: in which R1, R2, R3, R4 and R5 independently represent hydrogen, hydroxy or an ester group; R6 represents hydrogen, hydroxy, an ester group or an O-glycoside group such as O-rhamnose, O-glucoside, O-retinoside or O-xyloside; and represents a single bond or a double bond; or the pharmaceutically acceptable salts thereof...

20060105969 - Anthelmintic compositions: Combinations of avermectins and milbemycins and their derivatives with bis-aryl compounds and their use in combating parasite, especially helminth, infections....

20060105970 - Avermectins substituted in the 4\"-position having pesticidal properties: with the proviso that R1 is not sec-butyl or isopropyl if R2 is H and R3 is 2-hydroxyethyl, isopropyl, n-octyl or benzyl;or, if appropriate, in E/Z isomer, an E/Z isomer mixture and/or a tautomer thereof; a process for preparing and using these compounds and their tautomers; pesticides whose active compound...

20060105968 - Compositions comprising highly purified amphotericin b: A method for treating fungal infections in a mammal that comprises administering a therapeutically effective amount of a composition comprising amphotericin B and a pharmaceutically acceptable carrier, wherein the amphotericin B is substantially pure....

20060105971 - Salts of avermectins substituted in the 4\"-position and having pesticidal properties: with the proviso that R1 is not sec-butyl or isopropyl when R2 is H and R3 is methyl; and, where applicable, their possible tautomers; a process for the preparation of those compounds and their tautomers and the use thereof; pesticidal compositions in which the active ingredient has been selected from...

20060105972 - Method to enhance delivery of glutathione and atp levels in cells: A therapeutic method is provided comprising treating a mammal subject to hypoxia with an amount of 2(R,S)-D-ribo-(1′,2′,3′,4′-tetrahydroxybutyl)thiazolidine-4(R)-carboxylic acid (RibCys) or a pharmaceutically acceptable salt thereof effective to both maintain, restore or increase both the ATP levels and the glutathione (GSH) levels in said tissue....

20060105973 - Antisense modulation of hydroxysteroid 11-beta dehydrogenase 1 expression: Antisense compounds, compositions and methods are provided for modulating the expression of hydroxysteroid 11-beta dehydrogenase 1. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding hydroxysteroid 11-beta dehydrogenase 1. Methods of using these compounds for modulation of hydroxysteroid 11-beta dehydrogenase 1 expression and for treatment of...

20060105980 - Aptamer therapeutics useful in the treatment of complement-related disorders: The invention provides nucleic acid therapeutics and methods for using these nucleic acid therapeutics in the treatment of complement-related disorders....

20060105975 - Aptamer-mediated intracellular delivery of therapeutic oligonucleotides: Materials and methods are provided to modulate, in a controlled manner, the intracellular deliver of therapeutic agents, including therapeutic oligonucleotides using nucleic acid aptamers....

20060105974 - Conjugates of photosensitizers and oligonucleotides for selective photochemiotherapy: This invention relates to oligonucleotide targeting agents and their use in the treatment of diseased cells by selective photochemotherapy (PCT). PCT is a method of treating human diseases and disorders, bacteriological indications and other pathological conditions. PCT is based on the topical or systemic application of a photosensitizing agent, a...

20060105983 - Cytotoxic agents: A method of killing a cell that is lacking in effective p53 protein activity, particularly as compared to wild type, is provided characterized in that it comprises delivering to the cell a single stranded DNA including a portion with at least one base, internally located with respect to any 3′...

20060105977 - Desmoglein 4 is a novel gene involved in hair growth: This invention provides methods and compositions for inhibiting the expression of desmoglein 4. This invention also provides pharmaceutical compositions for inhibiting hair growth in a subject....

20060105978 - Dose forms: The present invention relates to antiviral therapies and compositions for treating or preventing Hepatitis C infections in patients and relates to other methods disclosed herein. The invention also relates to kits and pharmaceutical packs comprising compositions and dosage forms. The invention also relates to processes for preparing these compositions, dosages,...

20060105982 - Non-invasive gene targeting to ocular cells: Liposomes containing therapeutic genes are conjugated to multiple targeting agents to provide transport of the encapsulated gene across the blood-retinal barrier and the plasma membrane of ocular cells. Once across the blood-retinal barrier and ocular cell membrane, the encapsulated gene expresses the encoded therapeutic agent within the ocular cells to...

20060105976 - Rnai modulation of apob and uses thereof: The invention relates to compositions and methods for modulating the expression of apolipoprotein B, and more particularly to the downregulation of apolipoprotein B by chemically modified oligonucleotides....

20060105979 - Synergistic inhibition of vegf and modulation of the immune response: The invention provides methods and compositions for treating asthma and allergy by inhibiting VEGF expression and modulating the immune system from a Th2 response to a Th1 response....

20060105981 - Therapeutic agents for treatment of solid tumors comprising an expression-inhibiting substance against wilms' tumor gene (wt1): The present invention relates to therapeutic agents for treatment of solid tumors comprising an expression-inhibiting substance (an antisense oligonucleotide derivative, a WT1 mutant gene, a WT1 mutant protein, a low molecular weight substance, and the like) against the Wilms' tumor gene (WTI)....

20060105984 - Chromium complex with insulin-like activity: A chromium complex for use in treating metabolic disorders, particularly Type 1 and Type 2 diabetes....

20060105985 - Treatment of mucositis: Disclosed are compositions and methods for alleviating mucositis, wherein said methods and compositions are directed to the formulation or use of selected nucleoside derivatives, especially ADP-ribose, that conform to the general formula A-B-X and pharmaceutically acceptable salts thereof, wherein “A” is a nucleoside structure selected from adenosine, guanosine, and uridine;...

20060105986 - Antimicrobial molecule: The present invention relates to a compound having antimicrobial activities. The present invention also provides methods for the production and purification of flocculosin, the antimicrobial compound of the invention, including the steps of cultivating the microorganism Pseudozyma flocculosa. Analogs and derivatives of flocculosin are described herein....

20060105990 - Antiadhesive carbohydrates: Provided is a pharmaceutical or dietetic product, which serves for reducing and/or blocking the adhesion of pathogenic substances and organisms to eucaryontic cells, in particular mammal cells. Said preparation contains at least one carbohydrate having an uronic acid unit on one of the ends thereof. 10 to 100% of the...

20060105988 - Antipruritic composition for external use on skin: It is the object of the present invention to provide a composition which has an antipruritic effect on skin and further exhibits good appearance and feeling of usage. The present invention relates to an antipruritic composition for external use on skin, which contains a mucopolysaccharide or a derivative thereof in...

20060105989 - Food for improving arthritis: The present invention provides a food for improving arthritis comprising proanthocyanidins (A) and a mucopolysaccharide and/or an amino sugar (B). Preferably, the proanthocyanidins contain at least 20 wt % of OPCs....

20060105991 - Medical composition for protuberance of epithelium: A medical composition for protuberance of epithelium, which comprises a solution comprising a polysaccharide or a medically acceptable salt thereof, wherein the solution has a viscosity of: (1) from 50 to 500 mPa·s at a shear rate of from 7.7 to 10.0 s−1; (2) from 45 to 300 mPa·s at...

20060105987 - Sulfur-containing phospholipid derivatives: The present invention provides a lipid compound comprising at least one non-polar moiety and a polar moiety, wherein each or at least one non-polar moiety is of the formula X—Y-Z-, wherein X is a hydrocarbyl chain, Y is selected from at least one of S, Se, SO2, SO, and O,...

20060105993 - Methods and compositions using immunomodulatory compounds for treatment and management of cancers and other diseases: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or...

20060105992 - Pharmaceutical formulations of cyclodextrins and selective estrogen receptor modulator compounds: This invention relates to compositions that contain cyclodextrin derivatives and selective estrogen receptor modulators and methods for the production of the compositions of the invention. The invention further relates of methods of administering the compositions of the present invention to a human or animal....

20060105994 - Treatment of prostate cancer: A chemical agent of the diterpene family obtained from a member of the Euphorbiaceae family of plants for use in the treatment of prophylaxis of prostate cancer or a related cancer or condition....

20060105995 - Tafi inhibitors and their use to treat pulmonary fibrosis: The invention relates to TAFI inhibitors and their use to treat pulmonary fibrosis....

20060105996 - Inositolized phospholipids: The present invention relates to a phospholipid dreivative having a substituted or unsubstituted polyhydroxylated aliphatic carbocycle attached to the sn-1 or sn-2 position of the glycerol backbone, a pharmaceutical composition comprising said phospholipid, a method for preparing said phospholipid and a medicament comprising said phospholipid....

20060105997 - Mitotic kinesin inhibitors: The present invention relates to 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 in mammals....

20060105998 - Antiprotozoal ring-substiuted phospholipids: Disclosed are novel ring containing phospholipids represented by the structural formula A-X—PO3—W and physiologically acceptable salts thereof and a process for the preparation of these compounds. The compounds can be used for the treatment of protozoal diseases and especially leishmaniasis....

20060105999 - Novel inhibitors of beta-lactamase: The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel β-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic β-lactamase inhibitors presently available, and which do not require β-lactam pharmacophore. The invention also provides...

20060106001 - Novel phytic citrate compounds and process for preparing the same: wherein said R is H or citrate and wherein at least one R is citrate. The salt of the chemical compound is the Na+, K+, Mg2+, or Ca2+ salt of said chemical compound. The chemical compound is a chelator which chelates sodium, potassium or lithium, magnesium, calcium, copper, iron, lead,...

20060106000 - Use of inositol-tripyrophosphate in treating tumors and diseases: Inositol-tripyrophosphate is an allosteric effector of hemoglobin due to its ability to cross the plasma membrane of red blood cells and deliver oxygen to solid tumors, by lowering the oxygen affinity of the hemoglobin of red blood cells. The present invention is directed to the use of inositol-tripyrophosphate to reduce...

20060106002 - Therapeutic agent for steroid depending-and/or steroid resistant- ulcerative colitis: The present invention is directed to a pharmaceutical composition for the treatment of steroid depending and/or steroid resistive ulcerative colitis. The pharmaceutical composition, which is administered to treat steroid depending and/or steroid resistive ulcerative colitis, contains, as the active ingredients, at least one compound selected from a group consisting of...

20060106003 - Combination of a macrolide t-cell immunomodulator and a calciferol for the treatment of skin diseases or of inflammatory bowel disease: Synergistic combinations of a macrolide T-cell immunomodulator or immunosuppressant such as 33-epichloro-33-desoxyascomycin and a calciferol or tacalcitol are provided, which are useful in particular in the treatment of dermatological diseases such as atopic dermatitis, acen and psoriasis or of inflammatory bowel disease (IBD)....

20060106004 - Unique methods and formulations of bio-identical sex steroids for the treatment of pathophysiologic aberrations of menopause: Consistent relief of physical and psychological disturbances in menopause is achieved by the administration of estrogenic hormones, which are bio-identical to natural estradiol and estriol, in a ratio ranging from 1.1:1.0 to 10.0:1.0, either with or without the combined administration of testosterone in a ratio of total estrogen to testosterone...

20060106005 - Funtionalised metallocenes as anticancer drugs: wherein R1, R2, R3 and R4 represent a combination of H, alkyl, aryl or trimethylsilyl; L represents side chain substituents, at least one of which contains a group which enables the compound to become water-solubilised; X is halo, alkoxy, acetate or H2O; Y is a counter-ion; M is a metal;...

20060106006 - Vanadium compounds for treating cancer: The invention provides methods for treating cancer and compounds that are useful for the treatment of tumors, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates useful for preparing the compounds....

20060106007 - Hiv integrase inhibitors: cyclic pyrimidinone compounds: The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses intermediates useful for making the pyrimidone compounds. Additionally, pharmaceutical compositions and methods for treating...

20060106008 - Pharmaceutical use of fused 1,2,4-triazoles: The use of fused 1,2,4-triazoles for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions has been described. Also a novel class of fused 1,2,4-triazoles, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the...

20060106009 - Use of caboxamides for the treatment of tinnitus: The present invention relates to the use of carbarnazepine derivatives in treating tinnitus....

20060106010 - Methods for inhibiting bone loss: The current invention provides methods and pharmaceutical formulations that are useful for inhibiting the loss of bone. These methods and formulations can be used without the associated adverse effects of estrogen therapy, and thus serve as an effective and acceptable treatment for osteoporosis....

20060106011 - 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....

20060106012 - Benzoxazine and quinoxaline derivatives and uses thereof: m

20060106014 - Methods for treating diabetes: Disclosed are methods for the treatment of diabetes by administering a composition comprising a pharmaceutically acceptable amount of a dual inhibitor of both 5-lipoxygenase (5-LO) and 12/15-lipoxygenase (12/15-LO) enzymes or of both 5-lipoxygenase (5-LO) and 15-lipoxygenase (15-LO) enzymes. The invention is also directed to methods of controlling blood glucose level...

20060106013 - Pi3-kinases: s

20060106015 - Novel use of benzothiazole derivatives: The use of compounds of formula (I) wherein X, A, B, D, R1 and R2 are as defined in the Specification and pharmaceutically acceptable salts thereof in the manufacture of a medicament for the treatment or prophylaxis of diseases or conditions in which inhibition of kinase Itk activity is beneficial...

20060106016 - Dicarboxamide derivatives: e

20060106017 - Novel o-acyloxime derivatives, preparation method thereof, and pharmaceutical composition containing the same for prevention and treatment of cardiovascular disease: The present invention relates to novel O-acyloxime derivatives, a preparation method thereof and a pharmaceutical composition comprising the same for prevention and treatment of cardiovascular disease. The O-acyloxime derivatives according to the present invention may valuably be used for prevention and treatment of cardiovascular diseases such as hyperlipidemia, coronary arterial...

20060106018 - Acetylenic compounds useful in treating inflammatory disorders: This invention is directed to acetylenic compounds as inhibitors of a nicotinamide adenine dinucleotide oxidase hydride donor useful in treating or ameliorating a reactive oxygen species mediated inflammatory disorder....

20060106019 - Novel substituted pyrazolo[1,5 a]-1,3,5-triazine derivatives and their analogues, pharmaceutical compositions containing same, use thereof as medicine and methods for preparing same: The invention concerns novel substituted pyrazolo[1,5 A]-1,3,5-triazine derivatives and some of their structural analogues, and their therapeutic uses, more particularly for preventing and treating pathologies involving central and/or peripheral neuronal degeneration. The invention also concerns methods for preparing same and novel synthesis intermediates. The compounds of the invention correspond more...

20060106020 - Tetracyclic inhibitors of janus kinases: The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer....

20060106022 - Imidazo[4,5-b]pyrazinone inhibitors of protein kinases: e

20060106021 - New antitumoral derivatives of et-743: Derivatives of Et-743 or Et-770 or Et-729 are provided. The derivatives are of the general formula (Ia) wherein the substituent groups take various permitted meanings....

20060106023 - Novel imidazopyrazines as cyclin dependent kinase inhibitors: In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyrazine 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,...

20060106024 - Microbicidal composition: A microbicidal composition containing: (a) 1,2-benzisothiazolin-3-one; and (b) at least one microbicide selected from among benzalkonium chloride, benzethonium chloride, benzyl alcohol, caprylyl glycol, chlorphenesin, 2,2′-dithiobis(N-methylbenzamide), diazolidinyl urea, ethylenediamine tetraacetic acid, ethylparaben, imidazolidinyl urea, methylparaben, phenoxyethanol, linoleamidopropyl PG-dimonium chloride phosphate, cocamidopropyl PG-dimonium chloride phosphate, propylparaben, cis-1-(3-chloroallyl)-3,5,7-triaza-1-azoniaadamantane chloride, dehydroacetic acid or its...

20060106025 - Dna-pk inhibitors: m

20060106026 - 4-(4-methylpiperazin-1-ylmethyl)-n-[4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide for treating anaplastic thyroid cancer:

20060106027 - Phenyl-[4-(3-phenyl-1h-pyrazol-4-yl)-pyrimidin-2-yi)-amine derivatives: The invention relates to phenyl-[4-(3-phenyl-1H-pyrazol-4-yl)-pyrimidin-2-yl]-amine derivatives and to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives—alone or in combination with one or more other pharmaceutically active compounds—for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease,...

20060106028 - Polycyclic aromatics and derivatives thereof and processes for their preparation: This invention relates to novel biologically active polycyclic aromatics produced by cultivation of Micromonospora echinospora ssp. challisensis NRRL 12255. The invention also relates to their pharmaceutically acceptable salts, prodrugs and derivatives, and to methods of obtaining them by post-biosynthesis chemical modification. The invention further relates to the use of the...

20060106029 - Novel aminopyridine derivatives having aurora a selective inhibitory action: wherein m1 and m2 are 1, 2, or 3; n1 and n2 are 0 or 1; i is an integer of any of 1 to m1; j is an integer of 1 to m2; R is aryl, heteroaryl, or cycloalkyl any of which may be substituted; Rai and Rai′ is...

20060106030 - Structurally rigid dopamine d3 receptor selective ligands and process for making them: A family of structurally rigid dopamine D3 receptor selective ligands is described. The family of structurally rigid dopamine D3 receptor selective ligands has the formula wherein A is cis or trans —CH═CH—, —C═C—, or cyclohexyl. B is cis or trans —CH═CH— or absent. R1 represents an optionally substituted phenyl group,...

20060106031 - Novel heterocyclyls as selective melanin concentrating hormone receptor antagonists for the treatment of obesity and related disorders: wherein m, n, p, R1, R2 and X, are herein defined, said compounds being novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity,...

20060106032 - Synthesis of n2 - (substituted arylmethyl) -3- (substituted phenyl) indazoles as novel anti-angiogenic agents: Novel compounds of 2-(substituted arylmethyl)-3-(substituted phenyl)-2H-indazoles and 1-(substituted arylmethyl)-3-(substituted phenyl)-1H-indazoles are synthesized, and useful as anti-angiogenic agents....

20060106033 - Pyrazolopyridines 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:...

20060106034 - Drug efflux pump inhibitor: wherein, R1 and R2 represent hydrogen atom, a halogen atom, hydroxyl group or the like, W1 represents —CH═CH—, —CH2O—, —CH2CH2— or the like; R3 represents hydrogen atom, a halogen atom, hydroxyl group or an amino group; R4 represents hydrogen atom, a group of —OZ0-4R5 (Z0-4 represents an alkylene group, a...

20060106035 - Phenyl-substituted pyrazolopyrimidines: The invention relates to novel phenyl-substituted pyrazolopyrimidines, process for their preparation, and their use for producing medicaments for improving perception, concentration, learning and/or memory....

20060106036 - Tumorigenesis inhibitor: A compound having a xanthine oxidase inhibitory activity, such as 1-(3-cyano-4-neopentyloxyphenyl)pyrazole-4-carboxylic acid and the like, can be a drug for preventing cancer including colon cancer and the like, as an agent for suppressing tumorigenesis....

20060106037 - Purin-6-one-derivatives: The compounds of a certain formula (I) in which e.g. R2, R3, R4 and R5 have the meanings as given below are novel effective PDE2 inhibitors. R2 is hydrogen, 1-4C-alkyl, 1-hydroxy-2-4C-alkyl, 1-4C-alkylcarbonyl or 1-(acetyloxy)-2-4C-alkyl and R3 is Arylbutyl, Heteroarylbutyl, Arylpropyl, Heteroarylpropyl, Arylethyl or Heteroarylethyl; wherein Aryl is phenyl, naphthalenyl or...

20060106039 - Combinations: The present invention relates to a pharmaceutical composition, comprising (a) a phosphodiesterase 5 inhibitor or a pharmaceutically acceptable salt thereof and (b) at least one of the active ingredients selected from the group consisting of (i) an anti-diabetic agent; (ii) HMG-Co-A reductase inhibitors; (iii) an anti-hypertensive agent; and (iv) a...

20060106038 - Methods for treating and/or preventing aberrant proliferation of hematopoietic cells: The invention relates generally to methods for treating and/or preventing aberrant proliferation of hematopoietic cells. More particularly, the invention relates to methods for treating and/or preventing aberrant proliferation of hematopoietic cells comprising selectively inhibiting phosphoinositide 3-kinase delta (PI3Kδ) activity in hematopoietic cells. The methods may be used to treat any...

20060106040 - 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...

20060106041 - Synthesis of indole analogs of 1-benzyl-3-(5'-hydroxymethy 1-2' -furyl) indazole (yc-1) as anti-platelet agents: The present invention synthesizes a series of novel indole analogs of 1-benzyl-3-(5′-hydroxymethyl-2′-furyl)indazole (YC-1), and their anti-platelet activity....

20060106043 - Method for treating hiv infection through co-administration of tipranavir and etravirine: A method for treating HIV infection through co-administration of tipranavir and etravirine....

20060106044 - Methods for inhibiting the transmission of hiv using topically applied substituted 6-benzyl-4-oxopyrimidines: A method for inhibiting sexual transmission of HIV comprising topically applying to the skin or epithelial tissue of a human a composition comprising a non-nucleoside reverse transcriptase inhibitor (“NNRTI”) that is able to inhibit viral replication for periods exceeding 12, 24, or even 36 days, at concentrations below even 10...

20060106042 - Substituted heterocyclpyrmidines: m

20060106046 - Melanin-concentrating hormone receptor antagonists containing piperidine derivatives as the active ingredient: [wherein R1 is hydrogen, hydroxyl, lower alkyl, or the like; R2, R3a, R3b, R4a, R4b, R5a, R5b and R6 each stands for hydrogen, halogen, or the like; W1 and W2 each independently stands for —O—, —CH2—, or the like; Y1, Y2, Y3 and Y4 stand for —CH—, —CF—, —N—, or...

20060106045 - Spiroindolinepiperidine derivatives: Insecticidal, acaricidal, nematicidal or molluscicidal compounds of formula (I) wherein Y is a single bond, C═O, C═S or C═(O)q where q is 0, 1 or 2; and R1, R2, R3, R4, R8, R9 and R10 are as defined in the claims or salts or N-oxides thereof, processes for preparing them...

20060106047 - Trisubstituted thiophenes as progesterone receptor modulators: The present invention is directed to novel trisubstituted thiophene derivatives, pharmaceutical compositions containing them and their use in the treatment or prevention of disorders and diseases mediated by agonists and antagonists of the progesterone receptor. The clinical usage of these compounds are related to hormonal contraception, the treatment and/or prevention...

20060106048 - Furoisoquinoline derivative and use thereof: wherein A represents (1) a bond, (2) a group represented by the formula —CRa═CRb— (Ra and Rb each represent a hydrogen atom or C1-6 alkyl) and the like; R1 represents (1) cyano or (2) an optionally esterified or amidated carboxyl group; R2 represents (1) a hydrogen atom, (2) an optionally...

20060106049 - Histone deacetylase inhibitors and methods of use: Disclosed are methods of treating an acute myeloid leukemia patient of cytogenetic subgroups having increased histone deacetylase recruitment by administering a histone deacetylase inhibitor to the patient....

20060106050 - Thrombin receptor antagonists: R1, R2, R3, R9, R10 and R11 are as defined in the specification; are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds....

20060106051 - Imidazo-fused oxazolo[4,5-b]pyridine and imidazo-fused thiazolo[4,5-b]pyridine based tricyclic compounds and pharmaceutical compositions comprising same: ,

20060106052 - Method of using sulfonamide substituted imidazoquinolines: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain sulfonamide or sulfonamide functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases....

20060106053 - Antitumor benzoylsulfonamides: The present invention provides antitumor compounds of the formula (I); and antitumor methods....

20060106054 - Phosphodiesterase 10a inhibitors: e

20060106055 - Novel quinuclidine derivatives and medicinal compositions containing the same:

20060106056 - Novel quinuclidine derivatives and medicinal compositions containing the same:

20060106057 - Stabilization of quinapril using magnesium oxide: The present invention is directed to ACE inhibitor-containing compositions stabilized by the presence of magnesium oxide. Preferably, the ACE inhibitor, quinapril, is protected from certain forms of degradation when prepared in a pharmaceutical composition consisting essentially of magnesium oxide as the stabilizing agent. The presence of magnesium oxide also lends...

20060106058 - Chemical compounds: 3-carboxy quinoline derivatives, which are useful as YAK3 inhibitors are described herein. The described invention also includes methods of making such 3-carboxy quinoline derivatives as well as methods of using the same in the treatment of diseases mediated by inappropriate YAK3 activity....

20060106059 - Melanocortin receptor ligands: c

20060106060 - Methods for the treatment of synucleinopathies (lansbury): Methods are provided of treating synucleinopathies, such as Parkinson's Disease, Diffuse Lewy Body Disease and Multiple System Atrophy, comprising administering to a synucleinopathic subject a farnesyl transferase inhibitor compound....

20060106061 - Pgd2 receptor antagonists for the treatment of inflammatory diseases: t

20060106062 - Substituted 2-quinolyl-oxazoles useful as pde4 inhibitors: R7 and R8 and the nitrogen to which they are attached together form an optionally substituted ring; and the remaining variables are as defined in the specification. Also claimed are pharmaceutical compositions, the use of the compounds as PDE4 inhibitors, and combinations with other actives....

20060106066 - Benzyl substituted (piperidin-4-yl)aminobenzamido derivatives: The present invention is directed to N-benzyl substituted (piperidin-4-yl)aminobenzamido derivatives which are delta-opioid receptor modulators....

20060106064 - Butyrophenones and sigma-1 receptor antagonists protect against oxidative-stress: The present invention includes compositions and methods for the protection of one or more central nervous system cells from trauma, when administered before, during or after the trauma, wherein the composition includes an effective amount of a butyrophenone, e.g., a 1-linked phenyl butyrophenone that is electronegative along the butyl chain...

20060106065 - Methods of treating hepatitis virus infections with n-substituted-1,5-dideoxy-1,5-imino-d- glucuitol compounds in combination therapy: Provided are methods and compositions for treating hepatitis virus infections in mammals, especially humans. The methods comprise (1) administering N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds in combination with nucleoside antiviral agents, nucleotide antiviral agents, mixtures thereof, or immunomodulating/immunostimulating agents, or (2) administering N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds in combination with nucleoside antiviral agents, nucleotide antiviral agents, or...

20060106063 - Synthesis of n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms: Disclosed herein are methods for synthesizing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide. Also disclosed herein is the hemi-tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide and methods for obtaining the salt. Further disclosed are various crystalline forms of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide and its hemi-tartrate salt including various polymorphs and solvates....

20060106067 - Fused benzene derivative and use: s

20060106068 - Sigma receptor inhibitors:

20060106069 - Pyrrole inhibitors of erk protein kinase, synthesis thereof and intermediates thereto: The present invention relates to compounds useful of 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....

20060106070 - Novel pyridine-based metal chelators as antiviral agents: wherein A or B are independently —R6R7, or —CH(R8)CH(R9). R1 to R9 are various substituents selected to optimize the physicochemical and biological properties such as enzyme binding, tissue penetration, lipophilicity, toxicity, bioavailability, and pharmacokinetics. The compounds of the present invention are useful for inhibiting the activity of viral enzymes responsible...

20060106071 - Substituted amides: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis,...

20060106072 - Compounds having selective activity for retinoid x receptors, and means for modulation of processes mediated by retinoid x receptors: Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene,...

20060106073 - Process for the preparation of epothilone derivatives, new epothilone derivatives as well as new intermediate products for the process and the methods of preparing same: m

20060106075 - Benzothiazole derivatives having beta-2-adrenoreceptor agonist activity:

20060106074 - Er-b-selective ligands: The invention relates to novel compounds having the general formula: (1) wherein X is O or S which are useful as selective ER-β ligands in the treatment or prophylaxis of Alzheimer's disease, anxiety disorders, depressive disorders, osteoporosis, cardiovascular disease, rheumatoid arthritis or prostate cancer....

20060106076 - Compositions and methods for the non-invasive treatment of uterine fibroid cells: The proliferation of uterine fibroid leiomyoma cells is inhibited by certain Fibroid Cell Growth Inhibitor (FGI) agents. Pharmacological doses of FGI agents can be made high enough to not only inhibit proliferation, but to cause cell death. Non-invasive or minimally invasive, non-systemic delivery methods deliver the FGI agent to the...

20060106077 - Pin1-modulating compounds and methods of use thereof: The invention is directed to modulators, e.g., inhibitors, of Pin1 and Pin1-related proteins and the use of such modulators for treatment of Pin1 associated states, e.g., for the treatment of cancer....

20060106078 - Prostamide receptor antagonists: e

20060106079 - Method for preparing oltipraz: Provided is a method for preparing oltipraz. The method includes reacting methyl 2-methyl-3-(pyrazin-2-yl)-3oxopropionate with phosphorus pentasulfide in the presence of a mixed solvent of toluene and xylene, followed by recrystallization....

20060106080 - Crystal modification ii of 2-[2-(1-chloro-cyclopropyl)-3-(2-chlorophenyl)-2-hydroxy-propyl]-2,4-dihydro-3h-1,2,4-triazole-3-thions: o

20060106081 - Benzimidazole acetic acids exhibiting crth2 receptor antagonism and uses thereof: The invention relates to benzimidazole acetic acid compounds which function as antagonists of the Chemoattractant Receptor-homologous molecule expressed on T-Helper type 2 cells (CRTH2) receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to...

20060106083 - Aminoindazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them: Compounds which are indazole derivatives and pharmaceutically acceptable salts thereof, together with pharmaceutical compositions comprising them, as well as combinatorial libraries of indazole derivatives, as set forth in the specification, are disclosed; these compounds or compositions may be useful in the treatment of diseases caused by and/or associated with an...

20060106082 - Nitrooxyderivatives of cyclooxygenase-2 inhibitors: m

20060106084 - [(1h-indazol-3-yl)methyl]phenols and (hydroxyphenyl)(1h-indazol-3-yl)methanones:

20060106085 - Methods and compositions using pde4 modulators for treatment and management of central nervous system injury: Methods of treating, preventing and/or managing a central nervous system injury/damage and related syndromes are disclosed. Specific methods encompass the administration of a PDE4 modulator alone or in combination with a second active agent. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention...

20060106086 - Preparation of tegaserod and tegaserod maleate: Provided are processes for preparation of tegaserod and the maleate salt thereof....

20060106087 - Benzenesulfonate of 4-fluoro-2-cyanopyrrolidine derivative: A benzenesulfonate salt of (2S,4S)-2-cyano-4-fluoro-1-[(2-hydroxy-1,1-dimethyl)ethylamino]acetylpyrrolidine that has an excellent DPPIV inhibition activity as well as physical properties (e.g., stability) required for pharmaceutical preparations. The present invention allows easy obtaining of the compound in high-purity uniform crystal form with excellent solid-state stability....

20060106088 - 2,3,4-substituted cyclopentanones as therapeutic agents: b

20060106089 - Bissulfonamide compounds as agonists of galr1, compositions, and methods of use: Embodiments of the present invention provide bissulfonamide compounds that are agonists of GalR1. The present invention further provides compositions comprising bissulfonamide compounds that are agonists of GalR1, and methods of use of such compounds and compositions....

20060106090 - Cytotoxic agents comprising taxanes and their therapeutic use: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent...

20060106091 - Antigiardial agents and use thereof: The present invention provides a method of preventing or treating one or more of the following medical conditions, or treating symptoms of one or more of the following medical conditions: amebic infections, giardiasis, estrogen deficient states, osteoporosis, cardiovascular heart disease, high cholesterol levels, hyperlipidemia, cancer by administering to a subject...

20060106092 - Procyanidin b dimers for aromatase inhibition: Anti-aromatase procyanidin B suppresses estrogen production, thus preventing or treating estrogen-related diseases such as breast tumors, hormone-dependent tumors and hormone-related disorders....

20060106093 - Formulation and delivery method to enhance antioxidant potency of vitamin e: A formulation to deliver a full-spectrum of Vitamin E isomers for improved antioxidant capacity, bioavailability, dissolution and efficacy. The formulation includes dl-α-tocopheryl acetate or dl-α-tocopheryl succinate (synthetic Vitamin E), natural Vitamin E and mixed tocopherols, such as α-, β-, γ- and δ-tocopherol, as well as four isomers (α, β, γ...

20060106094 - Synthetic discodermolide analogs: f

20060106095 - Therapeutic agent for renal failure: The present invention relates to a therapeutic agent for renal failure comprising, as an active ingredient, a 4,8-inter-m-phenylene prostaglandin I2 derivative, and also relates to a method for treatment of renal failure using the same....

20060106096 - Azabicyclic carbamates and their use as alpha-7 nicotinic acetylcholine receptor agonists: The invention relates to novel benzothiophene-, benzofuran- and indole ureas and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory....

20060106097 - Metabolism-modulating agents and uses therefor: The present invention is directed to methods and agents for modulating adipogenesis. More particularly, the present invention relates to molecules that modulate the level or functional activity of inosine-5′ monophosphate dehydrogenase (IMPDH) and to their use in modulating the accumulation of lipids in adipocytes and/or the differentiation of preadipocytes to...

20060106098 - Andrographolide and its derivatives as tnf-alpha antagonists: Andrographolide and its derivatives represented by general formula (I) defined above are useful as TNFα (tumor necrosis factor alpha) antagonists or inhibitors which have inhibitory effect on the binding of TNFα to TNF-RI. Andrographolide exhibited inhibitor activity with IC50 values 60 μM on L929 cell proliferation/cytotoxicity assay without cell cytotoxicity....

20060106099 - Novel inhibitors of ubiquitin isopeptidases: A novel class of inhibitors of ubiquitin isopeptidases is disclosed that cause tumor cell death via molecular mechanisms independent of p53. Specifically, compounds containing an a,β-unsaturated ketone with a sterically accessible electrophilic β-carbon and related compounds are identified herein. Pharmaceutical compositions comprising the inhibitor compounds and methods of using the...

20060106100 - Cyclic palladium compounds having coordinated thereto bis (diphenylphosphine) ferrocene ligands which inhibit the activity of proteins and enzymes and treatment of diseases and disorders associated therewith: The invention relates to cyclopalladated compounds containing bis-diphenylphosphine-ferrocene ligands and their analogues which are active inhibitors of proteins and enzymes, for example, those of the serine peptidase, cysteine-protease, metalo-protease and endopeptidase families, involved in the development and metastases of malignant tumors, e.g. of the thyroid. An exemplary compound is shown...

20060106101 - New double salts of (-)-hydroxycitric acid and a process for preparing the same: This invention relates to new double salts of (−)-hydroxycitric acid with group II metals. Preferred double salts are calcium and magnesium double salts of hydroxycitric acid of the formula II. This invention also includes a process for the preparation of these double salts by the addition of one metal compound...

20060106102 - Napththalene derivatives which inhibit the cytokine or biological activity of microphage migration inhibitory factor (mif): Where Y, R1-R8 and R101-R108 are as defined in the specification. Compounds of formula (II) and methods of inhibiting the cytokine or biological activity of Macrophage Migrating Inhibitory Factor (MIF) comprising contacting MIF with a compound of formula (I) are provided. The invention also relates to methods of treating diseases...

20060106103 - Treating neurological disorders using selective antagonists of persistent sodium current: The present invention provides methods of treating neurological disorders in a mammal by administering to the mammal an effective amount of a selective persistent sodium channel antagonist that has at least 20-fold selectivity for persistent sodium current relative to transient sodium current....

20060106104 - Ophthalmic compositions and methods for treating eyes: Ophthalmic compositions including compatible solute components and/or polyanionic components are useful in treating eyes, for example, to relieve dry eye syndrome, to protect the eyes against hypertonic insult and/or the adverse effects of cationic species on the ocular surfaces of eyes and/or to facilitate recovery from eye surgery....

20060106105 - Process for making polymorphic form a of 4-[6-acetyl-3-[3-(4-acetyl-3-hydroxy-2-propylphenylthio)propoxy]-2-propylphenoxy] butyric acid: h

20060106106 - Beta-hydroxyphenylalkylamines and their use for treating glaucoma: β-hydroxyphenylalkylamines and their use for lowering and controlling ocular hypertension and treating glaucoma are disclosed....

20060106107 - L-tartrate salt of n-1-adamantyl-2-{3-[(2r)-2-({(2r)-2-hydroxy-2-[4-hydroxy-3-(hydroxymethyl)phenyl]ethyl}amino)propyl] phenyl}acetamide: This invention relates to the L-tartrate salt of N-1-Adamantyl-2-{3-[(2R)-2-({(2R)-2-hydroxy-2-[4-hydroxy-3-(hydroxymethyl)phenyl]ethyl}amino)propyl]phenyl}acetamide and its use as a medicament....

20060106108 - Method for scavenging radicals with urocanic acid, derivatives and analogues: The invention relates to antioxidants or radical scavengers and their reaction products. The invention provides compounds and compositions for use in methods for scavenging radicals or for modulating the immune response comprising urocanic acid or salts, derivatives, functional equivalents and analogues thereof....

20060106109 - Short term treatment for uterine disorder: This invention is directed to a method and device for treating a female patient's uterine disorder by occluding one or both of the patient's uterine artery. The treatment embodying features of the invention basically involves occluding one or both of the patient's uterine arteries with an intravaginal device to form...

20060106110 - Modified amino acid for the inhibition of platelet aggregation: A method of inhibiting blood platelet aggregation in a mammal is provided. The method comprises the administration of a platelet aggregation inhibiting amount of a modified amino acid or pharmaceutically acceptable salt thereof....

20060106111 - Phenylnaphthalene compounds: m

20060106112 - Treating neurological disorders using selective antagonists of persistent sodium current: The present invention provides methods of treating neurological disorders in a mammal by administering to the mammal an effective amount of a selective persistent sodium channel antagonist that has at least 20-fold selectivity for persistent sodium current relative to transient sodium current....

20060106113 - Method of delaying ejaculation: The invention provides a method of delaying ejaculation. The method comprises administering an effective amount of a tramadol material to a human male prior to sexual intercourse. The method is particularly useful for treating premature ejaculation....

20060106114 - Tertiary amino compounds having opioid receptor affinity: e

20060106116 - Composition for lessening oxidative stress: A method for lessening oxidative stress in vivo in a subject in need thereof, comprising administering to said subject a composition containing a reduced coenzyme Q and an oxidized coenzyme of Q....

20060106115 - Osteogenesis promoter containing beta-cryptoxanthin as the active ingredient: It is intended to provide an osteogenesis promoter having a remarkable effect of positively promoting osteogenesis and thus preventing/treating bone diseases; a preventive/a remedy for bone diseases such as osteoporosis having both of an osteogenesis-promoting effect and a bone resorption-inhibiting effect; and a method of screening an active ingredient for...

20060106117 - Compound and method for prevention and/or treatment of vaginal infections: The invention provides a method for treating and/or preventing vaginal infections, such as bacterial vaginosis, by administering xylitol to a subject in need of treatment. A composition containing xylitol for treating vaginal infections is also disclosed. It has been found that xylitol is capable of selectively inhibiting the growth of...

20060100130 - Catalysis of the cis/trans-isomerisation of secondary amide peptide compounds: The present invention is based on the finding that the cis/trans isomerisation of secondary amide peptide bonds in oligo- and polypeptides can be catalytically promoted. This catalysis is effected by enzymes which are hereinafter called “secondary amide peptide bond cis/trans isomerases (APIases). It can be assumed that the APIase activity...

20060100135 - Compositions and methods for modifying toxic effects of proteinaceous compounds: The present invention provides methods to produce immunotoxins (ITs) and cytokines with a reduced ability to promote vascular leak syndrome (VLS). The invention also provides ITs and cytokines which have been mutated to lack amino acid sequences which induce VLS....

20060100133 - High beta-conglycinin products and their use: The utility of soybeans having a composition of greater than 40% of the protein as beta-conglycinin and less than 10% of the protein as glycinin for making highly functional high beta-conglycinin compositions was discovered. The discovered ingredients are useful for mimicking the texturizing properties of casein while also maintaining or...

20060100134 - Membrane penetrating peptides and uses thereof: The present invention is directed to membrane penetrating peptides useful as in viv, ex vivo and in vitro intracellular delivery devices for compound of interest. More particularly, the invention involves identification of membrane penetrating peptides which may be used as protein carriers for delivery of a compound of interest to...

20060100132 - Method for diagnosing inflammatory bowel disease: The present invention relates to a method for identifying a compound capable of modulating the action of the DLG5 protein which method comprises subjecting one or more test compounds to a screen comprising a polypeptide containing the amino acid sequence shown in SEQ ID NO: 2, or a homologue thereof...

20060100131 - Modulation of stem cell differentiation by modulation of caspase-3 activity: Methods of directing stem cell fate for therapeutic purposes through the deliberate manipulation of caspase-3 activity are provided. The use of modulators of caspase-3 activity to modulate stem cell differentiation is described including activators and/or effectors of caspase-3, which can be used to induce stem cell differentiation, and inhibitors of...

20060100136 - Synergistic effects of combined administration of mirtazapine and a stimulant compound: The invention discloses combination therapies and formulations of a stimulant (e.g., amphetamine) and mirtazapine and their methods of use....

20060100137 - Methods of treating diabetes mellitus: Methods of treating diabetes mellitus in a patient in need of such treatment include administering an effective amount of an insulin drug to the patient in order to treat diabetes mellitus in the patient. Methods according to the present invention may “activate” the liver, potentially restoring normal glucose homeostasis to...

20060100138 - Implantable collagen compositions: The present invention relates to collagen compositions suitable for use in various tissue augmentation procedures....

20060100139 - Pharmaceutical used for treating hiv infection, the composition and uses thereof: A fusion inhibitor used to treat HIV infection, has an amino acid sequence as follows: X-SWETWEREIENYTKQIYKILEESQEQQDRNEKDLLE-Z, wherein X is either an amino group or -X1-X2, wherein X1 is an imino group, and X2 is either an acetyl group, a hydrophobic group, or a macromolecular carrier group; Z is a carboxyl...

20060100141 - Anti-allergic complex molecules: The present invention discloses novel anti-allergic complex molecules, and in particular, peptidic or peptidomimetic molecules, that includes a first part which is competent for cell penetration and a second part which is able to reduce or abolish mast cell degranulation, in particular to reduce or abolish allergy mediators, including histamine...

20060100140 - Combination of a) n-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]2-methylphenyl}-4- (3-pyridyl)-2-pyrimidine-amine and b) a histone deacetylase inhibitor for the treatment of leukemia: The invention pertains to a combination of a histone deacetylase inhibitor and N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine or a pharmaceutically acceptable salt thereof for simultaneous, separate or sequential use for the treatment of leukemia and especially N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-resistant leukemia....

20060100147 - Anticancer peptide: A polypeptide and methods of using the polypeptide for treating malignancy by administering to a subject a composition of the polypeptide. Pharmaceutical compositions of the polypeptide....

20060100146 - Awat-related methods and articles: This invention provides methods for treating a subject afflicted with acne or another sebaceous gland disorder comprising administering to the subject a therapeutically effective amount of an agent which inhibits acyl-CoA wax alcohol acyltransferase 1 (AWAT1) and/or acyl-CoA wax alcohol acyltransferase 2 (AWAT2), thereby treating the subject. This invention further...

20060100144 - Conjugates of insulin-like growth factor binding protein-4 and poly (ethylene glycol): A conjugate consisting of insulin-like growth factor binding protein 4 (IGFBP-4) and one or two polyethylene glycol) group(s), said polyethylene glycol) group(s) having an overall molecular weight of from about 30 to about 40 kDa is disclosed. This conjugate is useful for the treatment of cancer....

20060100149 - Conjugates of membrane translocating agents and pharmaceutically active agents: Membrane translation peptides, compositions comprising them, chimeric molecules comprising them, and methods of using them to achieve transmembrane transport of various agents....

20060100153 - Hsulf-1 nucleic acids, polypeptides and methods of using: HSulf-1 nucleic acids and polypeptides are provided, as are methods of using the nucleic acids and polypeptides....

20060100145 - Human chondroosteomodulin (tig2), production, and use for the treatment or diagnosis of bone diseases, cartilage diseases, cartilage diseases, obesity, inflammatory diseases, and skin diseases: The invention relates to the polypeptide COM and its derivatives, and methods for its preparation and recovery in a pure or partially purified form from body fluids and tissues, and its use as a medicament....

20060100152 - Methods and compositions in treating pain and painful disorders using 9949, 14230, 760, 62553, 12216, 17719, 41897, 47174, 33408, 10002, 16209, 314, 636, 27410, 33260, 619, 15985, 69112, 2158, 224, 615, 44373, 95431, 22245, 2387, 16658, 55054, 16314, 1613: The present invention relates to methods for the diagnosis and treatment of pain or painful disorders. Specifically, the present invention identifies the differential expression of 9949, 14230, 760, 62553, 12216, 17719, 41897, 47174, 33408, 10002, 16209, 314, 636, 27410, 33260, 619, 15985, 69112, 2158, 224, 615, 44373, 95431, 22245, 2387,...

20060100151 - Methods of treating osteoarthritis using il-17 receptor proteins in combination with tnf-receptor proteins: Methods for regulating levels of nitric oxide are disclosed. The methods utilize IL-17 receptors, which may be used in conjunction with inhibitor of IL-1 and/or TNF....

20060100148 - Peptide viral entry inhibitors: The present invention provides, inter alia, peptide compositions and methods for treating and preventing Flaviviridae virus (e.g., HCV) infections....

20060100150 - 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...

20060100143 - Polypeptide: The invention relates to a polypeptide, or part thereof, which inhibits the apoptotic activity of the tumour suppressor protein p53 and including screening methods to identify agents which interfere with the activity of said polypeptide....

20060100142 - Use of uk114 in the treatment of leishmaniasis: This invention relates to the use of the protein UK114, possibly associated with ubiquitin, for the treatment of leishmaniasis in humans and animals....

20060100154 - Long-acting gonadotropin-releasing hormone analogs and methods of use thereof: The present invention relates to the design, synthesis and biological evaluation of potent long-acting gonadotropin-releasing hormone (GnRH) analogs including agonists and antagonists comprising a GnRH peptide conjugated to emodic acid or an emodic acid derivative. These long acting analogs bind to GnRH receptors with high affinity and are devoid of...

20060100155 - Method for the therapeutic management of endometriosis: The present inventions provides a method for therapeutic management of extrauterine proliferation of endometrial tissue, chronic pelvic pain and fallopian tube obstruction by short term induction treatment with an LH-RH antagonist for 4 to 12 weeks. According to another aspect of the present invention, the short term LH-RH treatment is...

20060100156 - Cell nucleus-entering compositions: A pharmaceutically acceptable composition and method for entering a cell nucleus utilizes a cell nucleus-entering polypeptide including at least one of amino acid sequence LKKTET, amino acid sequence LKKTNT or amino acid sequence KSKLKK, or a conservative variant thereof, linked to a physiologically active agent having at least one of...

20060100157 - Novel use of peptide compounds for treating pain in painful diabetic neuropathy: The present invention concerns the use of compounds for treating pain in painful diabetic neuropathy, preferably in diabetic distal sensory polyneuropathy....

20060100159 - Preventing desensitization of receptors: Desensitization of receptors that control disease is prevented by inhibiting G-protein receptor kinases. This has applicability, e.g., for patients with heart failure or on a left ventricular heart device or a heart pump after surgery or about to undergo surgery and at high risk for a cardiac event or on...

20060100158 - Statine derivatives for the treatment of alzheimer's disease iii: s

20060100160 - Amino acid derived prodrugs of propofol, compositions and uses thereof: The present invention provides propofol prodrugs, methods of making propofol prodrugs, pharmaceutical compositions of propofol prodrugs and methods of using propofol prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as migraine headache pain and post-chemotherapy or post-operative surgery nausea and vomiting....

20060100161 - Mitotic kinesin inhibitors and methods of use thereof: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders....

20060100162 - Methods of mimicking the metabolic effects of caloric restriction by administration of mannoheptulose: A method of obtaining beneficial biological results associated with caloric restriction may be gained by administration of a composition containing at least one active agent which blocks metabolism of glucose as a source of energy in cells in glucose metabolism blocking effective amounts to an animal in need thereof....

20060100163 - Pharmaceutically active oligosaccharide conjugates: The present invention relates to pharmaceutically active oligosaccharide conjugates having the formula: (X—Ym)n—S, wherein component X is a pharmaceutically active compound, Y is a bifunctional linker, and S is an oligosaccharide consisting of 1 to 20 saccharide units, n is equal or less than the number of the saccharide units...

20060100164 - Novel antibacterial agents: This invention relates to novel macrolides, to the preparation of novel macrolides, to the use of such novel macrolides for preventing, treating, or ameliorating various conditions, and to the use of such novel macrolides as antibacterial agents....

20060100165 - Topical application of ivermectin for the treatment of dermatological conditions/afflictions: Dermatological conditions/afflictions such as rosacea, common acne, seborrheic dermatitis, perioral dermatitis, acneform rashes, transient acantholytic dermatosis, and acne necrotica miliaris, most notably rosacea, are treated by topically applying onto the affected skin area of an individual in need of such treatment, a topical pharmaceutical composition which comprises a thus effective...

20060100166 - Compounds for modulating the activity of exchange proteins directly activated by camp (epacs): The present invention relates to novel compounds for modulating the activity of exchange proteins directly activated by cAMP (Epacs). In particular, the present invention relates to cAMP analogues that specifically modulate the activity of Epacs. The invention further relates to pharmaceutical compositions comprising the novel compounds, and the use of...

20060100167 - Methods and compositions for the treatment of autoimmune disorders using clofarabine: This invention relates to methods of treating or preventing an autoimmune disorder comprising the administration of clofarabine or a pharmaceutically acceptable salt, hydrate, solvate, clathrate, prodrug or metabolite thereof to a patient in need of such treatment. The invention further relates to methods of treating or preventing an autoimmune disorder...

20060100168 - Method of treating cancer using adenosine and its analogs: The present invention provides methods of treating individuals having malignancies associated with estrogen receptor activity comprising administering to an individual affected with said malignancy, an effective amount of adenosine analog in a pharmaceutical carrier to downregulate or diminish estrogen receptors in the cells. The invention further provides methods of identifying...

20060100169 - Method to reduce an inflammatory response from arthritis: The present invention provides a therapeutic method for treating an inflammatory response caused by autoimmune stimulation, comprising the administration to a patient in need thereof of an antiinflammatory amount amount of an A2A adenosine receptor agonist. The autoimmune stimulation can be caused by arthritis, particularly rheumatoid arthritis. Optionally, the method...

20060100170 - Isopycnic pharmaceutical formulation: The present invention is directed to pharmaceutical compositions comprising an aqueous solution in which the density of the aqueous solution is isopycnic or substantially isopycnic with a pharmaceutical agent. The present invention is also directed to methods for storing such pharmaceutical compositions and formulations, and to the use of such...

20060100171 - Branched alpha-glucans for weight management: Highly branched α-glucan having an average molar weight of at least 105 Da can be used for inducing or enhancing satiety and/or satiation in humans or animals by incorporation of the α-glucan into a liquid nutritional or pharmaceutical composition, preferably together with a food protein. The α-glucan induces a viscosity...

20060100174 - Configuration of glycosaminoglycans: The present invention provides stable glycosaminoglycan (GSG) structures and methods of use of such GAG structures. These structures comprise a core of free GAG, a coating of crosslinked GAG surrounding the core, and a layer of a positively charged moiety surrounding the crosslinked GAG layer. These GAG structures provide improved...

20060100173 - Ophthalmic solution: An improved ophthalmic composition comprising an anionic polymeric substance, such as Hyaluronic Acid and/or Carboxymethylcellulose, in combination with any of various cationic monomeric or dimeric antimicrobial agents, such as Cetylpyridinium Chloride and/or Alexidine Dihydrochloride, wherein said compositions provide additional comfort and biocompatibility with lenses without significantly affecting the antimicrobial efficacy...

20060100172 - Use of prebiotics, preferably glucooligosaccharide, for the prevention of the onset of type ii diabetes: The invention relates to the use of prebiotics for the preparation of food or pharmaceutical compositions which are intended for the treatment and/or prevention of hyperglycaemic syndromes and, in particular, for the treatment of Type II diabetes and/or the prevention of the onset of Type II diabetes in patients with...

20060100175 - Novel therapeutic use of low molecular weight heparins: The invention concerns the use of low molecular weight heparin for preventing and/or treating motor neuron diseases....

20060100176 - Carboxylic acid diesters, methods for the production thereof and methods for the production of pharmaceutical active substances coupled to free amino groups with polysaccharide or polysaccharide derivatives: The invention relates to carboxylic acid diesters of starch fractions or starch fraction derivatives in addition to solids and solutions containing said carboxylic acid diesters. The invention also relates to methods for the production of said carboxylic acid diesters, methods for the production of pharmaceutical active substances coupled to free...

20060100178 - Dermal agent: A dermal agent for preventing or treating acne, comprising an ascorbic acid derivative which liberates in vivo ascorbic acid, and a zinc salt or comprising a zinc salt of the ascorbic acid-2-phosphate, and a composition comprising tretinoin and an ascorbic acid derivative or a salt thereof, relieving in the irritation...

20060100177 - Stabilized ascorbic acid derivatives: An ascorbic acid derivative, which is a compound represented by the following general formula (1) or a salt thereof: [Chemical Formula 11] (1)(wherein X and Y each represents H or a protective group for OH, R1 and R2 each represents an alkly group having from 1 to 19 carbon atoms,...

20060100179 - Compositions and methods for use in targeting vascular destruction: Treatment of warm-blooded animals having a tumor or non-malignant hypervascularation, by administering a sufficient amount of a cytotoxic agent formulated into a phosphate prodrug form having substrate specificity for microvessel phosphatases, so that microvessels are destroyed preferentially over other normal tissues, because the less cytotoxic prodrug form is converted to...

20060100180 - Composition containing an androgenous 11b-halogen steroid and a progestational hormone, and male contraceptive based on said composition: The invention relates to a novel chemical composition containing an androgenous 11β-halogen steroid and the progestational hormone of formula (I), to a pharmaceutical composition containing said chemical composition and to a male contraceptive based on said pharmaceutical composition....

20060100182 - pharmaceutical compositions for the treatment of urinary incontinence: Pharmaceutical compositions for the treatment of urinary incontinence with a cholinergic and musulotropic substance, combined or not combined with a little resorbed estrogen agent, by local route, wherein the cholinergic and musculotropic substance is oxybutynin, or one of its salts, and the little resorbed estrogen agent is chosen from estriol,...

20060100181 - Combinations for the treatment of inflammatory skin disorders: The invention features methods and compositions for the treatment of inflammatory skin conditions....

20060100183 - Therapeutic agents targeting the ncca-atp channel and methods of use thereof: The present invention is directed to therapeutic compositions targeting the NCCa-ATP channel of an astrocyte, neuron or capillary endothelial cell and methods of using same. More specifically, antagonists of the NCCa-ATP channel are contemplated. The compositions are used to prevent cell death and to treat secondary damage associated with spinal...

20060100184 - 5-beta-sapogenin and pseudosapogenin derivatives and their use in the treatment of dementia: The invention discloses the use of sapogenin derivatives in the treatment of cognitive disfunction and similar conditions. Methods of treatment and pharmaceutical compositions are also disclosed...

20060100185 - 5-androsten-3beta-ol steroid intermediates and processes for their preparation: The present invention provides 5-androsten-3β-ol steroid intermediates and processes for their preparation....

20060100186 - Trandsdermal compositions and methods for treatment of fibromyalgia and chronic fatigue syndrome: Compositions and methods for alleviating the symptoms associated with chronic fatigue syndrome and fibromyalgia syndrome are provided. The compositions are based on use of a transdermal gel formulation delivery system for androgens, either alone or in combination with other hormones....

20060100187 - Synergistic combinations of macrolide t-cell modulator or immunosuppressant and a retinoid: Additive or synergistic combinations of a macrolide T-cell immunomodulator or immunosuppressant such as 33-epichloro-33-desoxyascomycin and a retinoid, such as etretinate, isotretinoin or tazarotene, optionally with a further pharmaceutically active agent, especially an antibacterial, are provided, which are useful in particular in the treatment of dermatological diseases such as eczema, atopic...

20060100188 - Treatment methods: There are disclosed methods for treating cancer in a patient in need of such treating comprising administering temozolomide according to improved dosing regimen and/or schedules based on the patient's MGMT level. Additional improved methods for treating patients with temozolomide are also disclosed....

20060100189 - Method of treating or preventing pathologic effects of acute increases in hyperglycemia and/or acute increases of free fatty acid flux: One aspect of the present invention relates to a method of treating or preventing pathologic sequelae of acute hyperglycemia and/or increased fatty acid flux in a subject. This method involves administering an ROS inhibitor to the subject. In addition, methods of promoting neovascularization, inhibiting oxidation or excessive release of free...

20060100190 - Motexafin lutetium phototherapy with low fluences for treating vascular inflammation: Described herein are compositions, methods, therapies, strategies, techniques and processes for treating vascular inflammation in blood vessels by administering a photo-activatable compound and low light fluence in the range of about 10 to about 400 Joules/cm of illuminated length in the general vicinity of the inflammation....

20060100193 - Factor xa inhibitors: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat...

20060100192 - Heteroaryl diazacycloalkanes, their preparation and use: The present invention relates to novel heteroaryl diazacycloalkane derivatives, which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic...

20060100191 - Mitotic kinesin inhibitors: The present invention relates to 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 is also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals....

20060100194 - Lactam compounds useful as protein kinase inhibitors: The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases....

20060100195 - Remedies for urinary frequency: The present invention relates to an agent for the treatment and/or prevention of pollakiuria comprising a compound having an antagonism to an EP1 receptor which is a prostaglandin E2 receptor subtype. A compound having an antagonism to an EP1 receptor antagonistically acts on an EP1 receptor which is a prostaglandin...

20060100196 - Substituted amines for the treatment of alzheimer's disease: Disclosed are compounds of formula (I) which are 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...

20060100197 - Fused-ring pyridine derivative, process for producing the same, and use: R2 is (1) an amino group, in which the nitrogen atom is converted to quaternary ammonium or oxide, (2) a nitrogen-containing heterocyclic group which may contain a sulfur atom or an oxygen atom as a ring-constituting atom, in which the nitrogen atom may be converted to a quaternary ammonium or...

20060100198 - Polymorphic and amorphous forms of the phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6h-azepino[5,4,3-ce]indol-6-one: The present invention relates to novel polymorphic and amorphous forms of a phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the...

20060100199 - Novel condensed imidazole derivatives: e

20060100200 - Process for making a non-nucleoside hiv-1 reverse transcriptase inhibitor:

20060100201 - Inhibitors of c-fms kinase: wherein A, X, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast...

20060100204 - Anti-cytokine heterocyclic compounds: e

20060100203 - Fungicides based on nitrogen-containing heterocycles:

20060100202 - Novel compounds:

20060100205 - 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 is a cannabinoid receptor antagonist. Also disclosed are methods of affecting weight loss, increasing energy expenditure, increasing satiety in an individual, or suppressing...

20060100206 - Heterocyclic cb1 receptor antagonists: s

20060100207 - Dihydropyridinone derivatives: The invention relates to novel dihydropyridinone derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development....

20060100209 - Formulations of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1h-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione: The instant invention provides formulations of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione; processes for the production of such formulations; and methods of treating HIV or AIDS with such crystalline materials or such formulations....

20060100208 - Pyrazole derivatives as cannabinoid receptor antagonists: One aspect of the invention is concerned with cannabimimetic pyrazole analogs. Another aspect of the invention is concerned with new and improved pyrazole analogs having high affinities and/or selectivities for the CB1 cannabinoid receptor. A further aspect of the invention is concerned with pharmaceutical preparations employing the inventive analogs and...

20060100211 - Pyrimidine derivatives: e

20060100212 - Oxadiazole ketone inhibitors of fatty acid amide hydrolase: Certain oxadiazole ketone compounds are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat anxiety, pain, inflammation, sleep disorders, eating...

20060100210 - Methods for treatment of scleroderma: Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes and other such inhibitors are useful for the treatment of scleroderma....

20060100213 - Triazoles and methods of use: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject...

20060100214 - Fast dissolving and taste masked oral dosage form comprising sildenafil: A fast dissolving and taste masked sildenafil solid dosage form comprising: (i) sildenafil granules which granules comprise at least 45% by weight of a salt of sildenafil, a solubilisation inhibitor for said salt of sildenafil and optionally a sweetening agent and (ii) one or more disintegrants wherein the disintegrants or...

20060100215 - 8a,9-dihydro-4ah-isothiazolo[5,4-b]quinoline-3,4-diones and related compounds as anti-infective agents: Certain compounds of Formula I and Formula II disclosed herein are potent and/or selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents....

20060100216 - Novel b1 bradykinin receptor antagonists: The invention encompasses novel compounds and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for treatment of diseases mediated by B1 bradykinin receptor....

20060100219 - Novel bradykinin-b1 antagonists, process for their preparation and their use as medicaments: in which A, Ar, G, Q, R1 and R4 are as defined in claim 1, their enantiomers, their diastereomers, their mixtures and their salts, in particular their physiologically acceptable salts with organic or inorganic acids or bases having useful properties, their preparation, medicaments comprising the pharmacologically effective compounds, their preparation...

20060100218 - Pde4b inhibitors: Compounds are described that are active on PDE4. Also described are crystal structures of PDE4B determined using X-ray crystallography, the use of PDE4B crystals and strucural information for identifying molecular scaffolds, for developing ligands that bind to and modulate PDE4B, and for identifying improved ligands based on known ligands....

20060100217 - Preparation of 4-haloalkylnicotinamides: m

20060100220 - Fungicidal mixtures based on imidazole derivatives: where X1 and X2 are halogen and phenyl which may be substituted by halogen or alkyl or X1 and X2 together with the bridging C═C double bond form a difluoromethylenedioxyphenyl group; X3 is cyano or halogen, and X4 is dialkylamino or isoxazol-4-yl which may carry two alkyl radicals, in a...

20060100221 - Novel compound: A compound of formula (I) and pharmaceutically acceptable salts or solvates thereof for use in therapy....

20060100222 - Selective phosphodiesterase 9a inhibitors as medicaments for improving cognitive processes: The invention relates to the use of selective phosphodiesterase 9A (PDE9A) inhibitors for producing medicaments for improving perception, concentration, cognitive processes, learning and/or memory....

20060100223 - Quinazoline derivatives and pharmaceutical compositions containing them: or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of...

20060100226 - 2-thiopyrimidinones as therapeutic agents: The present invention provides compounds of Formulas I-VII, or pharmaceutically acceptable derivatives thereof, wherein the compounds are as defined in the specification. These compounds are inhibitors of protein kinases, particularly inhibitors of MEKK protein kinases. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods...

20060100225 - Heteroaryl guanidines; inhibitors of viral replication: Certain compounds of Formula 1 described herein which possess potent antiviral activity. Certain compounds of Formula 1 that are potent and/or selective inhibitors of Hepatitis C virus replication. Pharmaceutical compositions containing one or more compounds of Formula 1, or a salt, solvate, or acylated prodrug of such compounds, and one...

20060100224 - Piperidine ouracil used as a medicament for treating bacterial infections: The invention relates to piperidine ouracil and a method for the production thereof in addition to the use thereof in the production of medicaments for treating and/or in the prophylaxis of diseases, especially bacterial diseases....

20060100227 - Pyrimidine derivaties: e

20060100228 - Cannabinoid receptor ligands:

20060100229 - Pyrazolopyridines and analogs thereof: Pyrazolopyridin-4-amines, pyrazoloquinolin-4-amines, pyrazolonaphthyridin-4-amines, and 6,7,8,9-tetrahydropyrazoloquinolin-4-amines, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed....

20060100230 - Indolin phenylsulfonamide derivatives: The invention relates to novel substituted indolin phenylsulfonamide derivatives, to a method for the production thereof and to the use thereof in medicaments, especially as potent PPAR-delta activating compounds for the prophylaxis and/or treatment of cardiovascular diseases, especially dyslipidaemia and coronary heart diseases....

20060100231 - Amorphous clopidogrel hydrogen sulfate: The invention relates to a novel amorphous form of clopidogrel hydrogen sulfate, to processes for its preparation thereof and to a pharmaceutical composition containing it....

20060100232 - Inhibitors of hiv-1 capsid formation: substituted aryl aminomethyl thiazole ureas and analogues thereof: wherein the variables A, R1, R2, R3, R4, X, Y, Z, A5, A6, A7, R8, R9, R12, and R13 are defined herein. Pharmaceutical compositions comprising such compounds and methods of treating animals infected with a virus having a capsid protein are provided herein. Methods of using such compounds to treat...

20060100234 - 8-substituted imidazopyridines: e

20060100233 - 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 pyrazole-tetrahydro pyridine derivative. The invention also provides specific pyrazole-tetrahydro pyridines, a library comprising at least two of...

20060100235 - Pharmaceutical use of substituted 1,2,4-triazoles: The use of substituted 1,2,4-triazoles for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions has been described. Also a novel class of substituted 1,2,4-triazoles, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the...

20060100236 - 5-ht4 receptor agonist compounds: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds....

20060100237 - Excitatory amino acid receptor antagonists: The present invention provides novel compounds of Formula (I) and Formula (I(a)), or the pharmaceutically acceptable salts thereof; methods for treating neurological disorders and neurodegenerative diseases, particularly pain and migraine, comprising administering a compound of Formula (I) or Formula (I(a)); and processes for preparing compounds of Formula (I) or Formula...

20060100238 - Aminated isoflavonoid derivatives and uses thereof: Aminated isoflavonoid synthesized by aminating the 4-keto group of isoflavanone and isoflavanone ring systems, pharmaceutical compositions containing same and uses thereof as therapeutic agents....

20060100239 - Method for producing optically active amines: The present invention provides a method for producing optically active amines of formula (9) or (10): which comprises reacting an imine equivalent of formula (6): with an alkene of formula (7) or an alkyne of formula (8): in the presence of a chiral catalyst, which method does not require additional...

20060100240 - Chemokine receptor binding heterocyclic compounds with enhanced efficacy: The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4...

20060100241 - Method for enhancing mutant protein activity: Provided is a method for enhancing the activity of a protein, which protein when mutated, folds in an incorrect conformation in the endoplasmic reticulum, by contacting the protein with an effective amount compound which specifically binds to the protein and induces the protein to fold into a proper conformation (a...

20060100242 - 4-(2-phenylsulfanyl-phenyl)-piperidine derivates as serotonin reuptake inhibitors: The invention provides compounds represented by the general formula (I) wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder....

20060100243 - Methylphenidate analogs and methods of use thereof: Provided are analogs of methylphenidate (“MPH”) that are useful for the treatment of drug addiction, attention deficit disorder, attention deficit hyperactivity disorder, and depression. The MPH analogs are extended duration compounds that bind to the dopamine transporter and the reuptake of dopamine in the afflicted individual's brain. Because of the...

20060100244 - Novel aryl-[4-halo-4(heteroarylmethylamino)-methyl]-piperidin-1-1yl]-methanone derivatives, methods for production and use thereof as medicaments: The invention relates to compounds of general formula (1) in which X and Y=a carbon with a bonded hydrogen atom (CH) or a nitrogen atom, A=a methyl, fluoromethyl, cyano, hydroxyl, methoxy group, or a chlorine or fluorine atom on condition that when A=methyl (CH3) and X and Y both=a carbon...

20060100245 - Substituted biphenyl-4-carboxylic acid arylamide analogues: Substituted biphenyl-4-carboxylic acid arylamide analogues capable of modulating receptor activity, are provided. Such ligands may be used to modulate receptor activity in vivo or in vitro, and are particularly useful in the treatment of pain and other conditions associated with receptor activation in humans, domesticated companion animals and livestock animals....

20060100246 - Pyridine derivatives: This invention is to provide a process for producing 2-amino-4,6-disubstituted nicotinic acid ester analogs and salts thereof, comprising the reaction shown by the following scheme. The ester analogs can be prepared in one pot, and in good yield by using tertiary alkyl cyanoacetate. Furthermore, the method is useful for preparing...

20060100247 - Treatment of diabetes with thiazolidinedione and metformin: A method for the treatment and/or prophylaxis of diabetes mellitus, conditions associated with diabetes mellitus and certain complications thereof, in a mammal which method comprises administering an effective non-toxic and pharmaceutically acceptable amount of an insulin sensitiser and a biguanide antihyperglycaemic agent, to a mammal in need thereof and a...

20060100248 - Blockade of voltage dependent sodium channels: Compounds of Formula I and pharmaceutically acceptable salts thereof, are capable of blockading voltage-dependent sodium channels and are useful in particular, in treating glaucoma and multiple sclerosis....

20060100249 - Pharmaceutical compositions comprising dihydropyridinone compounds and an immunoregulatory or an antiinflammatory agent and their uses: The present invention relates to compositions comprising 1,2-dihydropiridin-2-one compounds and an immunoregulatory or anti-inflammatory agent. The compositions are useful for the prevention or the treatment of neurodegenerative diseases, for example demyelinating disorders....

20060100250 - Biphenyl derivatives and their use as fungicides: A fungicidally active compound of formula (1): where Het is a substituted 5- or 6-membered heterocyclic ring; R1 is hydrogen, formyl, CO-C1-4 alkyl, COO-C1-4 alkyl, C1-4 alkoxy(C1-4)alkylene, CO-C1-4 alkylenoxy(C1-4)alkyl, propargyl or allenyl; R2, R3, R4 and R5 are each, independently, hydrogen, halogen, methyl or CF3; each R6 is, independently, halogen,...

20060100252 - Aminoalcohol derivatives: f

20060100251 - Substituted phenylalkanoic acids: which are useful in the treatment of metabolic disorders related to insulin resistance or hyperglycemia. These compounds include inhibitors of protein tyrosine phosphatase (PTP-1B) that are useful in the treatment of diabetes and other PTP-1B mediated diseases, such as cancer, neurodegenerative diseases and the like. The compounds of the invention...

20060100253 - Novel compounds for the treatment of neurological disorders: i

20060100254 - Thiazolyl-dihydro-indazole:

20060100256 - Process for preparing 2,6-diamino-4,5,6,7-tetrahydro-benzothiazole: 2,6-diamino-4,5,6,7-tetrahydro-benzothiazole, which is useful for making pramipexole, is made by: (i) reacting bromine with a solution of 4-acetamido-cyclohexanone in water to produce 2-bromo-4-acetamido-cyclohexanone; (ii) after step (i), adding thiourea to produce 6-acetyl amino-2-amino-4,5,6,7-tetrahydro-benzthiazole; (iii) after step (ii), adding an aqueous solution of hydrobromic acid to produce 2,6-diamino-4,5,6,7-tetrahydro-benzthiazole dihydrobromide; and (iv)...

20060100255 - Substituted indolealkanoic acids derivative and formulations containing same for use in the treatment of diabetic complications: Disclosed is a compound of the formula (I) its hydrates and/or pharmaceutically acceptable salts, which are useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their preparation....

20060100257 - Inhibitors against the activation of ap-1 and nfat: wherein X represents a connecting group whose number of atoms in the main chain is 2 to 5 (said connecting group may be substituted), A represents hydrogen atom or acetyl group, E represents an aryl group which may be substituted or a hetero aryl group which may be substituted, ring...

20060100258 - Growth promotion method: R6 and R7 are either the same or different and selected from hydrogen and a non-deleterious substituent or one of R6 and R7 are absent when there is a double bond present, pharmaceutically or veterinarily acceptable salts or derivatives, pro-drugs, tautomers and/or isomers thereof to a subject in need thereof....

20060100259 - Process for the preparation of substituted triazole compounds: The present invention is directed to a novel process for the preparation of substituted triazole compounds, useful in the treating or ameliorating a selective kinase or dual-kinase mediated disorder. The process of the present invention preferentially produces the desired regioisomer of the substituted triazole compounds....

20060100260 - Substituted pyrazoline carboxanilides for use as pesticides: e

20060100261 - Furan or thiopene derivative and medicinal use thereof: [wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, p is 0, 1 or 2, and when p is 2, each R may be the same or different, R1 is a hydrogen atom or an optionally substituted hydrocarbon group, R2 is an optionally substituted aromatic...

20060100262 - Tetracyclic indole derivatives as antiviral agents: h

20060100263 - Antipyretic compositions and methods: Methods and compositions containing bicifadine are provided for the treatment and prevention of hyperthermia in mammalian subjects. The methods and compositions may be used to prevent or treat fever, pyresis, menopausal hot flashes; peri menopausal hot flashes, postmenopausal hot flashes, hot flashes caused by anti-estrogen therapy, hot flashes secondary to...

20060100264 - 3,3'-diindolylmethane immune activating compositions: The invention provides immune response activating compositions and methods of use. The general methods deliver an immune response activator to a patient determined to be in need thereof, comprising the steps of: (a) administering to the patient a predetermined amount of an immune response activating, optionally substituted DIM; and (b)...

20060100265 - 4-(1-(sulfonyl)-1h-indol-2-yl)-4-(hydroxy)-cyclohexa-2,5-dienone compounds and analogs thereof as therapeutic agents: This invention pertains to certain 4-(1-(sulfonyl)-1H-indol-2-yl)-4-(hydroxy)-cyclohexa-2,5-dienone compounds, and analogs thereof, including compounds of the following formula, which are, inter alia, antiproliferative agents, anticancer agents, and/or thioredoxin/thioredoxin reductase inhibitors: formula (I) wherein: Ar is a 1-(sulfonyl)-1H-indol-2-yl group; the bond marked α is independently: (a) a single bond; or: (b) a double...

20060100266 - Indole compounds useful as serotonin selective agents: Novel indole compounds are disclosed. Also disclosed are methods for using the compounds to treat human and animal disease, pharmaceutical compositions of the compounds, and kits including the compounds....

20060100267 - Novel crystal forms of atorvastatin hemi-calcium and processes for their preparation as well as novel processes for preparing other forms: The present invention provides novel forms of atorvastatin designated Forms VI, VIII, IX, X, XI and XII and novel processes for their preparation as well as processes for preparing atorvastatin Forms I, II, IV, V and amorphous atorvastatin....

20060100268 - Method of treating atherosclerosis or restenosis using microtube stabilizing agent: The present invention is a method of preventing or reducing atherosclerosis or restenosis, and a pharmaceutical preparation used therefor. In particular, it is a method of preventing or reducing atherosclerosis or restenosis after arterial injury by treatment with a low dose of a microtubule stabilizing agent such as taxol or...

20060100269 - Use of 10-aminoaliphatyl-dibenz[b,f]oxepines for the treatment of degenerative ocular disorders: The present invention relates to novel uses of 10-aminoaliphatyl-dibenz[b,f]oxepines for the treatment of degenerative ocular disorders....

20060100270 - Methods for preventing, attenuating or treating pulmonary hypertension using a serotonin transporter inhibitor, and pharmaceutical compositions for the treatment thereof: The invention relates to a method for preventing, attenuating or treating pulmonary hypertension in an individual in need thereof, comprising administering at least one 5-HTT inhibitor to said individual....

20060100271 - Stabilized aqueous ranitidine compositions: An ethanol free aqueous pharmaceutical ranitidine composition of ranitidine, or pharmaceutically acceptable salt thereof, is stabilized with an effective amount of hydroxyethyl cellulose. Preferred excipients include methyl paraben, and either sorbitol or sucrose....

20060100272 - Formulations for the treatment of pain: Formulations and methods are provided for the treatment of pain, and neuropathic pain in particular. The formulations are eutectic mixtures of a capsaicinoid and a local anesthetic agent and/or an anti-pruritic agent....

20060100273 - Anhydrous silver dihydrogen citrate compositions: Anhydrous silver dihydrogen citrate compositions comprise silver dihydrogen citrate and citric acid. The anhydrous compositions can be prepared by freeze-drying. The anhydrous compositions can be reconstituted with a suitable diluent to form silver dihydrogen citrate compositions. The anhydrous compositions can be reconstituted and applied to a variety of substrates to...

20060100275 - Agent for treating interstitial cystitis: wherein R1 represents hydroxyl group or a lower alkoxy group, or a pharmacologically acceptable salt thereof. Since the phenoxyacetic acid derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof or a hydrate or solvate thereof has a selective β3-adrenoceptor stimulating activity and a remarkable action to...

20060100274 - Therapeutic avenanthramide compounds: Methods and compositions are disclosed for reducing pro-inflammatory molecules, adhesion molecules, and vascular smooth muscle cell proliferation, and for increasing NO production. The present invention describes the use of phenolic compositions, purified from oats or synthetically produced, to decrease the effective amount of pro-inflammatory molecules and/or cell adhesion molecules. Alternatively,...

20060100276 - Method of treating neutrophil-related diseases with topical anesthetics: A therapeutic method is provided to treat neutrophil-associated pulmonary diseases, such as chronic obstructive pulmonary disease, by locally administering to a mammal in need of such treatment, an effective amount of a topical anesthetic, such as lidocaine, or a pharmaceutically acceptable salt thereof....

20060100277 - Antibiotics cyan-416 a, cyan-416 b, cyan-416 c, cyan-416 d and cyan-416 e, and ester derivatives of cyan-416 b: The invention relates to new antibiotics designated Cyan-416A, Cyan 416B, Cyan-416C, Cyan-416D and Cyan-416E to their production by fermentation of Acremonium sp. NRRL 30631 to methods for recovery and concentration from the crude solutions, and to a process for purification and to semisynthetic ethers of Cyan-416B....

20060100278 - Dosage forms and related therapies: This invention is directed in part to novel doses, dosage formulations, and routes of administration of such doses and dose formulations, said dose and dose formulations containing one or more copper chelators, for example, one or more trientine active agents, including trientine analogues, trientine salts, trientine prodrugs, and trientine derivatives,...

20060100279 - Production of dha in microalgae in low ph medium: Methods for production of highly unsaturated fatty acids by marine microorganisms, including the heterotrophic marine dinoflagellate Crypthecodinium, using low levels of chloride ion are disclosed. Specifically, methods of increasing production of highly unsaturated fatty acids by marine microorganisms while growing in low chloride media by manipulating sodium ion and potassium...

20060100280 - Cell growth regulator: The present inventors examined cell growth of human colon cancer cell lines and breast cancer cell lines using L-2-phenylglycine, which is considered to be an amino acid transporter ATB0,+ inhibitor, as a test substance to reveal a concentration-dependent cell growth inhibitory effect. This result shows that inhibition of ATB0,+ activity...

20060100281 - Method of treating tinnitus: e

20060100282 - Novel diaminopropane-based metal chelators as antiviral agents: wherein A is selected from the group consisting of —(CH2)a—, —(CH2)bO(CH2)c—, —(CH2O)d—, and —(CH2)eN(R4)(CH2)f—; a and c vary from 0 to 10; b, e, and f vary from 2 to 10, and d varies from 1 to 10. X and Y are independently —CR5R6, or —CH(R7)CH(R8). R1 to R8 are...

20060100283 - Phenylcyclohexylpropanolamine derivatives, preparation and therapeutic application thereof: where R1 represents H or a (C1-C4)alkyl, —CO(C1-C4) alkyl, (C1-C4) alkylphenyl or —CO-phenyl group, said phenyl optionally being substituted; R2 represents H, a halogen atom, an —S(O)z(C1-C4)alkyl group, where z is equal to 0, 1 or 2, an —NHSO2(C1-C4)alkyl group, an —NHSO2-phenyl group or an —NHSO2—(C1-C4) alkylphenyl group, said phenyl...

20060100284 - Growth promotor: The invention relates to an animal growth promoting composition. The liquid solution comprises 1.1 to 5% by weight of sorbic acid or a sorbate calculated as sorbic acid, 45 to 93.9% by weight of formic acid and 5 to 50% by weight of propionic acid. The invention also relates to...

20060100285 - Hydroxamic acid derivatives having anti-inflammatory action: Compounds of formula (I) are described: The compounds (I) inhibit TNFα production and may therefore be useful in the treatment of inflammation, of auto-immune diseases, and of pathological conditions which involve excessive production of that cytokine. The compounds (I) are also inhibitors of the histone deacetylase enzyme and may therefore...

20060100286 - Treatment of canine hemangiosarcoma with a histone deacetylase inhibitor: The present invention is directed to a method of treating cancer, particularly canine hemangiosarcoma. The method includes the continuous and regular administration of a formulation including a histone deacetylase inhibitor as part of the standard canine diet. The preferred histone deacetylase inhibitor is SAHA. The formulation is administered following splenectomy...

20060100287 - Insulin-like growth factor-1 secretagogue: The present invention relates to an IGF-1 secretagogue containing one or two or more compounds selected from capsaicinoids, capsinoids and synthetic capsaicin, which has no problem of skin irritation, etc., and is effective for, for example, reducing skin wrinkle and sagging skin by the increase of skin's thickness and elasticity,...

20060100288 - Oil-in-water type emulsion with low concentration of cationic agent and positive zeta potential: A well tolerated oil-in-water emulsion useful as a delivery vehicle of hydrophobic ingredients such as pharmaceutical drugs, wherein the emulsion particles have a net positive charge and comprises 0.001 to 0.1% of a cationic agent, 0 to 1% of a non ionic surfactant and 0 to 0.5% of an anionic...

20060100289 - Nitrone compounds, pharmaceutical compositions containing the same and methods for treating inflammation and neuropathic pain: Disclosed are nitrone compounds and pharmaceutical compositions containing such compounds. The nitrone compounds have one to six additional carbons bridging between the nitrone functionality and the nitrone aryl ring. The disclosed compositions are useful as therapeutics for inflammation-related conditions and analgesia in mammals, such as arthritis, and for neuropathic pain...

20060100290 - Treatment of allergic rhinitis and asthma: This invention provides a method of treating allergic rhinitis in a mammal comprising administering a therapeutically effective amount of atomoxetine to a mammal in need of such treatment, and also provides a method of treating asthma in a mammal comprising administering a therapeutically effective amount of atomoxetine to a mammal...

20060100291 - Antibacterial compounds: There is an ongoing need for new antibiotics which may be effective against bacteria that are otherwise difficult to control. The present invention therefore relates to new antibacterial triketone compounds of Formula (1), or salts, metal complexes or tautomeric forms of these compounds. The compounds have potential as novel antibiotics....

20060094641 - Method for providing natural therapeutic agents with high therapeutic index: Methods for identifying and providing new therapeutic agent(s) by selecting at least one polypeptide encoded by a natural allelic variant of one preselected gene having a therapeutic potential; determining the therapeutic index of the selected polypeptide(s) and retaining as therapeutic agent(s) those polypeptide(s) whose therapeutic index is higher than that...

20060094642 - Method of increasing bone toughness and stiffness and reducing fractures: The invention relates to a method for increasing the toughness and/or stiffness of bone and/or reducing the likelihood and/or severity of bone fracture by administering a parathyroid hormone. The method can be employed to increase toughness or stiffness of bone at a site of a potential or actual trauma, such...

20060094643 - Compositions of hyaluronic acid and methods of use: The invention provides compositions for the treatment of disorders characterized by dryness including dry eye and dry mouth. The compositions commonly comprise a conjugate of hyaluronic acid and polylysine. These conjugates are attached to affected body tissues or surfaces using transglutaminase, and preferably endogenous transglutaminase....

20060094644 - Capreomycin derivatives and their use as antibacterials: The present subject matter relates to phenylurea capreomycin derivatives, and to metabolites and pharmaceutically acceptable salts and solvates thereof. The compounds of the present subject matter are useful as antibacterial agents for treating bacterial infections and for treating disorders caused by bacterial infections. The present subject matter also relates to...

20060094645 - Method for defining and treating chemically-induced immune disorders using tumor necrosis factor (tfnalpha), interleukin-1 (ll-1), and interleulin-6r(ll-6r) antagonists: Compositions and methods are disclosed for treating chemically-induced immune disorders. Pharmacological compositions comprising at least one TNF antagonist, at least one IL-1 antagonist, and at least one IL6R antagonist are disclosed....

20060094646 - Methods for inhibiting growth of prolactin-responsive cancer cells with cyclosporine a or other cyclophilin inhibitors: Methods are provided for inhibiting growth of prolactin-responsive cancer cells and treating prolactin-responsive malignancies via administration an agent such as cyclosporine A which directly inhibits an enzymatic activity of a cyclophilin....

20060094650 - Agent for improving life expectancy in therapy of malignant tumor: A medicament for improving prognostic survival in therapy of malignant tumor is provided that may improve prognostic survival in DIC patients where the basal disease is malignant tumor, especially malignant tumor in hematopoietic organs. The medicament according to the invention comprises as a main active ingredient Activated Protein C, which...

20060094651 - Formulations and methods of production of fgf-20: The present invention provides improved formulations comprising FGF-20, its fragments, derivatives, variants, homologs, analogs, or a combination thereof, and improved methods for production....

20060094649 - Hla-a1,-a2,-a3,-a24,-b7, and-b44 tumor associated antigen peptides and compositions: A peptide or composition comprising at least one epitope or analog from CEA, HER2/neu, MAGE2, MAGE3, or p53....

20060094652 - Hybrid polypeptides with selectable properties: The present invention relates generally to novel, selectable hybrid polypeptides useful as agents for the treatment and prevention of metabolic diseases and disorders which can be alleviated by control plasma glucose levels, insulin levels, and/or insulin secretion, such as diabetes and diabetes-related conditions. Such conditions and disorders include, but are...

20060094657 - Inhibiting development of microvessels within coronary or peripheral vessel walls for restenosis/atherosclerosis prevention or therapy: Disclosed and claimed are compositions and methods for therapy and/or prevention of restenosis and/or atherosclerosis. The compositions can include an agent for inhibiting VEGF and an agent for including vessel maturation; for instance, the soluble VEGF receptor and ang-1. Embodiments can include kits....

20060094656 - Method for fostering bone formation and preservation: A method of inducing bone formation in a subject in need of such inducement comprises the steps of mechanically inducing an increase in osteoblast activity in the subject and elevating blood concentration of at least one bone anabolic agent in the subject. The method steps may be performed in any...

20060094648 - Methods for treating or preventing ischemic injury: A therapeutic or prophylactic treatment method of myocardial ischemia, such as due to myocardial infarction, by administering erythropoietin, alone or in combination with other drugs, to a patient suffering from or at risk of cardiac injury, such as myocardial ischemia. The erythropoietin is administered in a concentration such that the...

20060094655 - Modified growth hormones: Provided are modified growth hormone polypeptides, nucleic acid molecules encoding modified growth hormone polypeptides and methods of generating modified growth hormone polypeptides. Also provided are methods of treatment using modified growth hormone polypeptides....

20060094654 - Neuroprotective complex for treatment of cerebral ischemia and injury: The invention provides a pharmaceutical composition useful in treating cerebral ischemia and cerebral injury. The pharmaceutical composition is also useful as a prophylactic treatment during surgical procedures wherein the potential for ischemic tissue damage is present. Also included in the invention is a method for preparing the pharmaceutical composition, as...

20060094653 - Pancreatic polypeptide family motifs and polypeptides comprising the same: The present invention relates to novel Pancreatic Polypeptide Family (“PPF”) polypeptides. The PPF polypeptides of the invention generally include at least two PPF motif, have at least 50% sequence identity to PYY (3-36) over its length and will generally retain, at least in part, a biological activity of a PP,...

20060094647 - Treatment of inflammatory bowel disease using growth factors: The present invention is based upon methods of treating inflammatory conditions in the intestinal tract of mammals using growth factor related polypeptides. Methods of using fibroblast growth factor-CX (FGF-CX) polynucleotide sequences and the FGF-CX polypeptides encoded by such nucleic acid sequences, or variants, fragments and homologs thereof, are claimed in...

20060094659 - Antagonist peptides to the c5a chemotactic function of vitamin d binding protein: It has been demonstrated that one of Vitamin D Binding Protein (DBP) biological functions is to enhance the chemotactic activity of C5a and C5a des Arg. The present invention has found that peptides having sequences that substantially correspond to a specific region in the N-terminal domain I of DBP can...

20060094658 - Method and compositions for the treatment of gastrointestinal disorders: Compositions and related methods for treating IBS and other gastrointestinal disorders and conditions (e.g., gastrointestinal motility disorders, functional gastrointestinal disorders, gastroesophageal reflux disease (GERD), duodenogastric reflux, Crohn's disease, ulcerative colitis, inflammatory bowel disease, functional heartburn, dyspepsia (including functional dyspepsia or nonulcer dyspepsia), gastroparesis, chronic intestinal pseudo-obstruction (or colonic pseudoobstruction), and...

20060094660 - Inhibitor of the shh signalling patway and a testosterone supressing agent for the treatment of cancer: A method of protecting a patient from possible adverse effects of a treatment involving inhibition of the SHH-signalling pathway in the patient, the method comprising suppressing testosterone or its effect in the patient. A method of treating a proliferative disease such as cancer in a patient the method comprising inhibiting...

20060094661 - Ny-eso-1 peptide analogs: Some embodiments relate to analogs of peptides corresponding to class I MHC-restricted T cell epitopes and methods for their generation. These analogs can contain amino acid substitutions at residues that directly interact with MHC molecules, and can confer improved, modified or useful immunologic properties. Additionally classes of analogs, in which...

20060094662 - Pharmaceutical compositions for sustained drug delivery: Sustained delivery formulations comprising a water-insoluble complex of a peptide and a plurality of ligands are disclosed. The formulations of the invention allow for loading of high concentrations of peptide in a small volume and for delivery of a pharmaceutically active peptide for prolonged periods, e.g., one month, after administration...

20060094663 - Interleukin-1 receptor antagonists, compositions, and methods of treatment: Peptides that are designed to inhibit the biological activity of the IL-1R type 1 receptor and inhibit IL-1R/IL-1RacP related cell signaling and biological activity are disclosed. Compositions comprising IL-1R antagonists of the present invention are useful in the treatment of IL-1 related diseases or conditions such as arthritis, rheumatoid arthritis,...

20060094664 - Deoxycholic acid derivatives for the treatment of acute dysfunctions of portal and hepatic venous circulation: Use of compounds and their salts of formula (I), as reported in the description, in the preparation of drugs for the treatment of acute dysfunctions of portal and hepatic venous circulation....

20060094665 - Pharmaceutical angiostatic dipeptide compositions and methods of use thereof: Disclosed are methods of inhibiting neovascularization in a subject by administering to the subject a pharmaceutical preparation of R′-Glu-Trp-R″....

20060094666 - Water-soluble chitosan-indole-3-propionic acid conjugates: Water-soluble chitosan-indole-3-propionic acid conjugates useful as active constituents in pharmaceutical as well as cosmeceutical and agricultural applications are described....

20060094667 - Glucopyranosyloxypyrazole derivatives and use thereof in medicines: (wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo (lower alkyl) group or a halogen...

20060094668 - Coadministration of tigecycline and digoxin: The invention pertains to treatment of bacterial infections with tigecycline and cardiac insufficiency with digoxin by coadministration to a human in need thereof....

20060094669 - Method for treating bacterial infections in horses or pigs with tilmicosin: The invention relates to methods of treating a bacterial infection in a horse or a pig. The method involves administering to the horse or pig a composition comprising (i) a salt made from tilmicosin and a lipophilic acid and (ii) a pharmaceutically acceptable solvent combined together to form an injectable...

20060094671 - Compositions of treating hepatitis virus infections with n-substituted-1,5-dideoxy-1,5-imino-d-glucitol compounds in combination therapy: Provided are methods and compositions for treating hepatitis virus infections in mammals, especially humans. The methods comprise (1) administering N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds in combination with nucleoside antiviral agents, nucleotide antiviral agents, mixtures thereof, or immunomodulating/immunostimulating agents, or (2) administering N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds in combination with nucleoside antiviral agents, nucleotide antiviral agents, or...

20060094670 - Inhibitors of adp-ribosyl transferases, cyclases, and hydrolases: wherein A is a nitrogen-, oxygen-, or sulfur-linked aryl, alkyl, cyclic, or heterocyclic group, the group being further substituted with an electron contributing moiety; B is hydrogen, or a halogen, amino, or thiol group; C is hydrogen, or a halogen, amino, or thiol group; and D is a primary alcohol,...

20060094674 - Combination of mtor inhibitor and a tyrosine kinase inhibitor for the treatment of neoplasms: The invention features methods and compositions including an mTOR inhibitor and a tyrosine kinase inhibitor for reducing the proliferation of and enhancing the apoptosis of neoplastic cells. The addition of an MEK inhibitor to this combination further enhances the effectiveness of this therapeutic method....

20060094676 - Compositions and methods for treating cancer using compositions comprising an inhibitor of endothelin receptor activity: Elevated ETRB activity, BCL-2A1 activity and/or PARP-3 activity was detected in cancer cells, and determined to be associated with growth and proliferation of the cancer cells. Accordingly, methods are provided for treating cancer by reducing or inhibiting the ETRB activity, BCL-2A1 activity and/or PARP-3 activity. Also provided are methods of...

20060094672 - Compositions and methods of use of targeting peptides against placenta and adipose tissues: The present invention concerns compositions comprising and methods of identification and use of targeting peptides for placenta or adipose tissue. In certain embodiments, the targeting peptides comprise part or all of SEQ ID NO:5-11, SEQ ID NO:13-22 OR SEQ ID NO:144. The peptides may be attached to various therapeutic agents...

20060094683 - Immunomodulatory oligonucleotides: Oligonucleotides containing unthylated CpG dinucleotides and therapeutic utilities based on their ability to stimulate an immune response in a subject are disclosed. Also disclosed are therapies for treating diseases associated with immune system activation that are initiated by unthylated CpG dinucleotides in a subject comprising administering to the subject oligonucleotides...

20060094680 - Immunostimulatory oligonucleotide multimers: The invention provides an immunostimulatory nucleic acid. In certain embodiments according to this aspect of the invention, the sequence of the immunostimulatory oligonucleotide and/or immunomer is at least partially self-complementary....

20060094681 - Immunostimulatory oligonucleotide multimers: The invention provides an immunostimulatory nucleic acid. In certain embodiments according to this aspect of the invention, the sequence of the immunostimulatory oligonucleotide and/or immunomer is at least partially self-complementary....

20060094677 - Inhibition of apoptosis-specific eif-5a (\"eif-5a1\") with antisense oligonucleotides and sirna as anti-inflammatory therapeutics: The present invention relates to apoptosis specific eucaryotic initiation factor 5A (eIF-5A), referred to as apoptosis-specific eIF-5A or eIF5A1, nucleic acids and polypeptides and methods for inhibiting or suppressing apoptosis in cells using antisense nucleotides or siRNAs to inhibit expression of apoptosis-specific eIF-5A. The invention also relates to suppressing or...

20060094682 - Kinase inhibitors for the treatment of diabetes and obesity: The present invention discloses a method of treating an individual or animal with diabetes and/or obesity. The method comprises administering to the individual or animal a therapeutically effective amount of a protein tyrosine kinase inhibitor. Preferably, the preventative and therapeutic methods of the present invention involve administering—to a mammal in...

20060094675 - Method for the repair of mutated rna from genetically defective dna and for the specific destruction of tumor cells by rna trans-splicing, and a method for the detection of naturally trans-spliced cellular rna: Methods and products for the repair of genetically defective DNA in the region of a mutated exon, for the specific destruction of tumor cells, and for the identification of naturally trans-spliced RNA. The methods inter alia are based on the utilization of cellular RNA splicing components....

20060094679 - Method of preventing or treating liver disease: An object of the present invention is to provide a method of preventing or treating liver disease, particularly non-alcoholic fatty liver disease, hepatic fibrosis, cirrhosis, or liver cancer. The present invention is directed to a method of preventing or treating liver disease comprising administering to a patient in need thereof...

20060094678 - Nuclease resistant double-stranded ribonucleic acid: This invention relates to modified double-stranded oligoribonucleic acid (dsRNA) having improved stability in cells and biological fluids, and methods of making and identifying dsRNA having improved stability, and of using the dsRNA to inhibit the expression or function of a target gene....

20060094673 - Polymer surfactants for gene therapy applications: A composition and method capable of delivering pharmaceutical or biomedical materials includes a tri-block surfactant having a hydrophilic block, a charged water-soluble block and a hydrophobic block....

20060094684 - Use of rapamycin to inhibit immune response and induce tolerance to gene therapy vector and encoded transgene products: Disclosed are methods for transient co-administration of rapamycin together with a gene therapy vector encoding a transgene. The present invention is directed to inhibiting the immune response of a host to the administered gene therapy vector and encoded trans gene product, thus allowing persistent trans gene expression and repeated administration...

20060094685 - Medicinal composition for drug-induced neuropathy: The present invention relates to an agent for the prophylaxis or treatment of drug-induced neuropathy, which contains cytidine 5′-diphosphocholine (CDP-choline) as an active ingredient. The agent for the prophylaxis or treatment of drug-induced neuropathy of the present invention shows a potent ameliorating effect on drug-induced neuropathy and is also superior...

20060094686 - Use of corrinoids for application in skin diseases: in which R stands for CN, OH, CH3 or H2O, for building up and improving the resistance of the skin is claimed. The compounds are suitable in particular for preventive treatment in cases of predisposition to chronic skin diseases, for the prevention and treatment of allergic skin reactions, for the...

20060094687 - Formulations: Ecteinascidin formulations, methods of preparing the same, articles of manufacture and kits with such formulations, and methods of treating proliferative diseases with the same formulations are provided....

20060094688 - Histamine release inhibitor: The present invention provides a histamine release inhibitor comprising a pectin or a salt thereof or a pectin hydrolysate as an active ingredient, and a pharmaceutical composition, a cosmetic, and food and drink comprising the inhibitor....

20060094689 - Production of fungal extracellular immune stimulating compounds: A process is described for the production of an immunostimulant by submerged cultivation of Lentinus edodes in which mycelium from agar plates or a fermentation broth is added to a liquid medium in a shake flask or a bioreactor containing nutrients such as malt extract, yeast extract, peptone and glucose...

20060094690 - Antimicrobial locking solutions comprising taurinamide derivatives and biologically acceptable salts and acids, with the addition of small concentrations of heparin: The present invention relates to inhibiting or preventing infection and protecting against patency complications after a blood catheter has been inserted in a patient comprising administering to the device a pharmaceutically effective amount of a composition comprising: (A) at least one taurinamide derivative, (B) at least one compound selected from...

20060094691 - Inclusion complexes of rosiglitazone: A host-guest complex, wherein the host is a cyclodextrin or a mixture of cyclodextrins (the Cyclodextrin) and the guest is 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione, (Compound (I)) or a pharmaceutically acceptable derivative thereof or a mixture thereof; a process for the preparation of said complex, a pharmaceutical composition comprising such complex and the use...

20060094692 - Pharmaceutical formulations of camptothecins and process for making same: This invention relates to pharmaceutically elegant formulations of highly lipophilic camptothecin derivatives....

20060094693 - Methods and compositions for treating glucose-associated conditions, metabolic syndrome, dyslipidemias and other conditions: The invention relates, in part, to of Glu-boroPro containing compounds and methods of use thereof in the prevention or management of conditions that are associated with impaired glucose tolerance such as diabetes. The invention also relates to compositions of Glu-boroPro containing compounds and methods of use thereof in the prevention...

20060094694 - Heterocyclic compounds and thrombopoietin receptor activators: wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X...

20060094695 - Hypoestoxides, derivatives and agonists thereof for use in the prophylaxis and treatment of obesity: Methods of treating a host suffering from obesity or an overweight condition are provided. Methods of preventing obesity or an overweight condition are also provided. The methods include delivery of a hypoestoxide, hypoestoxide derivative or hypoestoxide agonist, or hypoestes dried leaf powder to a host suffering from obesity or an...

20060094696 - Oestrogen derivatives as inhibitors of steroid sulphatase: The present invention provides a compound comprising a steroidal ring system and an optional group R1 selected from any one of —OH, a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein the D ring of the steroidal ring system is substituted by...

20060094697 - Methods of simultaneously treating ocular rosacea and acne rosacea: A method for simultaneously treating ocular rosacea and acne rosacea in a human in need thereof comprising administering systemically to said human a tetracycline compound in an amount that is effective to treat ocular rosacea and acne rosacea but has substantially no antibiotic activity....

20060094698 - Self-administered contraceptive injection of oily solution: The subject invention provides a pharmaceutical formulation in the form of an oily solution for injection to a subject comprising a contraceptively and/or therapeutically effective amount of a long-acting progestogen and a contraceptively and/or therapeutically effective amount of a long-acting androgen dissolved in a pharmaceutically acceptable oily medium wherein the...

20060094699 - Combination therapy using an 11beta-hydroxysteroid dehydrogenase type 1 inhibitor and a glucocorticoid receptor agonist to minimize the side effects associated with glucocorticoid receptor agonist therapy: Combination therapy comprising the administration of an 11β-hydroxysteroid dehydrogenase type 1 inhibitor and a glucocorticoid receptor agonist for treating some forms of cancer, diseases and disorders having inflammation as a component, and to minimize the side effects associated with glucorticoid receptor agonist therapy....

20060094700 - Heat sterilization of a steroid in the presence of phosphate: A process for sterilizing a water-insoluble steroid composition comprising heat sterilizing the steroid in the presence of phosphate is disclosed herein. Compositions related thereto are also disclosed....

20060094702 - 5-ht4 receptor antagonists: p

20060094701 - Use of beta-2 bronchodilator drugs: Improved use of selective β2 sympathomimetic bronchodilator drugs in the therapy of obstructive or inflammatory airways disease, e.g. asthma, comprises use in enantiomeric rather than conventional racemic form. The improved use reduces occurrence of side effect, e.g. exacerbation of basal disease status or compromise or deterioration of lung function....

20060094703 - Novel amorphous hydrate of a cephalosporin antibiotic: A process for the preparation of cefdinir of the formula (I) the said process comprising the steps of: i) condensing 7-amino-3-cephem-4-carboxylic acid of the formula (XII) wherein R1 is as defined above with compound of the formula (XIII) in the presence of a tertiary amine and an organic solvent, followed...

20060094704 - Treatment of premature ejaculation: This invention relates to the use of cyclic guanosine 3′,5′-monophosphate phosphodiesterase type five inhibitors, including in particular the compound sildenafil, for the treatment of premature ejaculation in patients with normal erectile function....

20060094705 - Quetiapine analogs and methods of use thereof: The invention relates to novel compounds and methods of using them for modulating sleep....

20060094706 - Pyrazolopyrimidines as protein kinase inhibitors: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention,...

20060094707 - Constrained compounds as cgrp-receptor antagonists: The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and...

20060094708 - Certain chemical entities, compositions, and methods: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed....

20060094709 - Methods for the treatment of bipolar disorder using carbamazepine: Carbamazepine, in extended release form, is useful in the treatment of patients suffering from bipolar disorder. In order to minimize the time it takes to reach efficacy, carbamazepine, in extended release form, can be administered to the patient at an initial daily dose which is then increased in daily increments...

20060094710 - Piperidine-pyridazones and phthalazones as pde4 inhibitors: The compounds of a certain formula 1, in which the given substituents have the meanings as indicated in the description, are novel effective PDE4 inhibitors....

20060094711 - 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents: e

20060094712 - New benzothiadiazine compounds:

20060094713 - New benzothiadiazine compounds:

20060094714 - Compounds and their use to treat diabetes and related disorders: The invention relates generally to compounds described herein. More specifically, the invention relates to compounds and pharmaceutical compositions containing such compounds. Methods of the invention comprise administration of a compound of the invention for the treatment of diabetes and related disorders....

20060094715 - 5-ht4 receptor antagonists for the treatment of heart failure: This invention provides the use of a 5-HT4 receptor antagonist in the manufacture of a medicament for treating or preventing heart failure. Particular heart disorders to be treated are selected from the group comprising chronic heart failure, congestive heart failure, chronic congestive heart failure and heart failure resulting from ischaemic...

20060094716 - 1-pyridin-4-yl-urea derivatives: The invention relates to novel 1-pyridin-4-yl urea derivatives and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use...

20060094717 - Indole, azaindole and related heterocyclic ureido and thioureido piperazine derivatives: e

20060094720 - Nk1 antagonists:

20060094718 - O-substituted hydroxyaryl derivatives: “A” represents an acyl group which may be substituted, (provided that unsubstituted acetyl group and unsubstituted acryloyl group are excluded,) or a C1 to C6 alkyl group which may be substituted, or A may bind to connecting group X to form a cyclic structure which may be substituted, “E” represents...

20060094719 - Tetralin histamine-3 receptor antagonists: as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by antagonizing histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound...

20060094721 - Sulfonamides as potassium channel blockers: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides sulfonamides, and compositions and methods utilizing sulfonamides that are useful in the treatment of diseases by blocking potassium channels associated...

20060094722 - Combination drug: The present invention provides pharmaceutical agents comprising a dipeptidyl peptidase IV (DPPIV) inhibitor and a biguanide agent in combination, which enhance the effects of active circulating glucagon-like peptide-1 (GLP-1) and/or active circulating glucagon-like peptide-2 (GLP-2)....

20060094723 - Composition comprising a pde4 inhibitor and a pde5 inhibitor: The invention relates to the combined administration of a PDE4 inhibitor and a PDE5 inhibitor for the treatment of a disease in which phosphodiesterase 4 (PDE4) and/or phosphodiesterase 5 (PDE5) is detrimental....

20060094724 - Fused furan compound: wherein Ring X is benzene, pyridine, or the like; Y is an optionally substituted amino, an optionally substituted cycloalkyl, an optionally substituted aryl, an optionally substituted saturated heterocyclic group, an optionally substituted unsaturated heterocyclic group; A is a single bond, lower alkylene, lower alkenylidene, lower alkenylene or an oxygen atom;...

20060094725 - N-heterocyclic derivatives as nos inhibitors: where m, n, p, A1, R1, R2, R3 and R4 are described herein, as well as other N-heterocyclic derivatives, are useful as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are...

20060094727 - Inhibitors of macrophase migration inhibitory factor and methods for identifying the same: e

20060094726 - Quinoline derivatives as nk-2 and nk-3 receptor antagonists:

20060094728 - Combination of a src kinase inhibitor and a bcr-abl inhibitor for the treatment of proliferative diseases: A combination and methods are disclosed which are useful for the treatment of cancer and/or leukemia....

20060094729 - N-(-3-methoxy-5-methylpyrazin-2-yl)-2-(4-'1,3,4-oxadiazol-2-yl!phenyl)pyridine-3 sulphonamide as an anticancer agent: The use of N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulphonamide, or a pharmaceutically acceptable salt thereof, in the treatment of cancer and/or pain in a warm blooded animal such as man is described....

20060094732 - Arylvinylazacycloalkane compounds and methods of preparation and use thereof: Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the...

20060094731 - New medicament: The present invention relates to the use of a compound of formula (1) wherein R1 is pyridyl or thiazolyl, any of which may optionally be substituted with C1-8alkyl or C2-8alkenyl: and a) R2 is methoxy and n is zero or one; or b) R2 is chlorine and n is zero...

20060094730 - Water-soluble thalidomine derivatives: Thalidomide derivative (I) and their bases or salts are new: where R represents CHR1NR2R3, CHR1NR4C(O)CHR5NR2R3, W or CHR5NR4C(O)W, where R1, R4 and R5 represent independently each other H, C1-4 alkyl, R2 is a C1-4 alkyl, R3 is a C1-4 alkyl, or R2 and R3 together represents 1,3-propylene, 1,4-butylene, 1,5-pentylene, 1,6-hexylene,...

20060094733 - Purine derivatives as liver x receptor agonists: The invention relates to methods for the treatment or prevention of an LXR mediated disease or condition, including cardiovascular disease and atherosclerosis, novel compounds for use in such methods and pharmaceutical compositions comprising compounds for use in such methods....

20060094734 - Composition and method for inducing alertness: An alertness inducing composition contains the active ingredients caffeine and taurine and various inert substances in a dry formulation. Caffeine and taurine are delivered in an oral formulation that obviates the need for ingesting significant quantities of liquid or sugar....

20060094735 - Compounds, compositions, and methods: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed....

20060094736 - Synthesis and antimalarial activity of pyrrolo[3,2-f]quinazoline-1,3-diamine derivatives: The invention relates to derivatives of pyrroloquinazolinediamine, more specifically derivatives of 7-(substituted)-7H-pyrrolo[3,2-F] quinazoline-1,3-diamines that are non-toxic and are also effective in the treatment of malaria, including P. falciparum and P. vivax strains. The derivatives are certain carbamate derivatives, succinimide derivatives, alkylcarboxamides derivatives and acetamide derivative, phthalimides, alkylamines and all other...

20060094737 - Novel uracil derivatives and medicinal use thereof: It is intended to provide an uracil derivative represented by the following general formula (I): (I) wherein X represents a group selected from among NHCO, NHCH2, CO, CONH and CH2NH; R1 represents hydrogen or optionally substituted C1-6 alkyl; R2 represents a group of the following general formula (II) or (III):...

20060094738 - Small molecules that replace or agonize p53 function: This invention provides a novel screening system for identifying p53 mimetics/agonists. Also provided are small organic molecules that act as effective p53 mimetics/agonists....

20060094739 - 3-aryl-3-hydroxy-2-methylenepropionic acid esters as fungicides: i

20060094740 - Polycyclic compounds as potent alpha2-adrenoceptor antagonists: wherein X, Z, R1 to R10, R15, R16, m, n, r and t are as defined in claim 1, or a pharmaceutically acceptable salt or ester thereof, useful as an alpha-2 antagonist. The compounds of formula I can be used for the treatment of diseases or conditions where antagonists of...

20060094741 - Remedies for neuropathic pain and model animals of neuropathic pain: (wherein R1, R2, R3, R4, R5, R6, R7, R8, A, and B have the same definitions as those described in the specification), and an animal model produced by administering (+)-4a-(3-hydroxyphenyl)-2-methyl-1,2,3,4,4a,5,12,12a-octohydro-trans-quinolino[2,3-g]isoquinoline. The present invention makes it possible to perform drug treatment for neuropathic pain. The therapeutic effect of a compound against...

20060094742 - Prostaglandin ep4 antagonists: h

20060094743 - Isoquinoline compounds and medicinal use thereof: The present invention relates to an isoquinoline compound represented by the following formula (I) or (II), an optically active form thereof, a pharmaceutically acceptable salt thereof, a water adduct thereof, a hydrate thereof and a solvate thereof, as well as an agent for the prophylaxis and/or treatment of a disease...

20060094744 - Pharmaceutical dosage forms of stable amorphous rapamycin like compounds: The present invention provides a pharmaceutical dosage form comprising stable amorphous rapamycin like compounds and a pharmaceutically acceptable excipient and methods of making the pharmaceutical dosage form....

20060094746 - Thieno[2,3-c] isoquinolines for use as inhibitors of parp: e

20060094745 - Use of an mtor inhibitor in treatment of uterine leiomyoma: The invention provides for the use of an mTOR inhibitor in the treatment or inhibition of fibroids....

20060094747 - Substituted carboxylic acids: which are useful in the treatment of metabolic disorders related to insulin resistance or hyperglycemia. These compounds include inhibitors of protein tyrosine phosphatase (PTP-1B) that are useful in the treatment of diabetes and other PTP-1B mediated diseases, such as cancer, neurodegenerative diseases and the like. The compounds of the invention...

20060094748 - Aryl sulfonic pyridoxines as antiplatelet agents: Aryl sulfonic pyridoxine compounds with antiplatelet aggregation characteristics for the treatment of cardiovascular and cardiovascular related disease, are described. The methods are directed to administering pharmaceutical compositions comprising aryl sulfonic pyridoxines....

20060094749 - Substituted pyridoxines as anti-platelet agents: Compounds with antiplatelet aggregation characteristics for the treatment of cardiovascular and cardiovascular related disease, are described. The methods are directed to administering pharmaceutical compositions comprising a pyridoxine analogue....

20060094750 - Sulfonyl benzimidazole derivatives: or a pharmaceutically acceptable salt thereof, wherein A, B, R1, R2 and R3 are each as described herein, and compositions containing such compounds, and the use of such compounds in the treatment of a condition mediated by CB2 receptor activity such as, but not limited to, inflammatory pain, nociceptive pain,...

20060094751 - Quinuclidine derivatives and pharmaceutical compositions containing the same: Carbamates of formula (I) or pharmaceutically acceptable salts thereof, including quaternary ammonium salts of formula (II) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as antagonists of M3 muscarinic receptors....

20060094752 - Substituted indolizines and derivatives as cns agents: r

20060094753 - Use of inhibitors of jun n-terminal kinases for the treatment of glaucomatous retinopathy and ocular diseases: Compositions and methods for the treatment of glaucoma and other ocular diseases are disclosed. The compositions and methods are particularly directed to the use inhibitors of Jun N-terminal kinases (JNK), such as SP600125 in the treatment of glaucoma and other ocular diseases....

20060094755 - Novel quinoline-based metal chelators as antiviral agents: wherein A or B are independently —CR7R8, or —CH(R9)CH(R10). X is hydrogen, C1-C10 alkyl; —OH, or —NR11R12. R1 to R12 are various substituents selected to optimize the physicochemical and biological properties such as enzyme binding, tissue penetration, lipophilicity, toxicity, bioavailability, and pharmacokinetics of compounds of Formula 13. R1 to R12...

20060094754 - Quinolines as allosteric enhancers of the gabab receptors: e

20060094756 - Substantially pure cilostazol and processes for making same: The present invention provides substantially pure cilostazol. The present invention also provides cilostazol particles that have reduced particle size....

20060094757 - Substantially pure cilostazol and processes for making same: The present invention provides substantially pure cilostazol. The present invention also provides cilostazol particles that have reduced particle size....

20060094758 - N-substituted piperidine derivatives as serotonin receptor agents: or a pharmaceutically acceptable salt, amide, ester, or prodrug thereof. Also disclosed are methods of inhibiting an activity of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Disclosed are...

20060094759 - Novel piperdine derivatives and their use as monoamine neurotransmitter re-uptake inhibitors: This invention relates to novel piperidine 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....

20060094760 - Composition, system and method of treatment of gastrointestinal disorders with nizatidine oral solution: An alcohol-free, oral solution of nizatidine treats gastric and intestinal disorders. Oral doses of solution, which are equivalent to 150 mg twice daily, or 300 mg once daily, pill form of conventional nizatidine are orally administered and have a bioequivalency greater than 70%. The oral solution allows a wider population...

20060094761 - Dual antiplatelet/anticoagulant pyridoxine analogs: Compounds with antiplatelet aggregation and anticoagulant characteristics for the treatment of cardiovascular, cerebrovascular, and cardiovascular related diseases and symptoms, are described. The methods are directed to administering pharmaceutical compositions comprising aryl sulfonic pyridoxine and/or substituted pyridoxine analogs....

20060094762 - Magnesium salt of imidazole derivative: Magnesium salts of rabeprazole, processes for preparing them, pharmaceutical compositions of the salts and their use in treatment or prevention of gastrointestinal ulcers are provided....

20060094763 - Polymorphic forms of 6-[2-(methylcarbomoyl) phenyl sulfanyl]-3-e-[2-(pyridin-2-yl)ethenyl]indazole: The present invention relates to novel polymorphic forms of 6-[2-(methylcarbamoyl)phenylsulfanyl]-3-E-[2-(pyridin-2-yl)ethenyl]indazole, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a hyperproliferative disorder or a mammalian disease condition mediated by protein kinase activity....

20060094764 - Cyanothiophenes, their preparation and their use in pharmaceutical compositions: e

20060094765 - Use of a sri and vitamin b6 for the treatment of neurological and mental disorders: The invention is concerned with a method of treating neurological and/or mental disorders that are associated with, or pathogenetically related to deficient serotonin neurotransmission. The invention relates to a method of treating depressive disorders, anxiety disorders, post-traumatic stress syndrome or premenstrual syndrome, said method comprising the administration of serotonin re-uptake...

20060094766 - Epothilone derivatives for the treatment of multiple myeloma: e

20060094767 - 2,3-dihydro-6-nitroimidazo[2,1-b]oxazoles:

20060094769 - Novel aminodicarboxylic acid derivatives having pharmaceutical properties:

20060094768 - Thiophene derivative ppar modulators: The present invention is directed to compounds represented by the following structural formula, Formula I: and stereoisomers, pharmaceutically acceptable salts, solvates and hydrates thereof, wherein: (a) X is selected from the group consisting of O, S, S(O)2, N, and a bond; (b) U is an aliphatic linker wherein one carbon...

20060094770 - 1,2 diarylbenzimidazoles and their pharmaceutical use: e

20060094771 - Carvedilol pharmasolve solvate: This invention relates to carvedilol pharmasolve solvate, compositions containing this compound and methods of using carvedilol pharmasolve solvate to treat hypertension, congestive heart failure and angina....

20060094772 - Method for detecting intracellular cholesterol: The present invention relates to a method of detecting intracellular cholesterol. The method provides contacting a permeabilized cell with labeled cθ complex. Methods of using this detection method to identify agents which modulate cholesterol accumulation in a cell are also provided....

20060094773 - 3-phenyl substituted 3-substituted-4ketolactams and ketolactones: e

20060094774 - Cannabinoid crystalline derivatives and process of cannabinoid purification: Δ9 tetrahydrocannabinol (THC) esters comprising the reaction product of THC with at least one aryl sulfonyl chloride in the presence of at least one tertiary amine. The resulting aryl sulfonic THC esters are highly crystalline and stable at room temperature in air, allowing for indefinite storage. The aryl sulfonic THC...

20060094775 - Remedy for corneal ulcer: The present invention provides a pharmaceutical agent capable of effectively treating corneal ulcer, more particularly, a therapeutic agent for corneal ulcer, which contains triptolide or a derivative thereof or a pharmaceutically acceptable salt thereof....

20060094776 - Insecticidal (dihalopropenyl) phenylalkyl substituted dihydrobenzofuran and dihydrobenzopyran derivatives: where the asterisk denotes attachment at A; and q, r, s, u, v and w are integers independently selected from 0, 1 and 2; and t is an integer selected from 0 and 1. A, D, E, G, M, R through R11, and R16 through R27, inclusively, are fully described...

20060094777 - Teat disinfectant having zinc edta, and methods: Compositions, systems, and methods for the prevention of mastitis in milk producing animals are provided. In particular, the compositions comprise zinc EDTA and chlorhexidine. The composition is applied to the teat of a milk producing animal such as a cow either by dipping the teat therein or spraying the composition...

20060094779 - Estrogen receptor modulators: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone...

20060094778 - Vesicant treatment with phenyl-phenyl 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, diphenyl compound with vitamin D receptor (VDR) modulating activity....

20060094780 - Novel antibiotic compounds: The present invention relates to the determination that a group of trinervitadiene compounds possess antimicobial activity. The invention provides pharmaceutical and/or veterinary formulations comprising these compounds, as well as methods for treating a microbial infection or disease, and methods for disinfecting a surface....

20060094781 - Method of treating extracellular matrix: A method for treating skin tissue or extracellular matrix in a body region. A precursor of a photosensitive compound is introduced into the body region. One or more enzymes converting the precursor to the photosensitive compound are then introduced into the body region so as to convert the precursor to...

20060094782 - Compositions and dosage forms for enhanced absorption: Disclosed is controlled delivery of pharmaceutical agents and methods, dosage forms and devices therefore. In particular, formulation, dosage forms, methods and devices for enhanced absorption and controlled delivery drug compounds are disclosed....

20060094783 - Use of r-enantiomer of n-propargyl-1-aminoindan, salts, compositions and uses thereof: The subject invention provides methods of treating a subject afflicted with Parkinson's disease, memory disorder, depression, hyperactive syndrome, Attention Deficit Disorder, dementia, brain ischemia, stroke, head trauma injury, spinal trauma injury, neurotrauma, neurodegenerative disease, neurotoxic injury, multiple sclerosis, nerve damage, affective illness, schizophrenia or symptoms of withdrawal from an addictive...

20060094784 - Tgf-alpha expression inhibitors: An inhibitor against TGF-α expression and an inhibitor against transformation of a hepatitis and/or cirrhosis cell which comprise as an active ingredient a polyprenyl compound such as a polyprenyl carboxylic acid (for example, 3,7,11,15-tetramethyl-2,4,6,10,14-hexadecapentaenoic acid). The inhibitor can be used as an inhibitor against onset, recurrence (second oncogenesis), and malignant...

20060094785 - Use of amino acids for treatment of various conditions: A method of treating a patient for a condition characterized by symptoms that can be alleviated by interfering with or supplementing the activity of endogenous ligands on the a2S subunit of a voltage gated calcium channel, said method comprising: administering to a patient experiencing the condition an amount of one...

20060094786 - Treating syndrome x with substituted tetralins and indanes: The invention features tetralin and indane compounds, compositions containing them, and methods of using them as PPAR alpha modulators to treat or inhibit the progression of, for example, diabetes....

20060094787 - Pharmaceutical composition comprising 5-methyl-2-2'(chloro-6'-fluoroanilino) phenylacetic acid: Provided are compositions comprising aqueous suspensions of 5-methyl-2-(2′-chloro-6′-fluoroanilino)phenylacetic acid suitable for oral administration. Methods for making such compositions and methods for their stabilization are provided....

20060094788 - Prostaglandin derivatives: o

20060094789 - Alpha- and beta-amino acid hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors: α- and β-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease....

20060094790 - Use of sphingosine kinase activator as skin disease treating agent and method for treating skin diseases using the same: Disclosed is a non-natural ceramide compound effective for a sphingosine kinase activator, and thus useful for a skin disease treating agent. The sphingosine kinase activator enhances production of sphingosine-1-phosphate to show various physiological activities provided by sphingosine-1-phosphate. The physiological activities include the effects of: controlling multiplication and differentiation of keratinocytes,...

20060094791 - Aminated polyamines: the polyamine, upon binding to the biological counter-anion in the cell, functions in a manner biologically different than the intracellular polyamines; and further wherein at least one of said bridging groups ALK1, ALK2 and ALK3 contains at least one —CH(NRH)— group which is not alpha- to either of the nitrogen...