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Drug, bio-affecting and body treating compositions September class, title,number 09/06

20060211599 - Reversibly heat-gelable aqueous composition: The present invention relates to a reversibly heat-gelable aqueous composition comprising a reversibly heat-gelable aqueous composition according to conventional technique, to which a thixotropic property-increasing substance is added. The thixotropic property-increasing substance is preferably at least one member selected from the group consisting of sugar alcohol, lactose, carmellose or pharmaceutically...

20060211600 - Stem cell-derived factors for treating pathologic conditions: Compositions and methods for cellular and tissue protection, repair, and regeneration are described. Mesenchymal cell-derived paracrine factors confer a therapeutic benefit to a variety of injured, compromised or diseased tissues such as myocardial tissue....

20060211601 - Nitrosated and nitrosylated heme proteins: Nitrosylation of proteins and amino acid groups enables selective regulation of protein function, and also endows the proteins and amino acids with additional smooth muscle relaxant and platelet inhibitory capabilities. Thus, the invention relates to novel compounds achieved by nitrosylation of protein thiols. Such compounds include: S-nitroso-heme proteins, S-nitroso-t-PA, S-nitroso-cathepsin;...

20060211602 - Use of alanyl aminopeptidase inhibitors and pharmaceutical compositions containing said inhibitors: The present invention relates to the use of one inhibitor or of several inhibitors of alanyl aminopeptidases and/or of enzymes having a similar substrate specificity for the induction of the production of TGF-β1 and of the expression of TGF-β1 in and/or on Treg cells and relates to the use for...

20060211604 - Methods for treating inflammatory disorders using regulators of microvessel dilations: The invention relates to methods for treating inflammatory diseases. Methods for analyzing microcirculation structural changes are also provided....

20060211605 - Mucosal repair by tff dimer peptides: The present invention relates to the use of trefoil factor 1 (TFF1) and trefoil factor 3 (TFF3) dimers and a pharmaceutical composition comprising TFF dimers for increasing the viscosity of mucin in mucus layers and the repair of damaged mucus layers in the gastrointestinal tract (mouth, oesophagus, stomach, small and...

20060211603 - Ramoplanin derivatives possessing antibacterial activity: Novel ramoplanin derivatives are disclosed. These ramoplanin derivatives exhibit antibacterial activity. As the compounds of the subject invention exhibit potent activities against gram positive bacteria, they are useful antimicrobial agents. Methods of synthesis and of use of the compounds are also disclosed....

20060211606 - Peptides: This invention relates to biologically active polypeptides derived from the E peptide that forms the C-terminus of the insulin-like growth factor I (IGF-I) splice variant known as mechano growth factor (MGF). These peptides are modified to improve their stability compared to the naturally occurring E peptide....

20060211607 - Somatostatin-dopamine chimeric analogs: Disclosed is a series of somatostatin-dopamine chimeric analogs which retain both somatostatin and dopamine activity in vivo. An example is: 6-n-propyl-8β-ergolinglmethylthioacetyl-D-Phe-c(Cys-Tyr-D-Trp-Lys-Abu-Cys)-Thr-NH2...

20060211612 - Angiogenesis using hepatocyte growth factor: Methods for enhancing angiogenesis in a mammal using hepatocyte growth factor (“HGF”) are provided. In the methods, HGF can be administered to mammals suffering from, for instance, vascular insufficiency or arterial occlusive disease. Articles of manufacture and kits containing HGF are also provided....

20060211621 - Combined use of factor vii polypeptides and factor ix polypeptides: The invention concerns a pharmaceutical preparation comprising a factor VII or factor VII-related polypeptide and a factor IX or factor IX-related polypeptide. The invention also concerns use of a factor VII or factor VII-related polypeptide and a factor IX or factor IX-related polypeptide for manufacture of a medicament for pharmaceutical...

20060211622 - Isolated human nuclear hormone receptors, nucleic acid molecules encoding human nuclear hormone receptors, and uses thereof: The present invention provides amino acid sequences of peptides that are encoded by genes within the human genome, the nuclear hormone receptor peptides of the present invention. The present invention specifically provides isolated peptide and nucleic acid molecules, methods of identifying orthologs and paralogs of the nuclear hormone receptor peptides,...

20060211614 - Methods of inhibiting angiogenesis with fragments and homologs of troponin subunit 1: The present invention relates to methods of inhibiting angiogenesis associated with a disease or disorder with peptides homologous to amino acid residues 130-137 or 132-139 of human troponin subunit I....

20060211613 - Methods useful in the treatment of bone resorption diseases: The invention relates to a combined pharmaceutical preparation comprising parathyroid hormone and a bone resorption inhibitor, said preparation being adapted for (a) the administration of parathyroid hormone during a period of approximately 6 to 24 months; (b) after the administration of parathyroid hormone has been terminated, the administration of a...

20060211617 - Methods, compositions and articles of manufacture for contributing to the treatment of solid tumors: Methods, compositions and articles of manufacture for contributing to the treatment of a solid cancerous tumor are disclosed. The methods, compositions and articles of manufacture can utilize an endothelin B agonist (ETB) to enhance the delivery of a chemotherapeutic agent to a solid tumor in mammals, including humans....

20060211619 - Multivalent clostridial toxin derivatives and methods of their use: The present invention is directed to multivalent Clostridial neurotoxin derivatives having more than one binding domain directed to a cell surface feature of a target cell. Such modified neurotoxins are useful as therapeutic compositions to prevent exocytosis and secretion by the target cell. Conditions in which such compositions man be...

20060211609 - Novel agent for improving neurotransmission failure: A novel medicament for ameliorating neurotransmission dysfunction diseases is provided. A medicament for ameliorating neurotransmission dysfunction diseases comprising as a main active ingredient preferably a selenocysteine-containing protein such as Selenoprotein P or a selenocysteine-containing peptide that consists of said protein or a series of said peptides. A medicament suited for...

20060211610 - Peptide yy analogs: The invention provides analogs of PYY. The invention also provides compositions and methods useful for controlling biological activities such as cell proliferation, nutrient transport, lipolysis, and intestinal water and electrolyte secretion....

20060211618 - Polynucleotides and polypeptides of the erythropoietin gene: The present invention relates to new polynucleotides deriving from the nucleotide sequence of the EPO gene and comprising new SNPs, new polypeptides derived from the natural EPO protein and comprising at least one mutation caused by the SNPs of the invention as well as their therapeutic uses....

20060211620 - Polypeptides having antimicrobial activity and polynucleotides encoding same: The present invention relates to isolated polypeptides having antimicrobial activity and isolated polynucleotides encoding the polypeptides. The invention also relates to nucleic acid constructs, vectors, and host cells comprising the polynucleotides as well as methods for producing and using the polypeptides....

20060211616 - Purification of glucagon-like peptides: Method for purifying a glucagon-like peptide by reversed phase high performance liquid chromatography...

20060211615 - Surfactant peptide nanostructures, and uses thereof: This work describes a new class of short polypeptides that can self-assemble to form regular nanotubes with an average diameters of about 50 nm. These peptides (7 to 8 amino acids) have a structure very similar to those observed in surfactant molecules with a defined hydrophilic head group constituting of...

20060211611 - Therapies and compositions for controlling the stress mechanism and for stabilizing hemostasis in an organism: A theory has been presented that provides a simplified explanation of a cohesive mechanism of embryological development, hemostasis, coagulation, wound repair and tissue maintenance that operates continuously in the animal body to oppose the effects of stress. The theory endeavors to fit all known facts, and is based on the...

20060211608 - Use of a parathyroid hormone peptide analogs for the treatment of viginal atrophy: The invention features methods for the treatment of vaginal atrophy by administering a parathyroid hormone peptide or peptide analog and formulations thereof....

20060211623 - Conopeptides: The invention relates to novel conopeptides and/or novel Luses of conopeptides. The conopeptides of the invention are analogs of α-Conotoxin MII that are selective for α6-containing nAChRs as described herein....

20060211624 - Methods and compositions for the treatment of parkinson's disease and other alpha-synucleinopathies: The present invention provides novel methods for the treatment of Parkinson's disease and other α-synucleinopathies. The methods of the invention include treatment with inhibitors of transglutaminase, which can inhibit aggregation of α-synuclein. Also provided are screening assays for novel inhibitors of transglutaminase which may be used in the treatment of...

20060211625 - New hybrid oligomers, their preparation process and pharmaceutical compositions containing them: The present invention relates to compositions and methods for producing therapeutic oligomeric compounds. In one aspect the invention relates to methods for administering the oligomeric compounds for the treatment and prevention of disease, for example, a fungal infection, bacterial infection, or cancer, in a mammal. In particular, the invention relates...

20060211626 - Peptides and peptidomimetics useful for inhibiting the activity of prostaglandin f2alpha receptor: The invention relates to compositions which are useful for inhibiting prostaglandin F2α receptor. The compositions include, but are not limited to, linear peptides, peptide analogs, and peptidomimetics. Methods of using the compositions of the invention to treat preterm labor and dysmenorrhea are disclosed....

20060211627 - Methods and compositions for derepression of iap-inhibited caspase: The invention provides isolated agents having novel chemical structures and possessing superior activity as derepressors of IAP inhibited caspase. The invention further provides a method of derepressing an IAP-inhibited caspase. The invention further provides assay methods employing labeled compounds of the invention, especially fluorescent labeled compounds....

20060211629 - Inhibitors of serine proteases, particularly hcv ns3-ns4a protease: The present invention relates to compounds of formula I or formula Ia or pharmaceutically acceptable salts thereof, that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are useful as...

20060211628 - Treatment of multiple sclerosis with brain targeted anti oxidant compounds: A method of treating multiple sclerosis, the method comprises administering to a subject in need thereof a therapeutically effective amount of a compound, the compound having: (a) a combination of molecular weight and membrane miscibility properties for permitting the compound to cross the blood brain barrier of the organism; (b)...

20060211630 - Novel synthetic compounds, processes of manufacture and uses in the treatment of integrin-mediated disorders: This invention relates to nitroproline derivative compounds and procedures for their preparation and the preparation of pharmaceutical compositions containing the compounds. The invention also relates to the administration of compounds of the invention as agents for the treatment of mammalian diseases whose pathogenic and pathophysiological mechanisms depend on or are...

20060211633 - D-mannose contraceptives: The present invention concerns the use of D-mannose to prevent or inhibit uniting of sperm and egg/zygote in the conception process, both for specific target animals as well as general animal populations. It is emphasized that this abstract is provided to comply with the rules requiring an abstract that will...

20060211632 - Pxr agonists for cardiovascular disease: A method of treating or preventing coronary artery disease in an animal includes increasing blood serum apoA1 level in the animal by administering an effective amount of an agonist of the orphan nuclear receptor PXR. A method of identifying a substance useful for treating or preventing coronary artery disease in...

20060211631 - Transfusion preparation for peripheral intravenous administration and method of stabilizing vitamin b1: The infusion preparation for peripheral parenteral administration comprises an infusion (A) containing glucose with 80 to 200 g/L concentration, and an infusion (B) containing amino acid with 50 to 150 g/L concentration. The infusion (A) and the infusion (B) are separately put into a vessel that is divided with an...

20060211634 - Inhibitors of aminoglycoside 6'-n-acetyltransferases, compositions and uses thereof: e

20060211635 - Purifications of pomegranate ellagitannins and their uses thereof: Compositions of purified and biologically active ellagitannins are provided by separation from pomegranate husk using a method of extraction and purification using a solid polymeric adsorbent and the uses of the said compounds...

20060211636 - Macrolide antibiotics: The present invention relates to 11,12 γ lactone ketolides of formula (I) wherein R, R1, R2, R3 are as defined herein and pharmaceutically acceptable salts and solvates thereof, to process for their preparation and their use in therapy or prophylaxis of systemic or topical bacterial infections in a human or...

20060211640 - Antisense modulation of farnesoid x receptor expression: Antisense compounds, compositions, and methods are provided for modulating the expression of Farnesoid X Receptor (FXR). The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding FXR. Methods of using these compounds for modulation of FXR expression and for treatment of diseases associated with expression of FXR...

20060211638 - Exon 1 ss of pdgf alpha gene and utilization thereof: By using an antisense nucleotide, a ribozyme, a maxizyme, or an RNAi constructed based on the nucleotide sequence of exon 1 beta of the PDGF receptor alpha gene, which is expressed in specific cancer cells, or a polypeptide containing a portion thereof, translation of an mRNA transcribed from exon 1...

20060211646 - Formulations with anti-tumour action: The use of defibrotide as an anti-tumour agent, alone or in combination with other active ingredients with anti-tumour action, is described....

20060211639 - Immunostimulatory nucleic acids and cancer medicament combination therapy for the treatment of cancer: The invention involves administration of an immunostimulatory nucleic acid in combination with a cancer medicament for the treatment or prevention of cancer in subjects. The combination of drugs are administered in synergistic amounts or in various dosages or at various time schedules. The invention also relates to kits and compositions...

20060211644 - Immunostimulatory oligonucleotides: The invention relates to a class of short CpG immunostimulatory oligonucleotides that are useful for stimulating an immune response. Preferably the short oligonucleotides are soft or semi-soft oligonucleotides....

20060211637 - Methods of down regulating target gene expression in vivo by introduction of interfering rna: Methods and compositions are provided for down regulation of target gene expression in vivo by RNA interference. The methods are useful for target discovery and validation of gene-based drug development, and for treatment of human diseases....

20060211641 - Modulation of immunostimulatory properties of oligonucleotide-based compounds by utilizing modified immunostimulatory dinucleotides: The invention relates to the therapeutic use of oligonucleotides as immunostimulatory agents in immunotherapy applications. More particularly, the invention provides immunomers and an immunostimulatory oligonucleotides for use in methods for generating an immune response or for treating a patient in need of immunostimulation. The immunomers and an immunostimulatory oligonucleotides of...

20060211645 - Modulation of neurodegenerative diseases: Methods and compositions are disclosed for selectively interfering with protein synthesis in a central nervous system, meningial, or muscle cell by administrating a pharmacological agent. In particular, methods and compositions that interfere with SOD-1 protein synthesis are disclosed....

20060211647 - Nonviral vectors for delivering polynucleotides: Methods and compositions for delivering polynucleotides are provided. One embodiment provides a non-viral vector comprising a recombinant polynucleotide-binding protein comprising a protein transduction domain operably linked to a targeting signal. Methods for modifying the genome of non-nuclear organelles are also provided....

20060211643 - Polycations capable of forming complexes with nucleic acids: A polycation capable of forming a complex with a nucleic acid for carriage thereof. The polycation comprising at least one cyclic compound having a cavity. A polymer backbone is threaded into the cavity of the cyclic compound. A pair of bulky moieties cap the terminals of the polymer backbone to...

20060211642 - Rna inteference mediated inhibition of hepatitis c virus (hvc) gene expression using short interfering nucleic acid (sina): This invention relates to compounds, compositions, and methods useful for modulating Hepatitis C Virus (HCV) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of HCV gene expression...

20060211648 - Naphthalimide compositions and uses thereof: A method of treatment of a host with a cellular proliferative disease, comprising contacting the host with a naphthalimide and an antiproliferative agent, each in an amount sufficient to modulate said cellular proliferative disease, is described. In some embodiments, the naphthalimide comprises amonafide (5-amino-2-[2-(dimethylamine)ethyl]-1H-benz[de-]isoquinoline-1,3-(2H)-dione). Antiproliferative agents of the invention comprise...

20060211649 - Use of cytisine for enhancing physical performance: A method of decreasing fat and adipose tissue, and increasing endurance and alertness in humans comprises administering cytisine in a daily dosage between about 0.1 and 8 mg. Cytisine may be administered once per day or in multiple doses, either alone or in combination with other compounds and mixtures....

20060211650 - Reducing carbohydrate derivatives of adamantane amines, and synthesis and methods of use thereof: The present invention relates to reducing carbohydrate derivatives of adamantane amines of Formula A or pharmaceutically acceptable salts, solvates or derivatives thereof, wherein R1, R2, R3, and R4 are together or separately H, F, methyl or lower alkyl, alkenyl, or alkynyl groups, and Z is derived from a mono-, di-,...

20060211652 - Method of making a partially hydrolyzed fucoidan composition: Methods of making partially hydrolyzed fucoidan. Fucoidan from brown seaweeds is partially hydrolyzed and then mixed with other ingredients for use as a dietary supplement in beverage, capsule, or tablet form. The fucoidan is partially hydrolyzed with acid and heat. The partially hydrolyzed fucoidan can also be sulfonated. Other ingredients...

20060211651 - Persulfated oligosaccharide acting on selectins and chemokine: A persulfated saccharide compound capable of acting on selectin and chemokine. According to the present invention, there are provided a saccharide compound capable of interacting with L-selectin, P-selectin and chemokine; a pharmaceutical composition; and an agent for treating or preventing a disease of which sideration is associated with biological events...

20060211653 - Pharmaceutical compositions comprising aloe pectins, and methods for their production and use: Pectins having a combination of unexpectedly high molecular weights and low degrees of methylation have been isolated from Aloe vera plants, are superior gel pectins for forming calcium cross-lined gels. Such pectins can be obtained by extracting homogenized Aloe Vera plants or portions thereof. These pectins can be used to...

20060211654 - Pharmaceutical compositions of cholesteryl ester transfer protein inhibitor: A pharmaceutical composition comprises a solid amorphous dispersion of a cholesteryl ester transfer protein inhibitor and a concentration-enhancing polymer....

20060211655 - Repellent: The present invention relates to the use of an arthropod-repelling component from the pyrethroid/pyrethrin class in combination with an agonist of the nicotinergic acetylcholine receptors of arthropods for repelling arthropods, preferably on animals, in an effective and sustainable manner....

20060211656 - Aminopropanol derivatives as sphingosine-1-phosphate receptor modulators: e

20060211657 - Prodrugs of 2,4-pyrimidinediamine compounds and their uses: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications....

20060211658 - Amino-propanol derivatives as sphingosine-1-phosphate receptor modulator: e

20060211659 - Novel compounds of the n-acylamino amide family, compositions comprising them and uses thereof: The invention concerns novel compounds of the N-acylamino-amide family, compositions, in particular cosmetic or pharmaceutical, containing them, and their use for treating body or face skin ageing, whether chronobiologic or light-induced, and in particular skin ageing caused by decrease of skin elasticity and/or by collagen degradation in the structure of...

20060211660 - Combination therapy for topical application in the treatment of dry eye syndrome: A topical ophthalmic composition comprising 17-β-estradiol or its derivatives and an androgen in pharmaceutically acceptable vehicle, and method of using same for the alleviation of kerato-conjunctivitis sicca KCS (dry eye syndrome DES)....

20060211661 - 24 hydroxyvitamin d, analogs and uses thereof: The invention provides 24-hydroxyvitamin D compounds and methods for their use in the treatment and prophylaxis of hyperparathyroidism and hyperproliferative diseases, and in the modulation of the immune and inflammatory responses as well as the treatment of bone depletive disorders....

20060211662 - Combination therapy for topical application in the treatment of age-related macular degeneration and ocular hypertension: A topical drug composition for the treatment of age-related maculopathy, age-rlated macular degeneration, ocular hypertension, glaucoma or other eye disease resulting from increased intraocular pressure comprising a solution of anabolic androgenic agent and 17-β-estradiol suspended or dissolved in a suitable ophthalmic vehicle is disclosed. In the preferred embodiment, 17-β-estradiol, or...

20060211663 - Low dose estrogen interrupted hormone replacement therapy: A hormone replacement therapy, comprising a plurality of daily doses of a pharmaceutical preparation, the doses being administered continuously and consecutively in alternating phases of three daily doses, a relatively dominant estrogenic activity phase comprising three daily doses of a substance exhibiting estrogenic activity equivalent to about 1 mg per...

20060211666 - 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole and estrogen formulations: The present invention relates to new formulations containing one or more estrogens and 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures below:...

20060211664 - Method for treating erectile dysfunction and increasing libido in men: The present invention relates to a transdermal hydroalcoholic testosterone gel formulation that overcomes the problems associated with other testosterone delivery mechanisms by providing, among other things, a desirable pharmacokinetic hormone profile with little or no skin irritation. In addition, the gel is used in conjunction with pharmaceuticals aimed at treating...

20060211665 - Reduction of postoperative pain medication: A procedure for reducing the pain from orthopedic surgery, such as hip or knee replacement by injecting a mixture of components into the site of trauma (surgical incision or tissue twisting/stretching) before closing the wound. The mixture includes a local anesthetic agent, epinephrine, morphine and a corticosteroid....

20060211667 - Use of pregnane steroid derivatives for enhancing physical performance: wherein R1=H and R2=H, or R1 and R2 combined form a single bond; R3 is one of OH and O; R5 is one of an α-hydrogen and a β-hydrogen; R6 is one of α-methyl and H; R7 is one of α-methyl and H; R17 is one of H and OH;...

20060211668 - Use of ciclesonide for the treatment of inflammatory bowel diseases: The invention relates to the novel use of ciclesonide in the treatment of inflammatory bowel disease....

20060211670 - Antitumoral18a-homoestra-1,3,5(10)-trien-3yl 2-substituted sulfamates: The invention relates to the use of compounds of a general formula (I), wherein R2, R14 to R17 and X groups have the following significance: R2 is C1-C5-Alkyl, C1-C5-Alkoxy or a —O—C<SB>N</SB>FmHo rest, wherein n=1,2,3,4,5 or 6, m>1 and m+o=2n+1, R14 and R15 separately designate hydrogen or together a methyl...

20060211671 - Estrogen receptors: This invention relates to the field of estrogen receptors and particularly though not exclusively on the effect of estrogen receptors and ligands for estrogen receptors on the prevention or treatment of obesity. The invention also relates to the effect of estrogen receptors and their ligands on lipoprotein levels in mammals....

20060211673 - Modulation of neurodegenerative diseases through the estrogen receptor: Methods for modulating hormonal pathways involving the estrogen receptor in a subject with a neurodegenerative disorder, are provided. Estrogen receptor activity is modulated by administering an effective amount of an estrogen receptor modulating pharmacological agent to a subject such that the estrogen receptor modulating pharmacological agent interacts with the estrogen...

20060211669 - Synthesis of estetrol via estrone derived steroids: A process is provided for the making of estetrol starting from a 3-A-oxy-estra 1,3,5(10),15-tetraen-17-one, wherein A is a C1-C5 alkyl group, preferably a methyl group, or a C7-C12 benzylic group, preferably a benzyl group. This process is particularly suitable to industry....

20060211672 - Use of estrogen receptor-beta selective agonists for radiation-or chemotherapy-induced mucositis and radiation cystitis: The present invention provides a method of treating or inhibiting mucositis or radiation cystitis using an ERβ selective ligand. The present invention also provides compositions, including pharmaceutical compositions, containing the ERβ selective ligand and a traditional medicament for mucositis or radiation cystitis....

20060211674 - Combination comprising a vasculostatic compound and an alkylating agent for the treatment of a tumor: The invention relates to a pharmaceutical combination which comprises (a) a vasculostatic compound, (b) an alkylating agent and (c) optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use for the treatment of a tumor disease; a pharmaceutical composition comprising such a combination; the use of such...

20060211675 - Preventives/remedies for urinary disturbance: Preventives/remedies for voiding disturbance containing a compound having both of an acetylcholinesterase inhibitory action and an al antagonistic action which exhibits an excellent effect of improving the urinary function of the bladder (i.e., effects of improving urine flow rate and voiding efficiency) without affecting the urinary pressure or the blood...

20060211676 - Crystalline anhydrous cefdinir and crystalline cefdinir hydrates: A novel crystalline cefdinir anhydrate and novel crystalline cefdinir hydrates, ways to make them and use them, compositions comprising them and made with them, and methods of treatment using them are disclosed....

20060211678 - Aryl-amino substituted pyrrolopyrimidine multi-kinase inhibiting compounds: or stereoisomers or pharmaceutically acceptable salts thereof, are inhibitors of least two of the Abl, Aurora-A, Blk, c-Raf, cSRC, Src, PRK2, FGFR3, Flt3, Lck, Mek1, PDK-1, GSK3β, EGFR, p70S6K, BMX, SGK, CaMKII, Tie-2, IGF-1R, Ron, Ret, and KDR kinases in animals, including humans, for the treatment and/or prevention of various...

20060211677 - Diphenyl substituted cycloalkanes, compositions containing such compounds and methods of use: The instant invention provides compounds of formula: (I) which are 5-lipoxygenase activating protein inhibitors: formula (I). Compounds of formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cyto-protective agents....

20060211679 - Substituted lactams as inhibitors of abeta protein production: having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the...

20060211680 - Cinnamoyl compound and use of the same: The present invention relates to a cinnamoyl compound represented by the formula (I):...

20060211681 - Adenosine deaminase inhibitor and novel bacillus sp. iada-7 strain which produces it: The present invention relates to an adenosine deaminase inhibitor and a novel Bacillus sp. strain which produces it. Particularly, the present 5 invention relates to the adenosine deaminase inhibitor, and the novel Bacillus sp. IADA-7 producing the above adenosine deaminase inhibitor. The adenosine deaminase inhibitor of the present Invention shows...

20060211683 - Erastin and erastin binding proteins, and uses thereof: The invention relates to methods of screening for binding partners, especially binding partners essential for the biological activity of erastin (e.g. VDACs such as VDAC3). The invention also provides reagents and methods for effective killing of cancer cells with erastin and related compounds or derivatives....

20060211682 - Hexahydrodiazepinones as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes: The present invention is directed to hexahydrodiazepinone compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-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...

20060211686 - Alpha7 neuronal nicotinic receptor ligand and antipsychotic compositions: The present invention relates to a composition comprising an antipsychotic and an α7 nicotinic acetylcholine receptor ligand, a method of using the same, and a related article of manufacture....

20060211685 - Pharmaceutical compositions for the treatment and/or prevention of depression: The invention relates to new pharmaceutical compositions for the treatment and/or prevention of depression and methods for the preparation thereof. In a preferred embodiment, the instant invention is directed to pharmaceutical combinations comprising flibanserin as one active ingredient in combination with at least one additional active ingredient for the treatment...

20060211684 - Use of alpha-2 adrenergic receptor agonists: The present invention provides a strategy to compensate for deficiency in the alpha-2C receptor by administering an agonist of different receptors; the alpha-2A and/or dopamine d2 receptors. These receptors are fully functional and receptive to stimulation by an agonist. Agonism of the alpha-2A and/or dopamine d2 receptors by clonidine, Nolomirole...

20060211687 - Potassium salt of an hiv integrase inhibitor: A potassium salt of Compound A is disclosed, wherein Compound A is of formula (1): Compound A is an integrase inhibitor useful for preventing or treating HIV infection, for delaying the onset of AIDS, and for treating AIDS....

20060211688 - Vehicle for topical delivery of anti-inflammatory compounds: A vehicle for topical delivery which contains a liquid eutectic mixture of hydrophobic compounds....

20060211689 - Aminoquinoline derivatives and their use as adenosine a3 ligands: The present invention relates to an adenosine A3 receptor ligand of the general formula (I), within those preferably to the antagonists, including a salt, solvate or isomer (tautomer, desmotrop, and optically active isomer) thereof, to a pharmaceutical composition containing the ligand, to the use of the ligand, to its preparation,...

20060211690 - Microglia inhibitors for interrupting interleukin 12 and ifngamma-mediated immune reactions: The invention describes the use of microglia inhibitors for the production of pharmaceutical agents that inhibit immune reactions that are mediated by monocytes, macrophages and T cells, and their use for treating T-cell-mediated immunological diseases and non-T-cell-mediated inflammation reactions....

20060211691 - Use of 2h-[1,3]-oxazino[3,2-a] indole derivatives for the treatment of neuropathic pain: Use of a compound of formula (I), wherein R is H, a linear or branched alkyl chain having from 1 to 12 carbon atoms or an arylalkyl group, and of the acid addition salts thereof with pharmaceutically acceptable organic or inorganic acids, to prepare a pharmaceutical composition active in the...

20060211692 - Method for the production of pyrrolidine-1,2-dicarboxylic acid-1-(phenyl(-amide))-2-(phenyl(-amide)) derivatives and 1-(phenylcarbamoyl)-pyrrolidine-2-carboxylic acid derivatives as intermediate products: Process for the preparation of compounds of the formula I in which R, R1, R2 and R3 are as defined in Patent claim 1, and compounds of the formula IV in which R and R1 are as defined in Patent claim 1, are intermediates for the preparation of the compounds...

20060211693 - Cis-imidazolines: o

20060211694 - Diaryl substituted pyridinones: and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using...

20060211695 - Fused heterocyclic kinase inhibitors: d

20060211696 - Imidazo[1,2-b]pyridazine compound: Wherein R1 denotes a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group and the like; R2 denotes a halogen atom, a cyano group, a nitro group, a C1-10 alkyl group, a C2-10 alkenyl group, C2-10 alkynyl group and the like; R3 denotes a C6-14 aromatic hydrocarbon cyclic group...

20060211697 - 2-(2 or 4-substituted aryloxy)-phenol derivatives as antibacterial agents: Antimicrobial compounds, compositions and methods of treatment administering same, of 2-aryloxyphenol derivatives having a heterocyclic or polar functional substitution attached through a N—C or C—C bond at the position para or ortho relative to oxygen bridge on non-phenolic phenyl ring, as well as methods for their preparation and formation, wherein...

20060211698 - Bicyclic heteroaryl derivatives for treating viruses: Disclosed are compounds having formula I and related compositions and methods thereof. The compounds are useful for treating viral infections caused by the Flaviviridae family of viruses....

20060211699 - Quinoxaline dihydrohalide dihydrates and synthetic methods therefor: Crystalline polymorph forms of Gonadotropin Releasing Hormone receptor antagonists, including crystalline polymorphs of quinoxaline dihydrohalide dihydrates, in particular crystalline polymorphs of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]-piperazin-1-yl}methyl)-quinoxaline dihydrochloride dihydrate, methods of making the same, as well as pharmaceutical compositions, and dosage forms containing them are disclosed....

20060211700 - (r)-8,9-dichloro-2,3,4,4a-tetrahydro-1h,6h-pyrazino[1,2-a]quinoxalin-5-one for controlling iop and treating glaucoma: Compositions and methods for controlling intraocular pressure and treating glaucoma using (R)-8,9-dichloro-2,3,4,4a-tetrahydro-1H,6H-pyrazino[1,2-a]quinoxalin-5-one are disclosed....

20060211702 - Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors: n, R1, R2, R3, R4, L1, L2, Y and Z are as defined in classes and subclasses herein, and pharmaceutical compositions thereof, as described generally and in subclasses herein, which compounds are useful as inhibitors of protein kinase (e.g., RAF), and thus are useful, for example, for the treatment of...

20060211701 - Use of von tetrahydrobiopterine derivatives in the treatment and nutrition of patients with amino acid metabolic disorders: The use of tetrahydrobiopterine and the derivatives thereof in the production of a medicament to improve protein tolerance for the treatment of diseases arising from an amino acid metabolic disorder, e.g. hyperphenylalaninemia. The invention also relates to a composition which contains tetrahydrobiopterine or derivatives thereof in addition to a special...

20060211703 - Substituted alkyl-pyridazinones for the treatment of memory and learning malfunctions: The compounds of the general Formula I, wherein R1 stands for hydrogen or lower alkyl; one of symbols X and Y stands for hydrogen or halogen and the other represents a group of the general Formula II, R2 is hydrogen or lower alkyl; n is 1, 2 or 3; R3...

20060211704 - 2,4-disubstituted thiazolyl derivatives: wherein X and Y each independently are O, NR3, CH2 or S, with R3 being hydrogen or C1-4alkyl; q is 1 to 4; Z is O or NR4 with R4 being hydrogen or C1-4alkyl; r is 1 to 3; L is optionally substituted phenyl or L is Het with Het...

20060211705 - 'n-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamides metabolites: The present invention is directed to metabolites of ′N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide, the compound of formula (I), pharmaceutical compositions thereof, and to methods of using the metabolites and the pharmaceutical compositions in the treatment of oncological and immunological disorders....

20060211706 - Farnesyl protein transferase inhibitors and methods for treating proliferative diseases: e

20060211707 - Piperazine-alkyl-ureido derivatives: The invention relates to novel piperazine 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 as...

20060211708 - Ziprasidone free from colored impurities and a process for its preparation: Ziprasidone base or a pharmaceutically acceptable salt thereof free from colored impurities, in particular those giving the product a “slightly pink to pink” coloration....

20060211709 - Protein kinase modulators and methods of use: Substituted aryl 1,4-pyrazine derivatives and their use in treating anxiety disorders, depression and stress related disorders are disclosed....

20060211710 - Substituted aryl 1,4-pyrazine derivatives: The invention is directed to compounds of Formula I, described herein, as well as pharmaceutically acceptable salts thereof, which act as CRF1 antagonists and are useful in the treatment of disorders and diseases associated with CRF1 receptors, including CNS-related disorders and diseases....

20060211711 - 7-(alkinylamino)-triazolopyrimidines, methods for the production and use thereof to combat harmful fungi and agents containing said compounds: 7-alkinylamino-triazolopyrimidins of formula (I), wherein the substituents have the following meanings: L=halogen, alkyl, halogenalkyl, alkoxy, amino, NHR, NR2, cyano, S(O)nA1 or C(O)A2; R=alkyl or alkylcarbonyl, A1=hydrogen, hydroxy, alkyl, alkylamino or aialkylamino; n=0, 1 or 2; A2=alkenyl, alkoxy, halogenalkoxy or one of the groups cited in A1; m=1, 2, 3, 4...

20060211712 - Bicyclic anilide spirohydantoin cgrp receptor antagonists: that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in...

20060211713 - Compounds having selective hydrolytic potentials: Disclosed are compounds having selective hydrolytic potential. The disclosed compounds are useful as compounds having selective stability and are capable of undergoing programmed hydrolysis in biologic systems....

20060211714 - Quinazoline derivatives and their use in the treatment of cancer: The invention concerns quinazoline derivatives of the formula: (I); wherein X1, Q1, Z, R1, R2, Y, a and m are as defined in the description, which are erbB tyrosine kinase inhibitors, particularly EGFR tyrosine kinase inhibitors. Also claimed are processes for their preparation; pharmaceutical compositions containing them; and their use...

20060211717 - Quinoline and quinazoline derivatives and drugs containing the same: wherein R1 and R2 represent hydrogen, alkyl or the like; R3, R4, R5, and R6 represent hydrogen, halogen, alkyl, alkoxy or the like; R11 and R12 represent hydrogen, alkyl, alkylcarbonyl or the like; and A represents any one of formulae (i) to (x), provided that compounds wherein R3, R4, R5...

20060211716 - (3,4-dihydro-quinazolin-2-yl)-aryl-amines: e

20060211715 - Quinazoline protein tyrosine phosphatase inhibitors: wherein X is an unsubstituted or substituted phenyl, or is an unsubstituted or substituted 5 or 6 membered heteroaromatic ring. The compounds of the present invention are potent inhibitors of PTP1B. Accordingly, the invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity,...

20060211718 - Deazaflavin compounds and methods of use thereof: The present invention features 5-deazaflavin compounds, pharmaceutical compositions of 5-deazaflavin compounds and methods of treating a patient suffering from cancer, the method comprising administering to a patient one or more 5-deazaflavin compounds of the invention....

20060211719 - Heteroaryl aminoguanidine and alkoxyguanidines and their use as protease inhibitors: wherein X is O or NR9 and Het, R1, R7, R8, R12-R15, Ra, Rb, Rc, Z, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The...

20060211720 - Heterocyclic compounds as inhibitors of factor viia: The present invention relates generally to compounds that inhibit serine proteases. In particular it is directed to novel heterocyclic compounds, or a stereoisomer or pharmaceutically acceptable salt, solvate, or prodrug form thereof, which are useful as selective inhibitors of serine protease enzymes of the coagulation cascade; for example thrombin, factor...

20060211721 - Nutraceutical formulation of a cognitive enhancement system: A nutraceutical composition and method of use thereof includes core ingredients, huperzine A, dimethylaminoethanol (DMAE), thiamin, niacin, and pantothenic acid. The core ingredients provide a synergistic effect to improve and support cognitive function, such as learning, thinking, and judging and to promote alertness, awareness, attention and mental clarity. Combinations of...

20060211722 - Amino cyclobutylamide modulators of chemokine receptor activity: The present invention is directed to compounds of the formulas I and II: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R25, R26, Y, Z, l, m, n and the broken lines are as defined herein which are useful as modulators of...

20060211723 - Aporphine and oxoaporphine compounds and pharmaceutical use thereof: The invention provides aporphine and oxoaporphine compounds that may be used to manufacture a medicaments for preventing or treating vascular dysfunctions that may result in ischemic and metabolic diseases or preventing complications associated with these diseases in human and mammal. The ischemic diseases may include ischemic cerebral apoplexy, ischemic cerebral...

20060211726 - Ascomycin derivatives for combination treatment with tazorotene: A method is disclosed herein comprising administering a therapeutically effective amount of an ascomycin derivative topically in combination with tazarotene, wherein said method is effective in reducing adverse events associated with tazarotene. A method is also disclosed herein comprising administering a therapeutically effective amount of an ascomycin derivative topically in...

20060211724 - Hiv integrase inhibitors: The present invention concerns the compounds having the formula (1), N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof wherein (a) or (b); A, together with the two carbons of the phenyl ring to which it is attached forms a monocyclic aryl or a monocyclic Het2; R1 is...

20060211725 - Use: This invention relates to a new use of a compound of the following formula (I) or (II) for the manufacture of a medicament for preventing and/or treating chronic rejection in a transplanted organ or tissue....

20060211727 - Novel compounds: Novel substituted 1,5,7-trisubstituted-1,8-napthyridin-2(1H)-one compounds; 1,5,7 trisubstituted-1,6-napthyridine-2-(1H)-one compounds and 1,5,7-trisubstituted quinoline-2(1H)-one compounds, processes for the preparation thereof, the use thereof in treating CSBP/p38 kinase mediated diseases and pharmaceutical compositions for use in such therapy....

20060211728 - Thalidomide analogs: Thalidomide analogs that modulate tumor necrosis factor alpha (TNF-α) activity and angiogenesis are disclosed. In particularly disclosed embodiments, the thalidomide analogs are isosteric sulfur-containing analogs. Also disclosed are methods of treating a subject with the analogs....

20060211729 - Combination of anticholinergics and leukotriene receptor antagonists for the treatment of respiratory diseases: Pharmaceutical compositions comprising an anticholinergic and at least one leukotriene inhibitor for treatment of respiratory diseases, including allergic rhinitis, bronchial asthma, COPD and common cold, and methods of treatment....

20060211730 - Beta-sulfonamide hydroxamic acid inhibitors of tace/matrix metalloproteinase: that are useful in treating diseases or disorders mediated by TNF-α, such as arthritis (rheumatoid arthritis (RA), juvenile RA, psoriatic arthritis, osteoarthritis etc), tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection, ankylosing spondylitis, psoriasis, sepsis, multiple sclerosis, Crohn's disease, degenerative cartilage...

20060211731 - New substituted pyridine or piperidine compounds: a

20060211732 - Hydroxamic acid derivatives as antibacterials: A method for the treatment of bacterial infections in humans and non-human mammals, which comprises inhibiting bacterial growth by administering to a subject an antibacterially effective dose of a compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof:...

20060211733 - Methods of preventing and treating opioid bowel dysfunction: Methods of preventing and treating opioid bowel dysfunction are disclosed. In addition, methods of increasing the frequency of spontaneous complete bowel movements, methods for improving the quality of life of a patient suffering from opioid bowel dysfunction, methods for reducing a patient's dependence on laxatives, and methods for preventing or...

20060211734 - (piperidinyloxy)phenyl, (piperidinyloxy)pyridinyl, (piperidinylsulfanyl)phenyl and (piperidinylsulfanyl)pyridinyl compounds as 5-ht1f agonists: The present invention relates to compounds of formula 1: and pharmaceutically acceptable acid addition sails thereof. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or preverition of migraine in mammals, particularly humans....

20060211735 - 4-arylsulphonylpiperidine derivatives for antagonism of the 5-ht2a receptor: Compounds of formula (I): are selective antagonists of the 5-HT2A receptor, and hence are useful in treatment of adverse conditions at the central nervous system, such as sleep disorders and schizophrenia....

20060211736 - Glutarimide-containing polyketide analogs and methods thereof: The present invention provides library of glutarimide-containing polyketide analogs, such as analogs of migrastatin, iso-migrastatin, dorrigocin A and B, epi-dorrigocin, NK30424 A and B and lactimidomycin, methods of synthesizing and using these analogs and further methods of creating a combinatorial library of these compounds through chemical modifications....

20060211737 - Benzene, pyridine, and pyridazine derivatives: wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions...

20060211738 - Certain substituted diphenyl ureas, as modulators of kinase activity: Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non-covalent complexes, prodrugs, and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are also provided...

20060211739 - Use of selective p2x7 receptor antagonists: r

20060211740 - Novel compounds: The present invention relates to novel hydroxyethylamine compounds having Asp2 (β-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease....

20060211741 - Substituted sulfonylaminoarylmethyl cyclopropanecarboxamide as vr1 receptor antagonists: e

20060211742 - Amorphous lercanidipine hydrochloride and uses thereof: The invention provides a substantially pure amorphous lercanidipine hydrochloride having a purity of at least 95% pure, preferably at least about 97% pure, more preferably at least about 99% pure, and still more preferably at least about 99.5% pure. The invention further relates to methods of preparing substantially pure amorphous...

20060211743 - 3-pyridinecarboxamide reduces nerve degeneration: Neural degeneration is reduced in a patient determined to be suffering from chronic neurodegeneration by administering to the patient an effective amount of 3-pyridinecarboxamide (nicotinamide) and detecting a resultant decrease in the neural degeneration....

20060211744 - 3-pyridinecarboxamide reduces nerve degeneration: Neural degeneration is reduced in a patient determined to be suffering from chronic neurodegeneration by administering to the patient an effective amount of 3-pyridinecarboxamide (nicotinamide) and detecting a resultant decrease in the neural degeneration....

20060211745 - Methods and compositions for treating cancer: In one aspect the present invention provides methods for treating cancer in a mammal, including the step of administering to a mammal suffering from a cancer an amount of ebselen that is sufficient to inhibit the growth of the cancer. In another aspect, the present invention provides methods for enhancing...

20060211746 - Desferrithiocin derivatives and methods of use thereof:

20060211747 - Methods of screening for compounds which inhibit the activity of cdc34 in a zinc-mediated manner and compounds obtained by this method: The present invention relates to methods of searching/screening for compounds which inhibit the activity of the ubiquitin conjugating enzyme Cdc34 in a zinc-mediated manner, to compounds obtainable by such a method, to a method of treating mammalian subjects with such compounds, to pharmaceutical compositions containing such compounds, to the use...

20060211748 - Sulphydryl compounds in combination with sulpha compounds: The present invention discloses various compositions and methods for co-administration of one or more sulfa compounds or pharmaceutically acceptable salts thereof, and one or more sulphydryl compounds in the treatment or prevention of disease, wherein the disease has in whole or part microbial and/or inflammatory origins....

20060211749 - Treatment with omega-3 fatty acids and ppar agonist and/or antagonist and a combination product thereof: A method and composition for blood lipid therapy that comprises administering to the subject an effective amount of a PPAR agonist and/or antagonist and an omega-3 fatty acid. The methods and compositions include combination products or concomitant therapy for the treatment of subjects with hypertriglyceridemia, hypercholesteremia, mixed dyslipidemia, vascular disease,...

20060211750 - Triazole derivatives: m

20060211751 - Zolmitriptan crystal forms: The invention encompasses novel crystalline forms of zolmitriptan herein defined as Form B, D, C, E, F, G, H, I, J, K, M, N, O, P, Q, R, S, or Amorphous and to methods of making thereof. The invention also encompasses methods of making zolmitriptan crystalline Form A....

20060211752 - Use of phenylmethimazoles, methimazole derivatives, and tautomeric cyclic thiones for the treatment of autoimmune/inflammatory diseases associated with toll-like receptor overexpression: The present invention relates to the treatment of autoimmune and/or inflammatory diseases associated with overexpression of Toll-like receptor 3 (TLR3) as well as Toll-like receptor 4 (TLR4) and/or TLR3/TLR4 signaling in nonimmune cells, monocytes, macrophages, and/or dendritic cells in association with related pathologies. This invention also relates to the use...

20060211753 - Method and composition which reduces stimulation of muscles which dilate the eye: A method for optimizing pupil size in individuals suffering from excessive pupillary dilation in dim light as well as through medication is disclosed. Alpha 1 antagonist is applied in an eye drop formulation to the eye, resulting in reduced pupil size in dim light, but less reduction in pupil size...

20060211754 - Compositions comprising n-propanoyl derivatives of amino acids, aminocarbohydrates and derivatives thereof: The embodiments relate to compositions comprising therapeutically effective amounts of at least one N-propanoyl derivative of amino acids, aminocarbohydrates, and derivatives thereof. The compositions are useful the prevention and treatment of symptoms or syndromes associated with nervous, vascular, musculoskeletal, or cutaneous systems. The compositions may be topically or systemically administered...

20060211755 - 3-oxo-1, 3-dihydro-indazole-2-carboxylic acid amide derivatives as phospholipase inhibitors: The present invention provides a compound of formula I (1) wherein; R, is selected from the group consisting of C5-C13alkyl; C,—C,2haloalkyl, C4C,2alkenyl, C4-C12alkynyl, or C,—C5alkylcycloalkyl, C3-C8cycloalkyl, C, C5alkylheterocyclic, and aryl, wherein the, cycloalkyl, cycloalkenyl, heterocyclic and aryl substituents are optionally substituted with one to three substituents independently selected from C,—C8a)kyl,...

20060211756 - Novel heterocycle derivatives useful as selective androgen receptor modulators (sarms): The present invention is directed to novel heterocycle derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor....

20060211757 - Small molecule inhibitors of mdm2 and the uses thereof: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s)....

20060211758 - M3 muscarinic acetylcholine receptor antagonists: Novel thiazole aniline compounds, pharmaceutical compositions, methods of making them and uses thereof in treating M3 muscarinic acetylcholine receptor mediated diseases are disclosed....

20060211759 - Bis-heterocyclic compounds with antitumour and chemosensitising activity: Bis-heterocyclic compounds of general formula (I) are described which are useful as antitumour and chemosensitising agents....

20060211760 - Indolamide derivatives which possess glycogen phosphorylase inhibitory activity: A compound of the formula (1) or a pharmaceutically-acceptable salt wherein, for example, A is phenylene or heteroarylene; Y is selected from —C(O)R2, —C(O)OR2, —C(O)NR2R3, -(1-4C)alkyl [optionally substituted]-(2-4C)alkenyl, —SO2NR2R3, and —S(O)cR2 (wherein c is 0, 1 or 2); compounds which possess glycogen phosphorylase inhibitory activity and accordingly have value in...

20060211761 - Hmg-coa-reductase inhibitors: The invention relates to particular hydroxyl and protected hydroxyl derivatives of compounds known to be useful as HMG CoA-reductase inhibitors. In particular, herein are provided hydroxyl and protected hydroxyl compounds of Formula I and their corresponding lactones....

20060211762 - Omega-3 fatty acids and dyslipidemic agent for lipid therapy: A method and composition for blood lipid therapy by administering to the subject an effective amount of a dyslipidemic agent and omega-3 fatty acids. The method utilizes a single administration or a unit dosage of a combination of dyslipidemic agent and omega-3 fatty acids for the treatment of patients with...

20060211763 - Treatment with statin and omega-3 fatty acids and a combination product thereof: A pharmaceutical composition in unit dose form, comprising an essentially homogeneous solution comprising a statin essentially dissolved in solvent system comprising natural or synthetic omega-3 fatty acids or pharmaceutically acceptable esters, derivatives, conjugates, precursors or salts thereof, or mixtures thereof, wherein less than 10% of the statin is undissolved in...

20060211764 - Cell activator, process for producing cell activator and apparatus therefor: It is determined whether phase noise and parasitic oscillation take place on the basis of a carrier-to-noise (C/N) ratio calculated with amplitudes in an amplitude direction of signal points of a reception signal and a C/N ratio calculated with amplitudes in a phase direction of the signal points of the...

20060211765 - Novel compounds: The invention relates to substituted phenoxyacetic acids (I) as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation....

20060211766 - Gelled immunomodulating topical compositions and a method of treating warts and other human papilloma virus skin infections: Topical drug compositions of this invention contain delayed type contact sensitizing haptens in a unique non-flowable, non-toxic, non-volatile, anhydrous gel composition to achieve retained site application on warts and other human papilloma virus (HPV) skin infections. The preferred gelled compositions contain, but are not limited to, the sensitizing haptens, squaric...

20060211767 - Method of combating turf pests with a combination of imidacloprid and bifenthrin: This invention relates to a method of controlling surface insect pests of turf using bifenthrin and imidacloprid....

20060211768 - Means for the modulation of processes mediated by retinoid receptors and compounds useful therefor: In accordance with the present invention, there are provided methods to modulate processes mediated by retinoid receptors, employing high affinity, high specificity ligands for such receptors. In one aspect of the present invention, there are provided ligands which are more selective for the retinoid X receptor than is retinoic acid...

20060211769 - Methods for inhibiting angiogenesis and tumor growth: wherein G1 and G2 are each independently —NH—C(O)—O—(CH2)v—(C6H4)—X3; Y1 and Y2 are each independently —OH or C1-C4 alkoxy; X1 and X2 are each independently halo or C1-C4 alkoxy; X3 is fluoro, nitro, C1-C4 alkyl, C1-C4 alkoxy, or C1-C4 perfluoroalkyl; Z is —C≡C—, —C6H4—, cis —CH═CH—, trans —CH═CH—, cis —CH2—CH═CH—CH2—, trans...

20060211770 - Enhanced bimatoprost ophthalmic solution: A composition comprising from 0.005% to 0.02% bimatoprost by weight and from 100 ppm to 250 ppm benzalkonium chloride, wherein said composition is an aqueous liquid which is formulated for ophthalmic administration is disclosed herein. A method which is useful in treating glaucoma or ocular hypertension related thereto is also...

20060211771 - Phenyl benzamides: c

20060211772 - Processes for the preparation of atomoxetine hydrochloride: The present invention provides improved processes for the preparation of atomoxetine hydrochloride under reaction conditions that improve reaction yields and facilitate commercial synthesis. In particular, the invention is directed to the synthesis of atomoxetine HCl by adding HCl to a mixture of (R)-(−)-tomoxetine (S)-(+)-mandelate with an organic solvent, with or...

20060211773 - Polyamine-metal chelator conjugates: Many metal collators have polar or charged functional groups, which render them difficult to transport across a cell membrane. Polyimide-metal collator conjugates of the invention are compounds comprising a first moiety which is a metal collator and a second moiety which is a polyimide, where the polyimide moiety includes three...

20060211774 - Method of diagnosins a genetic susceptibility for bone damage: The present invention relates to the identification of a novel nucleotide polymorphism in the inhibin beta-A (INHBA) gene and the exploitation of this nucleotide polymorphism in the diagnosis of susceptibility to bone damage, particularly fracture. Also provided are transgenic non-human animals comprising the polynucleotides of the present invention and methods...

20060205633 - Therapeutic agent for diabetes: A pharmaceutical composition herein provided comprises at least one branched chain amino acid selected from the group consisting of isoleucine, leucine and valine, combined with at least one drug selected from the group consisting of anti-diabetic agents, agents for treating or preventing obesity and agents for treating or preventing diabetic...

20060205634 - Lactoferrin in the reduction of circulating cholesterol, vascular inflammation, atherosclerosis and cardiovascular disease: The present invention relates to methods of using lactoferrin (LF) to reduce circulating levels of cholesterol and vascular inflammation, in order to treat, prevent or reduce the incidence of atherosclerosis and cardiovascular disease....

20060205635 - Antigene oligomers inhibit transcription: Transcription of a gene in a mammalian cell is methylase-independently inhibited by contacting the cell with a nucleic acid oligomer of 12-28 bases complementary for a partially single-stranded target genomic sequence of the gene....

20060205637 - Fluoro-alkyl-cyclopeptide derivatives having anti-integrin activity: Compounds of formula (I) cyclo [NX1-R1-CO—NX2-R2-CO—NX3-R3-CO—NX4-CO—NX5-R5-CO], wherein at least one x-fluoroalkylated amino acid is present, are inhibitors of integrins, particularly those belonging to the alphavbeta3 and alphavbeta5 family, and thus are useful as medicaments, particularly for the treatment of the underlying diseases responsible for abnormal angiogenesis, such as retinopathy, acute...

20060205636 - Oxytocin as cardiomyogenesis inducer and uses thereof: The invention relates to oxytocin and oxytocin-related compounds and functional derivatives thereof, and uses thereof to induce differentiation of a non-cardiomyocyte (e.g. a stem/progenitor cell) to a cardiomyocyte. The invention further relates to the methods of prevention or treatment of conditions characterized by or associated with a cardiomyocyte loss or...

20060205638 - Process for preparing macrocyclic compounds: e

20060205639 - Pro-nanodispersion for the delivery of cyclosporin: A novel cyclosporine formulation, which is a pro-nanodispersion at room temperature, featuring solid particles of a relatively large particle size (at least about 150 nm) and yet which is a nanodispersion at body temperature....

20060205662 - Combination treatment with t-pa variant and low molecular weight heparin: The invention concerns an improved therapeutic regimen for the treatment of thrombolytic disorders, such as acute myocardial infarction (AMI). In particular, the present invention concerns the treatment of thrombolytic disorders, e.g., AMI, with a combination of a tissue plasminogen activator (t-PA) variant having improved fibrin specificity and extended plasma half-life...

20060205652 - Formulations and methods for delivery of growth factor analogs: Formulations, kits and methods for bone or cartilage repair, including treatment of osteogenic defects, including formulations of synthetic heparin-binding growth factor analogs, non-ionic polymers, gelling agents and calcium-containing agents....

20060205659 - Fumaric acid amides: wherein R1 represents OR3 or a D- or L-amino acid radical —NH—CHR4—COOH bonded via an amide bond, wherein R3 is hydrogen, a straight-chained or branched, optionally substituted C1-24 alkyl radical, a phenyl radical or C6-10 aralkyl radical and R4 is a side chain of a natural or synthetic amino acid...

20060205657 - Irrigation solution and method for inhibition of pain and inflammation: A method and solution for perioperatively inhibiting a variety of pain and inflammation processes at wounds from general surgical procedures including oral/dental procedures. The solution preferably includes at least one pharmacological agent that is a class I cytokine soluble receptor, and optionally additional multiple pain and inflammation inhibitory agents at...

20060205658 - Irrigation solution and method for inhibition of pain and inflammation: A method and solution for perioperatively inhibiting a variety of pain and inflammation processes at wounds from general surgical procedures including oral/dental procedures. The solution preferably includes at least one pharmacological agent that is an interleukin-1 (IL-1) soluble receptor, and optionally additional multiple pain and inflammation inhibitory agents at dilute...

20060205648 - Liquid, aqueous pharmaceutical compositions of factor vii polypeptides: The present invention is directed to liquid, aqueous pharmaceutical compositions stabilised against chemical and/or physical degradation containing Factor VII polypeptides, and methods for preparing and using such compositions, as well as vials containing such compositions, and the use of such compositions in the treatment of a Factor VII-responsive syndrome. The...

20060205649 - Metabolic-based methods for modulating gene expression: This invention provides methods for modulating cellular gene expression for genes operably linked to an NRSE element that is recognized by an NRSF transcriptional repressor, by changing the concentration of reduced nicotinamide adenine dinucleotide (NADH) in the cell....

20060205651 - Method of treating cancer: The invention relates to a method of treating cancer in an individual in need thereof including inhibiting tumour growth and metastasis. The invention also relates to a method of suppressing or preventing formation of metastases, or inhibiting the growth of metastases, particularly bone metastases, from primary tumours....

20060205646 - Methods for increasing cell and tissue viability: The present invention features methods of increasing cell or tissue viability by administering to the cell or tissue a protective protein. The invention also features methods of treating a condition characterized by cell or tissue damage in a subject by administering to the subject a protective protein. Also included are...

20060205644 - Methods of treating neurological diseases by regulating migration of neuroblasts in the adult nervous system with tenascin-r: This invention provides a method for regulating migration of neuronal progenitor cells in the nervous system of a mammal. The method comprises providing a mammal with TNR, a biologically active fragment of TNR, or a TNR agonist in an amount sufficient to direct migration of the neuronal progenitor cells. The...

20060205661 - Novel albumin-free factor viii formulations: A Factor VIII composition formulated without albumin, comprising the following formulation excipients in addition to Factor VIII: 4% to 10% of a bulking agent selected from the group consisting of mannitol, glycine and alanine; 1% to 4% of a stabilizing agent selected from the group consisting of sucrose, trehalose, raffinose,...

20060205654 - Novel human growth factors: The present invention relates to huXAG-1, huXAG-2 and huXAG-3 proteins which are novel human growth factors. In particular, isolated nucleic acid molecules are provided encoding the huXAG-1, huXAG-2 and huXAG-3 proteins. huXAG-1, huXAG-2 and huXAG-3 polypeptides are also provided as are vectors, host cells and recombinant methods for producing the...

20060205655 - Nucleic acids encoding (poly) peptides having chips activity: The invention relates to nucleic acid molecules encoding (poly)peptides having chemotaxis inhibiting (poly)peptides CHIPS activity, to recombinant vectors harboring such molecules, and the host cells carrying the vectors. The invention further relates to methods for preparing recombinant (poly)peptides having CHIPS activity and to the use of such recombinant (poly)peptides having...

20060205660 - Ob protein-immunoglobulin chimeras: The present invention concerns long-half derivative of the obesity protein OB. The invention specifically concerns OB protein-immunoglobulin chimeras and polyethylene glycol (PEG)-OB derivatives, which have extended half-life as compared to the corresponding native OB proteins. The invention further relates to methods for appetite and/or weight reducion and for treating other...

20060205642 - Oral methods of treatment using proanf peptides: A method of treatment of hypertension, congestive heart failure, pulmonary edema, nephrotic syndrome, acute and chronic renal failure, toxemia of pregnancy, hepatic cirrhosis, and/or hyperkalemia. Humans or other mammals are administered an effective amount of peptide(s) consisting of amino acids 1-30 (proANF 1-30), amino acids 31-67 (proANF 31-67) and amino...

20060205656 - P-superfamily conopeptides: The present invention is directed to P-superfamily conopeptides, to DNA encoding precursors of the P-superfamily conopeptides and to the precursor peptides....

20060205640 - Papillosin antimicrobial peptide, a gene coding said peptide, a vector, a transformed organism and a compound containing said organism: A antimicrobial peptide isolated from an extract from a marine invertebrate, whose amino acid sequence is as follows: GFWKKVGSAAWGGVKAAAKGAAVGGLNALAKHIQ (SEQ ID No. 1), its derivatives, its fragments and a polypeptide, as well as transformed host organisms capable of producing the peptide such as microorganisms, animal cells, digital cells and plants,...

20060205647 - Somatostatin and somatostatin agonists for decreasing body weight: The present invention relates to a method of decreasing body weight in a patient. The method includes the step of administering a therapeutically effective amount of a somatostatin or a somatostatin agonist ot said patient. A pharmaceutical/cosmetic composition comprises the somatostatin or somatostatin agonist. Such products are used to prepare...

20060205653 - Sources for, and types of, insecticidally active proteins, and polynucleotides that encode the proteins: The subject invention provides exciting new sources for surprising, new types of toxin complex (“TC”) proteins. The subject invention includes these new classes and types of TC proteins. The subject invention also includes polynucleotides that encode the subject proteins. The subject invention further provides vectors and cells comprising these polynucleotides....

20060205643 - Treatment of inflammatory conditions of the intestine: A method for the treatment and/or prophylaxis of an inflammatory condition of the intestine of a patient, comprises parenteral administration to the patient of an effective amount of high density lipoprotein (HDL)...

20060205650 - Treatment of neuropsychiatric disease with protease and neuraminidase inhibitors: The present invention provides a method of treating a neuropsychiatric disease characterized by an abnormally elevated level of a fragment of an isoform of a neural cell adhesion molecule, N-CAM, in the brain or cerebrospinal fluid of an affected human subject, comprising administering a therapeutically effective amount of at least...

20060205645 - Use of hypoxia inducible factor 2 alpha for curing neonatal respiratory distress syndrome and as a target for the treatment of pulmonary hypertension: The current invention relates to the field of hypoxia-induced disorders and more specifically to the use of hypoxia inducible factor 2α as a target in a method for the screening for molecules that can be used for the treatment of pulmonary hypertension. The invention further relates to the use of...

20060205641 - Vanilrep4 polypeptides and vanilrep4 polynucleotides: VANILREP4 polypeptides and polynucleotides and methods for producing such polypeptides by recombinant techniques are disclosed. Also disclosed are methods for utilizing VANILREP4 polypeptides and polynucleotides in diagnostic assays....

20060205665 - Intracellular delivery of biological effectors: The invention relates to a sequence of amino acids with the capacity to facilitate transport of an effector across a biological membrane. More specifically, the present invention relates to novel peptide transporters that specifically target certain cell types for the intracellular delivery of drugs and therapeutic agents....

20060205663 - Methods to produce lung surfactant formulations via lyophilization and formulations and uses thereof: Methods of producing lung surfactant formulations through solvent dissolution and lyophilization are described as well as surfactant formulations derived therefrom. Methods of treating respiratory distress dysfunction are also provided....

20060205664 - Mucin hypersecretion inhibitors and methods of use: Peptides are provided that comprise less than 24 amino acids. The peptides have an amino acid sequence selected from the group consisting of: (a) an amino acid sequence having from 4 to 23 contiguous amino acids of a reference sequence PEPTIDE 1; (b) an amino acid sequence substantially identical to...

20060205666 - Gamma-secretase inhibitors: Disclosed, as a γ-secretase inhibitor, is a compound consisting of an amino acid sequence which consists of at least three consecutive amino acids of the amino acid sequence Val-Val-Ile-Ala-Thr-Val-Ile-Val-Ile-Thr-Leu-Val-Met-Leu-Lys-Lys including Leu at position 11, wherein, between the Leu and one or both amino acids located immediately before or after it,...

20060205667 - Wt1 substitution pepides: Novel substituted type peptides of WT1 wherein the cysteine residue is substituted with a defined amino acid residue, polynucleotides encoding said peptides, cancer vaccines using those peptides or polynucleotides in vivo or in vitro, or the like are provided. Peptides which comprise an amino acid sequence of the formula: X—Y-Thr-Trp-Asn-Gln-Met-Asn-Leu...

20060205670 - Anti-angiogenic compounds: The present invention provides AA targeting compounds which comprise AA targeting agent-linker conjugates which are linked to a combining site of an antibody. Various uses of the compounds are provided, including methods to treat disorders connected to abnormal angiogenesis....

20060205668 - Central nervous system damage: The application provides peptides that interact with the inhibitory domains of the myelin proteins Nogo, TNR, and MAG. These may be used in the treatment of CNS damage, and for the development of further treatments. Also provided are methods and materials for immunizing subjects against the inhibitory domains of the...

20060205669 - G-type peptides and other agents to ameliorate atherosclerosis and other pathologies: This invention provides novel peptides, and other agents, that ameliorate one or more symptoms of atherosclerosis and/or other pathologies characterized by an inflammatory response. In certain embodiment, the peptides resemble a G* amphipathic helix of apolipoprotein J. The peptides are highly stable and readily administered via an oral route....

20060205673 - 2-amino-3-hydroxy-4-tert-leucyl-amino-5-phenyl-pentanoic acid amide derivatives: i

20060205671 - Compositions and methods for use of a protease inhibitor and adenosine for preventing organ ischemia and reperfusion injury: Methods and compositions including combined use of a serine protease inhibitor and adenosine when administered as a single pharmaceutical composition, concomitantly or sequentially in any order to a living subject for preventing organ ischemia or reperfusion injury. The methods and compositions disclosed herein can be used in such procedures as...

20060205672 - Novel peptides as ns3-serine protease inhibitors of hepatitis c virus: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease....

20060205675 - Combinations of dipeptidyl peptidase iv inhibitors and other antidiabetic agents for the treatment of diabetes mellitus: A method for the treatment of diabetes mellitus, especially Type 2 diabetes and conditions associated with diabetes mellitus in a mammal such as a human, which method comprises administering an effective, non-toxic and pharmaceutically acceptable amount of a dipeptidyl peptidase IV inhibitor and another antidiabetic agent, to a mammal in...

20060205674 - Prodrugs containing novel bio-cleavable linkers: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one or more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods...

20060205677 - Platinum-containing compounds exhibiting cytostatic activity, synthesis and methods of use: Platinum containing compounds exhibiting cytostatic activity, methods of synthesizing platinum-containing compounds exhibiting cytostatic activity pharmaceutical compositions comprising platinum containing compounds, and methods of using such compounds and compositions for treating cancer are disclosed....

20060205676 - Pyridine derivatives: in which R11 is hydrogen, C1-6 alkyl, halogen, hydroxy, C1-12 alkoxy, nitro, amino, C1-6 alkylsulfonylamino, C1-6 alkoxycarbonyl, C1-6 alkylamino, di (C1-6 alkyl)amino, C1-6 alkanoylamino, phenyl C1-6 alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2 represents hydrogen or halogen; R3 represents hydrogen, —CR31R32R33; R4 is hydrogen, carbamoyl, CN, carboxyl, etc.; R5 is amino, C1-6...

20060205678 - Treatment of symptoms associated with irritable bowel syndrome: Methods are provided for use in treating humans suffering from irritable bowel syndrome. In the subject methods, an effective amount of a nerve-acting agent, e.g., lidocaine, topiramate, mexiletine and gabapentin, etc. is administered to a human suffering from irritable bowel syndrome. Also provided are pharmaceutical compositions and kits for use...

20060205679 - Topical and oral formulations of cardiac glycosides for treating skin diseases: The present invention provides method, preparation and use of a variety of pharmaceutical compositions containing at least one digitalis glycoside such as oleandrin, odoroside-A, neriifolin, proscillaridin-A, methyl-proscillaridin-A, digitoxin, digoxin alone or at least one digitalis glycoside complexed with cyclodextrins. In another aspect, the present invention provides an effective method to...

20060205682 - Antibiotic and combinations of antibiotic and symptomatic relief agent formulations: Disclosed herein are antibiotic formulations and combinations of antibiotic and symptomatic relief agent formulations. The combinations are suitable to treat a variety of diseases, including an infection, while treating the symptoms associated with the disease. Also disclosed are methods of treating a disease or an infection and its symptoms, as...

20060205680 - Fungicidal agent combinations: s

20060205681 - Homogenous paste formulations: This invention provides for a pharmaceutical or veterinary paste formulation comprising: an effective amount of a therapeutic agent; fumed silica; an absorbent and a viscosity modifier; optionally a hydrophilic carrier and optionally, a colorant, stabilizer, surfactant, or preservative and methods of preparing these formulations. This invention also provides for, inter...

20060205683 - Processes for preparing clarithromycin and clarithromycin intermediate, essentially oxime-free clarithromycin, and pharmaceutical composition comprising the same: The present invention relates to processes for preparing protected silylated clarithromycin oxime, preferably 6-O-methyl-2′, 4″-bis(trimethylsilyl)-erythromycin A 9-O-(2-methoxyprop-2-yl)oxime (“S-MOP oxime”), and for converting protected silylated clarithromycin oxime, preferably S-MOP oxime, to clarithromycin. Processes for preparing protected silylated clarithromycin oxime according to the present invention, include reacting a silyl oxime derivative with...

20060205684 - Method of preparing 4-r-substituted 4-demethoxydaunorubicin: A method of synthesizing 4-R-substituted anthracyclines and their corresponding salts from 4-demethyldaunorubicin includes the steps of treating 4-demethyldaunorubicin with a sulfonylating agent to form 4-demethyl-4-sulfonyl-R3-daunorubicin. 4-Demethyl-4-R3-sulfonyl-daunorubicin is then subject to a reducing agent in the presence of a transition metal catalyst in a temperature range of about 30° C. to...

20060205685 - Azacytosine analogs and derivatives: Compounds and compositions of azacytosine analogs and derivatives are provided. In one aspect of the invention, analogs or derivatives of decitabine and azacitidine are provided with modification at the 4- and 6-position of the triazine ring, at the 1′-6′position of the ribose ring, or combinations thereof. Methods of synthesizing and...

20060205687 - Azacytosine analogs and derivatives: Compounds and compositions of azacytosine analogs and derivatives are provided. In one aspect of the invention, analogs or derivatives of decitabine and azacitidine are provided with modification at the 2-, 4-, or 6-position of the triazine ring, at the 1′-6′position of the ribose ring, or combinations thereof. Methods of using,...

20060205686 - Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase: The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B...

20060205689 - Bivm (basic, immunoglobulin-like variable motif-containing) gene, transcriptional products, and uses thereof: The subject invention provides polynucleotide sequences, designated BIVM, and transcriptional/translational products obtained from the polynucleotide sequences of the invention. The subject invention also provides polynucleotide and polypeptide sequences provided by SEQ ID NOs:1-28. Also provided are methods of detecting the presence of BIVM nucleic acids or polypeptides in samples suspected...

20060205688 - Method of modulating epithelial cell activity by modulating the functional levels of sphingosine kinase: The present invention relates generally to a method of modulating endothelial cell functional characteristics and to agents useful for same. More particularly, the present invention relates to a method of modulating vascular endothelial cell pro-inflammatory and angiogenic phenotypes by modulating the functional levels of intracellular sphingosine kinase. The method of...

20060205690 - Glycosaminoglycans for treatment of emotional dysfunctions: The present invention relates to the use of glycosaminoglycan fractions having an average molecular weight of 2400 (∀200) D for the preparation of pharmaceutical compositions suitable for the treatment of emotional dysfunctions, especially depressive disorders, anxiety disorders, anxiety neurosis, agitation, confusion....

20060205691 - Water-soluble iron-carbohydrate complexes, production thereof, and medicaments containing said complexes: Water soluble iron carbohydrate complex obtainable from an aqueous solution of iron(III) salt and an aqueous solution of the oxidation product of one or more maltrodextrins using an aqueous hypochlorite solution at a pH-value within the alkaline range, where, when one maltodextrin is applied, its dextrose equivalent lies between 5...

20060205692 - 1,1-and 1,2-bisphosphonates as apoliprotein e modulators: The present invention relates to methods of use 1,1- and 1,2-bisphosphonate compounds to modulate apolipoprotein E levels and use of such compounds in therapy, including cardiovascular and neurological disease states....

20060205693 - Antisense antiviral compounds and methods for treating a filovirus infection: The invention provides antisense antiviral compounds and methods of their use and production in inhibition of growth of viruses of the Filoviridae family, and in the treatment of a viral infection. The compounds and methods relate to the treatment of viral infections in mammals including primates by Ebola and Marburg...

20060205694 - Stabilized compositions of volatile alkylating agents and methods of using thereof: A composition and method for treatment of cancer. The composition for treating a skin disorder, comprising: a Nitrogen Mustard or an HX salt of the Nitrogen Mustard, wherein the Nitrogen Mustard or the HX salt of the Nitrogen Mustard is in a non-aqueous vehicle or carrier that does not include...

20060205695 - Novel derivatives of 4,4' dithiobis-(3-aminobutane-1-1-sulfonates) and compositions comprising the same: The invention relates to derivatives of 4,4′-dithiobis-(3-aminobutane-1-sulfonates) of formula (1), of use for the treatment and prevention of primary and secondary arterial hypertension....

20060205696 - [[2-(amino-3,4-dioxo-1-cyclobuten-1-yl)amino]alkyl]-acid derivatives for the treatment of pain: where R1 is H, alkyl or phenylalkyl; R2 is H, alkyl, alkenyl or phenylalkyl; or R1 and R2 taken together as Z are —CH2C—H2—, —CH2C(R6)(R7)CH2— or —CH2C(R8)(R9)—C(R10)(R11)CH2—, where R6, R8 and R10 are, independently, H, alkyl or hydroxyl and R7, R9 and R11 are, independently, H or alkyl; A is...

20060205697 - Novel betulin derivatives, preparation thereof and use thereof: e

20060205698 - 7-phenyl-substituted tetracycline compounds: 7-phenyl-substituted tetracycline compounds which are substantially free of positional isomers, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7-phenyl-substituted tetracycline compounds are described. 7-substituted tetracycline compounds which are substantially free of positional isomers, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7-substituted tetracycline compounds...

20060205699 - Topical treatment for psoriasis: The present treatment cocktail represents a dual mode topical treatment for the skin disease psoriasis. The composition contains at least an Analgesic Agent and a Drying Agent as selected from the group disclosed herein. The agents heal psoriatic plaques by promoting the exfoliation of existing psoriatic plaques and preventing additional...

20060205700 - Non invasive method for prevention and treatment of cancer: This invention relates to a novel non invasive method for preventing or treating cancer or its recurrence and to the novel use of compounds useful therein. Very low cost, rapid action and generally no side effects are also objects inherent to the invention, realized through novel use of otherwise well...

20060205701 - Solid peroral contraceptive preparations: The solid peroral contraceptive contains an effective ingredient combination of dienogest in a daily dosage of equal to or less than 2.0 mg and ethinyl estradiol in a daily dosage of less than 0.03 mg together with one or more pharmaceutically acceptable carriers. The dienogest is released in two stages,...

20060205702 - Combinations comprising antimuscarinic agents and corticosteroids: Combinations comprising (a) a corticosteroid and (b) an antagonist of M3 muscarinic receptors which is 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane, in the form of a salt having an anion X, which is a pharmaceutically acceptable anion of a mono or polyvalent acid are useful, e.g., for treatment of respiratory disease, e.g., asthma or chronic...

20060205703 - Stabilized steroid composition and method for its preparation: Stabilized, 17-substituted hydrocortisone containing compositions and methods of manufacture are disclosed. Isomerization of the hydrocortisone component of topical steroid compositions is markedly reduced by including an omega-6 acid component in the form of a free acid or as a compound such as an ester. Specifically disclosed are methods for preventing...

20060205704 - Modulation of neurodegenerative diseases through the progesterone receptor: Methods for modulating hormonal pathways involving the progesterone receptor in a subject with a neurodegenerative disorder, are provided. Progesterone receptor activity is modulated by administering an effective amount of an progesterone receptor modulating pharmacological agent to a subject such that the progesterone receptor modulating pharmacological agent interacts with the progesterone...

20060205707 - Biologically active microlides, compositions, and uses thereof: The present invention further provides a comprising a therapeutically effective amount of at least one compound of the present invention, alone or in combination with at least one additional therapeutic agent. The therapeutically effect amount can be a vacuolar-type (H+)-ATPase-inhibiting effective amount and/or an anticancer effective amount. The present invention...

20060205705 - Hsp90 inhibitors, methods of making and uses therefor: The invention provides purified 18,21-didehydro-18,21-dideoxo-18,21-dihydroxy-geldanamycin derivatives, pharmaceutically acceptable salts thereof and prodrugs thereof that are potent Hsp90 binding agents that are useful for the treatment and/or the amelioration of symptoms of cancer and other proliferative tissue disorders....

20060205706 - Process for enantioselective synthesis of single enantiomers of thio-substituted arylmethanesulfinyl derivatives by asymmetric oxidation: e

20060205708 - Aryl oximes: Aryl oxime derivatives of the formula (I), in which R1, R2, R3, X and B are as defined in Claim 1, act as phosphodiesterase IV inhibitors and can be employed for the treatment of osteoporosis, tumours, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases,...

20060205709 - Preventive/remedy for retinal nerve diseases containing alkyl ether derivatives or salts thereof: or its salt: wherein R1 and R2 represent each a substituent such as hydrogen, halogeno or alkyl; R3 represents alkylamino, amino or hydroxyl; the ring A represents a 5- or 6-membered aromatic heterocycle or a benzene ring; m and n are each an integer of from 1 to 6; and...

20060205710 - Spiroazacyclic compounds as monoamine receptor modulators: The present invention relates to spiroazacyclic compounds as monoamine receptor modulators; compositions comprising the same; methods of inhibiting an activity of a monoamine receptor with said compounds; methods of treating a disease condition associated with a monoamine receptor using said compounds; and methods for identifying a subject suitable for treatment...

20060205711 - Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions: e

20060205712 - Basic non-peptide bradykinin antagonists and pharmaceutical compositions therefrom: Non-peptide compounds of formula (I) having activity as specific antagonists of bradykinin (BK) B2 receptor. The compounds are chemically characterized by the presence of an alpha, alpha-disubstituted amino acid at least one amino group, free or salified, or the corresponding ammonium quaternary salt. These BK receptor antagonists are a novel...

20060205713 - Pyridazine derivatives and their use as therapeutic agents: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a...

20060205714 - Method of synthesis and isolation of solid n-desmethylclozapine and crystalline forms thereof: Disclosed herein are crystalline Forms A, B, C, D, and E of N-desmethylclozapine, methods of preparing the same, pharmaceutical compositions comprising the same, and methods of therapeutic treatment involving N-desmethylclozapine polymorphic forms....

20060205715 - 6-substituted nicotinamide derivatives as opioid receptor antagonists: A compound of the formula (I) or a pharmaceutically acceptable salt, enantiomer, racemate, diastereomers or mixtures thereof, or a solvate thereof, formulations and methods of use thereof, as opioid receptor antagonists are disclosed wherein the variables are as described herein....

20060205716 - Microbicidal agents: The invention relates to antimicrobial, synergistically active mixtures of p-chloro-m-cresol (CMC) and/or its sodium or potassium salt and 2-methyl-2H-isothiazol-3-one (MIT)...

20060205718 - Benzothiazole, thiazolopyridine, benzooxazole and oxazolopyridine derivatives: wherein A, B1, B2, R1, R2 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are...

20060205717 - Pyridodiazines as plant fungicides: Fungicidal compounds of general formula (1) wherein R, R1, R2, W, X, Y and Z are as defined in the specification....

20060205719 - Novel compounds having an antibacterial activity: n

20060205720 - Cannabinoid receptor ligands and uses thereof: Compounds of Formula (I) and (II) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein....

20060205721 - Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors: wherein said R2 substituent may optionally be substituted; R3 represents halo; hydroxy; optionally substituted C1-6alkyl; C2-6alkenyl or C2-6alkynyl, each optionally substituted; optionally substituted polyhaloC1-6alkyl; optionally substituted C1-6alkyloxy; optionally substituted polyhaloC1-6alkyloxy; C1-6alkylthio; polyhaloC1-6alkylthio; C1-6alkyl-oxycarbonyl; C1-6alkylcarbonyloxy; C1-6alkylcarbonyl; polyhaloC1-6alkylcarbonyl; cyano; carboxyl; aryloxy; arylthio; arylcarbonyl; NR6bR7b; C(═O)—NR6bR7b; —NR5—C(═O)—NR6bR7b; —NR5—C(═O)—R5; —S(═O)n1—R8b; —NR5—S(═O)n1—R8b; —S—CN; —NR5—CN; R4...

20060205723 - Indane acetic acid derivatives and their use as pharmaceutical agents, intermediates, and method of preparation: This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation....

20060205722 - 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...

20060205724 - Antagonizing nk-1 receptors inhibits consumption of substances of abuse: This invention pertains to the surprising discovery that administration of one or more NK1 receptor antagonists to a mammal can inhibit self-administration of a substance of abuse (e.g. alcohol). In one embodiment, this invention provides a method of inhibiting or reducing self-administration of a substance of abuse by a mammal....

20060205725 - Method for treating ocular hypertension and glaucoma: Provided is a method for treating ocular hypertension and glaucoma with reduced side effects such as keratoconjunctive disorders and macular edema, which comprises administering an ophthalmic composition comprising latanoprost as an active ingredient thereof to a subject in need of said treatment, wherein the ophthalmic composition contains substantially no benzalkonium...

20060205727 - Combination therapy for endothelial dysfunction, angina and diabetes: The combination of a HMG CoA reductase inhibitor like a statin, such as simvastatin, with a pFox inhibitor such as trimetazidine (“Simetazidine”) is particularly advantageous for treatment of end-stage complications, such as acute coronary syndrome (ACS) and chronic angina, especially in type II diabetics. The combination therapy is also useful...

20060205726 - Ester derivatives and medical use thereof: e

20060205728 - Novel scaffolds for beta-helix mimicry: Functionalized pyridazine derivatives having a low molecular weight and pharmaceutical compositions thereof are useful as alpha-helix mimetics and for treating conditions and/or disorders mediated by alpha-helix-binding receptors and proteins....

20060205729 - Aminopterin dosage forms and methods for inflammatory disorders: Embodiments of the present invention provide dosage forms and methods for treating a patient with an inflammatory disorder with a therapeutically effective amount of aminopterin, or a pharmaceutically acceptable salt thereof, that achieve efficacy without concomitant toxicity. Within certain embodiments, the present invention provides a method for treating an inflammatory...

20060205730 - Discovery of valuable properties for the primary energy source \"pes 2000 plus folic acid\": 1. Increased energy is produced by stimulating the Citric Acid Cycle, in 1957 Dr. Livingston successfully treated Pregnancy Toxemia in sheep, with intravenous oxaloacetic acid, demonstrating that Krebs Cycles can be stimulated by intravenous injection. 2. U.S. Pat. No. 5,475,031, “DISCOVERY OF A VALUABLE PROPERTY FOR SUCCINIC ACID AND OTHER...

20060205731 - Novel aminopyridine compounds having syk inhibitory activity: The present invention relates to an aminopyridine compound represented by the following general formula (I) or a salt thereof and an Syk inhibitor containing the compound or a salt thereof as an active ingredient. Here, X1, X2, X3, Z, Y1, Y2 represent a carbon atom or a nitrogen atom, R,...

20060205732 - Heterocyclic carboxamides and their use as fungicides: Compounds of general formula (I), in which Het represents a five or six membered saturated, partially unsaturated or aromatic ring containing between one and six heteroatoms of the group N, O, S, in which the heterocycle is substituted in an adjacent manner with —P-Q1-T-Q2, -GZ and Y, such that the...

20060205733 - Endothelin a receptor antagonists in combination with phosphodiesterase 5 inhibitors and uses thereof: The invention relates generally to combination therapies comprising an endothelin A receptor (ETA) antagonist and a phosphodiesterase 5 (PDE5) inhibitor, pharmaceutical compositions comprising ETA antagonist and PDE5 inhibitor and methods of treating various disorders comprising administering an ETA antagonist and a PDE5 inhibitor. In particular, the combination therapies and pharmaceutical...

20060205734 - Inhibitors of macrophage migration inhibitory factor and methods for identifying the same: e

20060205735 - Quinoline-4-carboxamide as nk-2 and nk-3 receptor antagonists:

20060205736 - Sulfonyl-substituted bicyclic compounds as modulators of ppar: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed....

20060205737 - Substituted arylamine compounds and methods of treatment: The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and...

20060205739 - Aroylfuranes and aroylthiophenes: The invention relates to novel substituted 2-(phenyl-, pyridyl- or pyrimidyl-carbonyl)-furanes and -thiophenes and related phenoxy/phenylthio-acetophenones and corresponding heterocyclic compounds, processes for the preparation thereof, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of neoplastic diseases and autoimmune...

20060205738 - Capped pyrazinoylguanidine sodium channel blockers: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers....

20060205740 - Chemical compounds: The present invention discloses pyrimidine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such pyrimidine derivatives are useful in the treatment of diseases associated with inappropriate ErbB family kinase....

20060205741 - Novel heterocyclic benzo[c]chromene derivatives useful as modulators of the estrogen receptors: The present invention is directed to novel heterocyclic benzo[c]chromene 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 hot...

20060205742 - Heterocyclic compounds and cerebral function improvers containing the same as the active ingredient: or the like; R1 represents hydrogen atom, C1-C6 alkyl or benzyloxy; R2 represents methyl or nil; R3 represents hydrogen atom, C1-C6 alkyl, C2-C6 alkenyl, C3-C8 cycloalkyl or —CH2R5 [wherein R5 represents phenyl (which may be substituted with C1-C6 alkyl, halogen atom or cyano)] or thienyl; R4 represents C1-C6 alkyl, C2-C6...

20060205743 - Protein kinase inhibitors: The Pyrazolo[1,5-a]pyrimidine derivatives represented by formula I and their pharmaceutically acceptable salts exhibit excellent kinase inhibiting activity. Drugs comprising the compounds as effective ingredients are therefore expected to be useful as therapeutic or prophylactic agents for a protein kinase mediated disorder in which kinase is implicated, such as inflammatory disease,...

20060205744 - Fused heterocyclic derivatives as ppar modulators: The present invention is directed to compounds represented by the following structural formula, Formula I: wherein (a) X is selected from the group consisting of a single bond, O, S, S(O)2 and N; (b) U is an aliphatic linker, (c) Y is selected from the group consisting of C, O,...

20060205745 - Microcrystal: Microcrystals of (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,6-dione having an average particle size of less than 50 μm; microcrystals of (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,6-dione having an average particle size of less than 50 μm and a crystallinity of 20% or more or the like, which possess excellent solubility, stability, bioavailability, dispersing property in a pharmaceutical formulation; and the...

20060205746 - Pharmaceutical compositions: Topical pharmaceutical compositions, e.g. in form of an emulsion, comprising a lavendustin derivative of formula (I): wherein R is methyl, methoxy or ethyl, or a pharmaceutically acceptable salt thereof, and an emollient, and optionally further excipients....

20060205747 - Non-sedating barbiturate compounds as neuroprotective agents: Methods of providing neuroprotection are disclosed comprising administering a non-sedative barbiturate compound in an amount sufficient to achieve neuroprotection in a mammalian subject. Preferred compounds are in the family of diphenylbarbituric acid and analogs. Preferred doses for a neuroprotective effect exceed the dosage of a corresponding sedative barbiturate without sedative...

20060205748 - Heterocyclic diamide invertebrate pest control agents: This invention provides compounds of Formula (I), N-oxides and suitable salts thereof, wherein A and B are independently O or S; each J is independently a phenyl ring, a naphthyl ring system, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused heterobicyclic ring system wherein...

20060205750 - Novel benzimidazole derivatives: (wherein A, B, C and D are independently nitrogen or optionally substituted methine; E is nitrogen, methine or hydroxy substituted methine; n is 0 or 1; T, U, V and W are independently nitrogen or optionally substituted methine; X is —N(SO2R4)—, —N(COR5)— or —CO—; Y is —C(R6)(R7)—, —O— or —N(R8)—,...

20060205749 - Remedy and/or preventive for lung diseases: The present invention provides a therapeutic and/or preventive agent for pulmonary disease that exhibits neutrophilic inflammation, such as, chronic obstructive pulmonary disease (COPD), pulmonary emphysema, chronic bronchitis, acute respiratory distress syndrome (ARDS), acute lung injury (ALI) and the like, which comprises 7-[2-(3,5-dichloro-4-pyridyl)-1-oxoethyl]-4-methoxy-spiro[1,3-benzodioxol-2,1′-cyclopentane] or a pharmaceutically acceptable salt thereof as an...

20060205751 - Novel compounds: e

20060205752 - Stabilized hydrocodone pharmaceutical compositions with ethylenediaminetetraacetic acid: Hydrocodone pharmaceutical formulations are stabilized with a stabilizing effective amount of ethylenediaminetetraacetic compound....

20060205753 - Use of methylnaltrexone and related compounds to treat post-operative gastrointestinal dysfunction: Methods and compositions for treating post-surgical gastrointestinal dysfunction are provided. Methods include administering a quaternary derivative of noroxymorphone (e.g., methylnaltrexone) to a patient after a segmental colectomy is performed on the patient....

20060205754 - Combination of a serotonin reuptake inhibitors and agomelatine: The present invention relates to the use of a combination of agomelatine and a serotonin reuptake inhibitor (SRIs), or an other compound, which causes an elevation in the level of extracellular serotonin, for the treatment of depression and other affective disorders....

20060205755 - Novel farnesyl protein transferase inhibitors as antitumor agents: and the pharmaceutically acceptable salts thereof. Y is C or CH. When Y is C then Z is not present and the optional bond from Y to the C-11 carbon of the tricyclic nucleus is present. When Y is CH then Z is present and Z is H or —OH....

20060205757 - 39-desmethoxyrapamycin, compositions and methods of use thereof: The present invention relates to medical uses of 39-desmethoxyrapamycin....

20060205756 - Antitussives: e

20060205758 - Method for reducing the mortality rate: A method for reducing the mortality rate in a patient comprising administering to the patient a therapeutically effective amount of a tiotropium salt....

20060205759 - Cycloalkylfused indole, benzothiophene, benzofuran and indene derivatives: The present invention provides cycloalkylfused indole, benzothiophene, benzofuran, and indene derivatives, and methods for using them to, for example, treat, prevent and/or ameliorate central nervous system diseases by antagonizing 5-HT1A receptors and modulating serotonin levels....

20060205760 - Molecules and methods for fluorescence microscopy: e

20060205761 - Ccr-2 antagonists for treatment of neuropathic pain: The invention is directed to methods of treating neuropathic pain and other neuropathic diseases and conditions with CCR-2 antagonists and pharmaceutical composition containing CCR-2 antagonists....

20060205762 - Substituted pyrroline kinase inhibitors: The present invention is directed to novel substituted pyrroline compounds useful as kinase inhibitors and methods for treating or ameliorating a kinase mediated disorder....

20060205763 - Substituted pyrroline kinase inhibitors: The present invention is directed to novel substituted pyrroline compounds useful as kinase inhibitors and methods for treating or ameliorating a kinase mediated disorder....

20060205764 - Inhibition of platelet aggregation: The present invention provides methods and compositions for preventing platelet aggregation and for treating individuals suffering from conditions or undergoing procedures that may result in unwanted platelet aggregation. In particular the invention provides to methods and compositions for arterial vessel pacification. The methods are based on the administration of a...

20060205765 - Inhibitors of akt activity: The present invention is directed to compounds which contain a five-membered heterocyclic ring fused to a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration...

20060205766 - Process for making crystalline form i of clopidogrel hydrogen sulphate: A process for preparation of crystalline Form I of clopidogrel hydrogen sulphate, that include separating the crystalline Form I of clopidogrel hydrogen sulphate from a solution of clopidogrel freebase in a solvent, which is 2-propanol or 2-butanol is provided....

20060205767 - Flavanoids and isoflavanoids for the prevention and treatment of cardiovascular diseases: The present disclosure provides non-naturally occurring polyphenol compounds that upregulate the expression of Apolipoprotein A-I (ApoA-I). The disclosed compositions and methods can be used for treatment and prevention of cardiovascular disease and related disease states, including cholesterol or lipid related disorders, such as, e.g., atherosclerosis....

20060205769 - Piperidine or 8-aza-bicyclo[3.2.1]oct-3-yl derivatives useful as modulators of chemokine receptor activity: Compounds of formula (I): wherein R1, R2, R3, R4, A and n are as defined; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal)....

20060205768 - Tropane derivatives and their use as ace inhibitors: The invention relates to novel tropane 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 as...

20060205770 - Novel salts of quinuclidine derivative: There is provided an acid addition salt of (−)-(3R)-quinuclidin-3-yl(1R)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate with an acid selected from the group consisting of (−)-(2S,3S)-tartaric acid, (+)-(2S,3S)-di-O-benzoyltartaric acid, (+)-(2S,3S)-di-O-(4-methylbenzoyl)tartaric acid, (−)-L-phenylalanine, benzenesulfonic acid, cyclohexanesulfamic acid, hydrobromic acid, naphthalene-2-sulfonic acid, sebacic acid, (+)-camphor-10-sulfonic acid, p-toluenesulfonic acid, ethanesulfonic acid, methanesulfonic acid and methyl phosphate, which has little hygroscopicity...

20060205772 - Amide derivatives and their use as inhibitors of 11-beta-hydroxysteroid dehydrogenase type i: Compounds of the formula (I) provide pharmacological agents which lower intracellular glucocorticoid concentrations in mammals, in particular, intracellular cortisol levels in humans. Therefore, the compounds of the instant invention improve insulin sensitivity in the muscle and the adipose tissue, and reduce lipolysis and free fatty acid production in the adipose...

20060205771 - Caspase inhibitors as anticancer agents: Disclosed are compositions and methods for treating cancer that contain caspase inhibitors and/or antioxidant compositions. Formulations containing noncaspase inhibitor anti-cancer agents are also disclosed....

20060205773 - Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same: s

20060205774 - 4-(4-(heterocyclylakoxy) phenyl-1-(heterocyclyl-carbonyl) piperidine derivavites and related compounds as histamine h3 antagonists for the treatment of neurological diseases such as alzheimer's: The present invention relates to novel phenyl piperidinyl derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders....

20060205775 - Biphenyl compounds useful as muscarinic receptor antagonists: wherein a, b, c, d, n, R1, R2, R3, R6, R7, W, and A are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such...

20060205777 - Biphenyl compounds useful as muscarinic receptor antagonists: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods...

20060205778 - Biphenyl compounds useful as muscarinic receptor antagonists: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods...

20060205779 - Biphenyl compounds useful as muscarinic receptor antagonists: wherein a, b, c, p, W, A, X1, R1, R2, R3, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using...

20060205782 - Method of providing an antihistaminic effect in a hepatically impaired patient: R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; each of A and B is hydrogen or hydroxy with the proviso that at least one of A or B is hydrogen; or a pharmaceutically acceptable salt and individual...

20060205776 - Methylphenidate solution and associated methods of administration and produciton: A methylphenidate solution and associated methods of administration and production, which includes methylphenidate and at least one organic acid dissolved in a solvent system, where the solvent system includes at least one non-aqueous solvent. The solvent system may include water. The non-aqueous solvent can include, but is not limited to...

20060205780 - 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....

20060205781 - 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....

20060205784 - Biphenyl compounds useful as muscarinic receptor antagonists: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of...

20060205783 - Tetrahydropyran heterocyclic cyclopentyl heteroaryl modulators of chemokine receptor activity: The present invention is further directed to compounds of the formulas: (I) (II) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24 and R25 are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or...

20060205785 - Benzimidazolidinone derivatives as muscarinic agents: Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed....

20060205786 - New use of iloperidone: The invention provides the use of iloperidone in the treatment of affective disorders including bipolar mood disorders....

20060205787 - Methods and compositions using 4-amino-2-(3-methyl-2,6-dioxopiperidin-3-yl)-isoindole-1,3-dione: This invention relates to racemic and stereomerically pure 4-amino-2-(3-methyl-2,6-dioxopiperidin-3-yl)-isoindole-1,3-dione, and prodrugs, salts and solvates thereof. Synthesis, methods of use, and pharmaceutical compositions of racemic and stereomerically pure 4-amino-2-(3-methyl-2,6-dioxo-piperidine-3-yl)-isoindole-1,3-dione, and prodrugs, salts and solvates thereof, are disclosed....

20060205788 - Compounds having activity at 5ht2c receptor and uses thereof: wherein R1 is hydrogen, fluoro, chloro, hydroxy, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, C1-6alkoxy or haloC1-6alkoxy; m is 0 when ═ is a double bond and m is 1 when ═ is a single bond; R2 is hydrogen, halogen, cyano, nitro, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, C1-6alkylthio, amino, mono- or di-C1-6alkylamino or...

20060205789 - Gacyclidine formulations: Improved formulations of gacyclidine for direct administration to the inner or middle ear....

20060205790 - Medicinal arylethanolamine compounds: p

20060205791 - Pharmaceutical process and compounds prepared thereby: The present invention relates to an improved process for the preparation of a sulfinyl compound of formula (I), or a pharmaceutically acceptable salt, hydrate or solvate thereof, from a sulfide compound of formula (II), wherein in both formulae (I) and (II) R1 and R3 are selected from the group consisting...

20060205793 - Flupirtine preparation for the treatment of neurodegenerative diseases of the visual apparatus and diabetes mellitus: The invention relates to the use of flupirtine in manufacture of a pharmaceutical preparation for therapy and/or prophylaxis of diabetes mellitus, diabetic retinopathy, diabetic maculopathy, genetically related maculopathies, apoptosis of the visual apparatus and/or human glaucomas and also a combination preparation comprising flupirtine and at least one further active ingredient...

20060205792 - Stilbenes and chalcones for the prevention and treatment of cardiovascular diseases: The present disclosure provides non-naturally occurring polyphenol compounds that upregulate the expression of Apolipoprotein A-I (ApoA-I). The disclosed compositions and methods can be used for treatment and prevention of cardiovascular disease and related disease states, including cholesterol or lipid related disorders, such as, e.g., atherosclerosis....

20060205794 - Phenethanolamine derivative for the treatment of respiratory diseases: e

20060205795 - Cancer treatment with epothilones: The use of an epothilone for the treatment of a proliferative disease comprising the step of daily administration of a therapeutically effective amount of an epothilone by continuous intravenous (i.v.) administration....

20060205796 - Method for treating pain or pruritis by administering opinoid receptor agonist comprising 2-phenylbenzothiazoling derivative: e

20060205797 - Compounds for the treatment of inflammatory disorders:

20060205798 - Crystal forms of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazole-5-ol: The present invention is directed to monohydrate and anhydrate crystal forms of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol, an estrogenic receptor modulator useful in the treatment of, for example, diseases related to abnormal levels of estrogen....

20060205799 - Anti-cancer and anti-microbial oxazolidinones: Disclosed herein are various novel oxazolidinone, imidazolidinone, and thiazolidinone analogs and methods of treating cancer and/or microbial infection using these analogs. Particular 4-oxazolidinone compounds are shown to have anti-cancer and anti-microbial activity....

20060205801 - Crystal and process for producing the same: A process for producing crystals of 2-ethoxy-1-[[2′-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-benzimdazole-7-carboxylic acid (compound (I)), characterized by dissolving or suspending the compound (I) or a salt thereof in a solvent comprising an aprotic polar solvent and crystallizing it. By the process, the contaminants which are contained in the compound (I) or its salt and are...

20060205800 - Therapeutic compounds: A compound having a substituted five or six-membered carbocycle or heterocycle directly bonded to a substituted aryl or heteroaryl ring, wherein said compound has an EC50 value of 20 nM or less at the prostaglandin EP2 receptor according to the cAMP assay. Methods, compositions, and medicaments related thereto are also...

20060205803 - 1,2 diarylbenzimidazoles and their pharmaceutical use: c

20060205802 - Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof: Compounds of formula (I) or pharmaceutically acceptable salts thereof: wherein R1, R2, R3, R4 and Z are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain....

20060205804 - Process for preparing 5-(4-fluorophenyl)-1-[2r,4r)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl) ethyl]-2-isopropyl-4-phenyl-1h-pyrrole-3-carboxylic acid phenylamide: A method for preparing 5-(4-fluorophenyl)-1[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide (I), a key intermediate in the synthesis of atorvastatin calcium, is described....

20060205805 - Crystalline forms of atorvastatin: The present invention is directed to new crystalline forms of Atorvastatin calcium (2:1), referred to hereinafter as polymorphic Forms X, A, B1, B2, C, D and E. The present invention also is directed to crystalline Form A of Atorvastatin calcium (2:1) that is stable against the formation of the AED...

20060205806 - Synergistic combination: The invention relates to the combined administration of PDE inhibitors and β2 adrenoceptor agonists for the treatment of respiratory disorders....

20060205807 - Amino-chroman compounds and methods for preparing same: The present invention relates to novel amino-chroman compounds, methods of preparing such compounds, and to synthetic intermediates useful in such methods....

20060205808 - Anti-inflammatory and cure for ageing, alzheimer's disease on phloroglucinol derivatives: The fresh seeds obtained from the fresh fruits of Garcinia subelliptica, were extracted with chloroform at room temperature. The CHCl3 extract was concentrated under reduced pressure to afford a brown residue. This residue was subjected to column chromatography (silica gel) and eluted with appropriate solvent system to give two phloroglucinol...

20060205809 - Pharmaceutical preparation containing palladium complex compounds and the uses thereof for treating cancer and autoimmune disease: The present invention relates to a pharmaceutical preparation containing at least one compound of general formula (1): Pd(S2COR)2 wherein R is a straight-chain or branched alkyl residue having 1 to 30 carbon atoms, a straight-chain or branched alkenyl residue having 2 to 30 carbon atoms, a monocyclic or polycyclic alkyl...

20060205810 - Platinum therapeutic combinations: The present invention provides combination compositions comprising Pt based compounds, including satraplatin, along with another chemotherapeutic agent such as temozolomide or lonafarnib. The combinations are useful for the prevention or treatment of cancer. Method of using the combinations to treat or prevent cancer are also provided...

20060205811 - Compounds that stimulate glucose utilization and methods of use: wherein W, Cyc, p, Y, X, Z, R, R1, R2, R3, R4, i and n are as defined for Formula (I) herein. The invention also relates to pharmaceutical compositions comprising compounds capable of stimulation of glucose oxidation, methods for increasing glucose oxidation rates in myocardial cells, and methods of treatment...

20060205812 - 5-amidino-2-hydroxybenzenesulfonamide derivatives, pharmaceutical compositions containing the same and intermediates for their preparation: T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor...

20060205813 - Novel 3,4-dihydroxyhydrocinnamic acid derivative: i

20060205814 - Essential n-3 fatty acids in cardiac insufficiency and heart failure therapy: The present invention concerns a method of therapeutic prevention and treatment of a heart disease chosen from cardiac insufficiency and heart failure including the administration of an essential fatty acid containing a mixture of eicosapentaenoic acid ethyl ester (EPA) and docosahexaenoic acid ethyl ester (DHA), either alone or in combination...

20060205815 - Choline esters useful for the treatment of cognitive dysfunctions and enhancement of memory, learning and cognition: The present invention provides compounds of formula I described herein. The present invention also provides a method of treating a cognitive dysfunction in a mammal. The method includes administering to the mammal an effective amount of a compound of formula I described herein (e.g., stearyl choline chloride)....

20060205816 - Chiral lactones: e

20060205817 - Method for preparing 4-hydroxyisoleucine diastereoisomers and enantiomers and derivatives thereof: The invention concerns a method for preparing 4-hydroxyisoleucine diastereoisomers and enantiomers and derivatives thereof of general formula (I), characterized in that it consists in reducing an isoxazole derivative of formula (II) in conditions directly resulting in the derivatives of formula (I), or in obtaining at least a lactone of structure...

20060205818 - Method for the treatment of von hippel-lindau (vhl) disease with phenylacetyl-derivatives: Provided are methods of treating von Hippel-Lindau disease (VHL). Specifically embodiments of the invention provide methods for the treatment of a patient afflicted with VHL using phenylacetyl-derivatives. Preferred embodiments of the invention provide for the use of phenylacetic acid (or its sodium salt), phenylacetylglutamine (or its sodium salt) and/or phenylacetylisoglutamine...

20060205819 - Methods of treatment inflammatory bowel with lxr agonists: The present invention relates generally to the use of LXR agonists in the prevention and/or treatment of inflammatory bowel diseases....

20060205820 - Formulations of anthraquinone derivatives: A compound of formula (I): in which A is a C alkylene group with a chain length between NH and N(O)R′R″ of at least 2 carbon atoms and R′ and R″ are each separately selected from C1-4 alkyl groups and C2-4 hydroxyalkyl and C2-4 dihydroxyalkyl groups, or R′ and R″...

20060205821 - Enantiomers of n-desmethyl venlafaxine: The present invention provides enantiomers of N-Desmethyl venlafaxine, as well as their use in pharmaceutical compositions and medically useful treatments, particularly including central nervous system uses....

20060205822 - 1-aminocyclohexane derivatives for the treatment of multiple sclerosis, emotional lability and pseudobulbar affect: The present invention relates to the treatment of individuals diagnosed with multiple sclerosis, emotional lability or pseudobulbar affect comprising administering to said individual an effective amount of a 1-aminocyclohexane derivative, namely memantine or neramexane....

20060205823 - Treatment of allergic diseases using a modulator of the notch signaling pathway: A method is provided for reducing an immune response to an allergen or antigenic determinant thereof in a mammal by administering a modulator of the Notch signalling pathway....

20060205824 - Chiral integrin modulators and methods of use thereof: The invention provides enantiomers of ajoene and derivatives of Z(−)-ajoene. The derivative of Z(−)-ajoene are useful for modulating integrin-mediated functions, for treating disorders, diseases or conditions in which integrins play a role, and for treating tissues to improve their condition for a subsequent use, such as transplantation....

20060205825 - Method for the preparation of sevoflurane: A method for the preparation of (CF3)2CHOCH2F (Sevoflurane) is presented, which comprises providing a mixture of (CF3)2CHOCH2Cl, potassium fluoride, water, and a phase transfer catalyst and reacting the mixture to form (CF3)2CHOCH2F....

20060205826 - Method of using carotenoids in the prevention of cognitive decline and for other neuroprotection functions: Administration of carotenoids provide a prophylactic and/or therapeutic effect to subjects who are suffering from or at risk to develop cognitive decline or other neurological effects, such as diabetic complications, especially those related to neural tissues like retinopathy, peripheral neuropathy and central nervous system....

20060199758 - Antimicrobial surfaces: V+2 represents a doubly positively charged moiety having the formula —+NR2-T-NR2+—, or 1,4-diazoniabicyclo[2.2.2]octane; T represents a saturated or unsaturated straight-chain hydrocarbon having 1-24 carbon atoms; R represents a saturated or unsaturated hydrocarbon group having 1-24 carbon atoms; phenyl; or benzyl; W represents a saturated or unsaturated straight-chain hydrocarbon having 10-24...

20060199759 - Mixtures of insulin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same: A mixture of conjugates in which each conjugate in the mixture comprises an insulin drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed. The mixture may exhibit higher in vivo activity than a polydispersed mixture of similar conjugates. The mixture may also be more effective at...

20060199760 - 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...

20060199767 - Cardiac muscle function and manipulation: A method of causing cardiomyocyte growth and/or differentiation, the method comprising exposing a cardiomyocyte to neuregulin (NRG) thereby activating the MAP kinase pathway in the cardiomyocyte and causing growth and/or differentiation of the cardiomyocyte. Use of neuregulin, neuregulin polypeptide, neuregulin derivatives, or compounds which mimic the activities of neuregulins in...

20060199763 - Derivatives of glp-1 analogs: The present invention relates to a pharmaceutical composition comprising a GLP-1 derivative having a lipophilic substituent; and a surfactant....

20060199764 - Fgf growth factor analogs: e

20060199761 - Insulin resistance improving agent: The invention provides an insulin resistance improving agent which contains, as an active component, a C-terminal globular domain of adiponectin, adiponectin, or a gene for the domain or adiponectin. The invention also provides a therapeutic agent for type 2 diabetes, which contains, as an active component, a C-terminal globular domain...

20060199766 - Pharmaceutical composition comprising a factor viia and a factor xiii: The present invention relates to the use of a factor VIIa and a factor XIII in the treatment or pro-phylaxis of bleeding episodes....

20060199765 - Pth functional domain conjugate peptides, derivatives thereof and novel tethered ligand-receptor molecules: Novel parathyroid hormone (PTH) peptides and analogs thereof of the PTH(1-34) fragment are disclosed that combine the N-terminal signaling domain (residues 1-9) and the C-terminal binding domain (residues 15-31) via a linker. Nucleic acid molecules and peptides for PTH(1-9)-(Gly)5-PTH(15-31) (PG5) and PTH(1-9)-(Gly)7-PTH(15-31) and a novel PTH receptor are disclosed. Additionally,...

20060199762 - Skin ulcer preventive curative agent containing human recombinant hgf: A neovascularization promoting composition, a granulation formation-promoting composition and a preventive or curative composition for skin ulcer, comprising a human recombinant HGF wherein five amino acid residues are deleted in the first Kringle domain thereof. The provided compositions of the present invention are useful as a drug capable of promoting...

20060199768 - Inhibitors of reca activities for control of antibiotic-resistant bacterial pathogens: Compounds for modulating RecA protein activity are provided. In some embodiments, the compounds modulate RecA activity by interfering with assembly of monomeric RecA protein subunits into a nucleoprotein filament. In some embodiments, the compounds modulate RecA activity by interfering with adenosine triphosphate hydrolysis by the RecA protein. Methods of screening...

20060199769 - Alpha-fetoprotein peptides and uses thereof: Therapeutic compounds which are cell proliferation modulators, preferably inhibitors. These modulators contain amino acid structures that are arranged as a hydrophilic analog of an alpha-fetoprotein. The modulator may be a peptide itself, e.g., an octapeptide like that of SEQ ID NO: 5; a peptidomimetic; or may be in the form...

20060199770 - Functionalized carbon nanotubes, a process for preparing the same and their use in medicinal chemistry: The present invention relates to functionalized carbon nanotubes, a process for preparing the same and their use, in particular in medicinal chemistry and more particularly in immunology....

20060199771 - Stereoselective antifibrillogenic peptides and peptidomimetics thereof: The present invention relates to antifibrillogenic agents for inhibiting amyloidosis and/or for cytoprotection for the treatment of amyloidosis disorders. These agents include peptides, isomers thereof and peptidomimetic compounds thereof. These agents comprise a peptide having a sequence identified from the glycosaminoglycan (GAG) binding region and the prot-prot interaction region of...

20060199773 - Crystalline forms of (1r,2s)-n-[(1,1-dimethylethoxy)carbonyl]-3-methyl-l-valyl-(4r)-4-[(6-methoxy-1-isoquinolinyl)oxy]-l-prolyl-1-amino-n-(cyclopropylsulfonyl)-2-ethenyl-cyclopropanecarboxamide, monopotassium salt: The present disclosure generally relates to crystalline forms of (1R,2S)-N-[(1,1 -dimethylethoxy)carbonyl]-3-methyl-L-valyl-(4R)-4-[(6-methoxy-1-isoquinolinyl)oxy]-L-prolyl-1-amino-N-(cyclopropylsulfonyl)-2-ethenyl-cyclopropanecarboxamide. The present disclosure also generally relates to a pharmaceutical composition comprising a crystalline form, as well of methods of using a crystalline form in the treatment of Hepatitis C and methods for obtaining such crystalline form....

20060199772 - Use of a proteasome inhibitor in the treatment of endothelial dysfunction and/or in a low-dose proteasome inhibitor therapy: The present invention relates to the use of a proteasome inhibitor for the manufacture of a medicament for the prevention, onset therapy, acute therapy and/or regression of diseases associated with endothelial dysfunction. The present invention also relates to the use of a proteasome inhibitor as a low-dose treatment....

20060199774 - Remedies: The present invention relates to a medicament, a food, a beverage or a feed, each comprising as an effective ingredient a compound having an enhancing action for NGF production, which is effective for a treatment, an amelioration of symptom, prevention or the like of a disease requiring enhancement of NGF...

20060199775 - Use of pkc-activating compounds as cardioprotectants and as apoptosis-inducing anti-tumor agents: Compounds for the inducing apoptosis in cancer cells are described. The described compounds induce the translocation of protein kinase C-δ to the mitochondria and the phosphorylation of mitochondrial phospholipid scramblase 3. The compounds also provide cardioprotection through the translocation and activation of protein kinase C-ε in cardiomyocytes, thereby inhibiting apoptosis...

20060199776 - Novobiocin analogues as anticancer agents: Novel analogues and derivatives of novobiocin are provided, including compounds having modifications to the amide side chain, coumarin ring, and sugar moieties. The compounds of the present invention are useful as heat shock protein 90 inhibitors, and may be used as anticancer and neuroprotective agents....

20060199781 - Assays based on btf3 activity: This invention pertains to the discovery that BTF3 plays a critical, negative-regulatory role in programmed cell death (PCD) in C. elegans and other species. Overexpression of BTF3 leads to decreased programmed cell death, while inactivation of BTF3 leads to increased programmed cell death. Methods of modulating (upregulating or downregulating) programmed...

20060199779 - Compositions and methods for short interfering nucleic acid inhibition of nav1.8: The invention provides short interfering nucleic acids, either single-stranded or double-stranded, that cause RNAi-induced degradation of mRNA from the Nav1.8 sodium channel gene; to pharmaceutical compositions comprising such short interfering nucleic acids; recombinant vectors comprising such short interfering nucleic acids; a method for inhibiting translation of an mRNA; a method...

20060199782 - Compositions and methods for therapeutic use: n is an integer from 2-8; X1 is a cholic acid group or deoxycholic acid group; and X2 and X3 are each independently selected from the group consisting of a cholic acid group, a deoxycholic acid group, and a saccharide group, wherein the saccharide group is selected from the group...

20060199778 - Methods and products related to non-viral transfection: The invention relates to compositions and methods for the non-viral delivery of nucleic acid molecules and/or organelles to cells in vitro and in vivo. The non-viral delivery complexes provided by the invention comprise cholera toxin B subunit or functional equivalents thereof and preferably cyclodextrin....

20060199780 - Methods for modulating t cell survival by modulating bcl-xl protein level: Methods for protecting a T cell from cell death are described. The methods involve contacting the T cell with an agent which augments the bcl-XL protein level in the T cell such that it is protected from cell death. The invention further pertains to methods for increasing the susceptibility of...

20060199777 - Novel technology of intracellular delivery of dna oligonucleotides to improve drug activity: The present invention relates to methods of intracellular delivery of oligonucleotides. More particularly, the present invention relates to the use of the delivery system to deliver G-quartet oligonucleotides as a cancer therapy or an anti-viral therapy....

20060199783 - Preparation of alkyl-substituted 2-deoxy-2-fluoro-d-ribofuranosyl pyrimidines and purines and their derivatives: The present invention provides (i) a process for preparing a 2-deoxy-2-fluoro-2-methyl-D-ribonolactone derivative, (ii) conversion of the lactone to nucleosides with potent anti-HCV activity, and their analogues, and (iii) a method to prepare the anti-HCV nucleosides containing the 2-deoxy-2-fluoro-2-C-methyl-o-D-ribofuranosyl nucleosides from a preformed, preferably naturally-occurring, nucleoside....

20060199784 - Compound selected from sulfated cellulose and salts thereof and dermatitis therapeutic agent: The present invention provides a compound selected from sulfated cellulose and salts thereof which can be used as an active ingredient for a cutaneous external preparation produced intending to prevent, soften, improve or cure atopic cutaneous symptoms and the like and which are excellent in a hydrolytic resistance, and dermatitis...

20060199785 - Beta-cyclodextrin derivatives as antibacterial agents: The invention provides a new class of antibiotics to which pathogenic bacteria have not been exposed, and thus should not have developed resistance. This new class of antibiotics are derivatives of β-cyclodextrin (β-CD), which is a cyclic molecule comprising seven D-glucose units....

20060199786 - Process and methods for the preparation of optically active cis-2-hydroxymethyl-4- (cytosin-1'-yl) -1,3-oxathiolane or pharmaceutically acceptable salts thereof: e

20060199787 - Compositions comprising oxophosphonate-based metalloproteinase inhibitors: The present invention relates to compositions useful for treating or controlling disease states or conditions associated with zinc containing proteinases, especially metalloproteinases. The active ingredient in these compositions is an alpha-oxo- or alpha-thioxophosphonate of formula (I). Out of the phosphonates of formula (I), some are known and others are new....

20060199788 - Anti-inflammatory phosphonate compounds: The invention is related to phosphorus substituted anti-inflammatory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds....

20060199789 - Medical composition: The present invention provides a pharmaceutical composition, which comprises 7-[2-(3,5-dichloro-4-pyridyl)-1-oxoethyl]-4-methoxy-spiro[1,3-benzodioxol-2,1′-cyclopentane] or a pharmaceutically acceptable salt thereof and a steroid agent; an agent for treating and/or preventing a pulmonary disease; the agent which comprises 7-[2-(3,5-dichloro-4-pyridyl)-1-oxoethyl]-4-methoxy-spiro[1,3-benzodioxol-2,1′-cyclopentane] or a pharmaceutically acceptable salt thereof and a steroid agent which are simultaneously or separately with...

20060199790 - Use of 3-methoxy-pregnenolone in the production of a medicament for treating neurodegenerative diseases: The invention relates to a novel use of derivatives of neurosteroids, particularly pregnenolone, for the treatment of acute or chronic lesions of the nervous system, especially certain neurodegenerative diseases, related in particular to the ability thereof to stabilize and/or increase the polymerization of neuronal microtubules....

20060199791 - Anti-microbial composition comprising a metal ion chelating agent: The present invention relates to compositions suitable for use as topical pharmaceutical compositions for use in the treatment or prophylaxis of a superficial microbial species infection, and/or as anti-microbial cleansing compositions for use in the sanitary cleaning of animate or inanimate surfaces. The pharmaceutical compositions comprise a physiologically acceptable metal...

20060199792 - Peroxynitrite decomposition catalysts and methods of use thereof: This invention provides a novel class of substituted macrocyclic metallic complexes. The complexes are useful as peroxynitrite decomposition catalysts. Pharmaceutical compositions, and methods of making and using the compounds, or a pharmaceutically acceptable salt, hydrate, prodrug, or mixture thereof are also described....

20060199793 - Sterol absorption inhibitor compounds: The present invention provides compositions, therapeutic combinations and methods including: (a) at least one peroxisome proliferator-activated receptor activator; and (b) at least one substituted azetidinone or substituted β-lactam sterol absorption inhibitor which can be useful for treating vascular conditions, diabetes, obesity and lowering plasma levels of sterols....

20060199794 - Spiroazacyclic compounds as monoamine receptor modulators: The present invention relates to spiroazacyclic compounds as monoamine receptor modulators; compositions comprising the same; methods of inhibiting an activity of a monoamine receptor with said compounds; methods of treating a disease condition associated with a monoamine receptor using said compounds; and methods for identifying a subject suitable for treatment...

20060199795 - Receptor agonists: e

20060199796 - Substituted benzofused heterocycles: The present invention relates to the compounds of Formula I, their preparation and pharmaceutical compositions comprising them. The compounds and pharmaceutical compositions are useful, for example, for the treatment and prevention of obesity, obesity-related disorders and eating disorders....

20060199797 - Use of an ibat inhibitor for the treatment of prophylaxis of constipation: The use of an IBAT inhibitor in the treatment and/or prophylaxis of constipation, in a warm-blooded animal, such as man is described....

20060199798 - Amino bustituted diaryl[a,d]cycloheptene analogs as muscarinic agonists and methods of treatment of neuropsychiatric disorders: Disclosed herein are analogs of clozapine and pharmaceutically acceptable salts, esters, amides, or prodrugs thereof; methods of synthesizing the analogs; and methods of using the analogs for treating neuorpsychiatric disorders. In some embodiments, the analogs are amino substituted diaryl[a,d]cycloheptenes....

20060199799 - Benzimidazolidinone derivatives as muscarinic agents: Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed....

20060199800 - Pyrimidine compounds and pests controlling composition containing the same: The present invention relates to a pyrimidine compound of the formula (I): wherein R1? represents a hydrogen atom, halogen atom or C1-C4 alkyl; R2? represents C3-C7 alkynyloxy; R3? represents a hydrogen atom, halogen atom or C1-C3 alkyl; X represents C4-C7 polymethylene, in which a CH?2#191-CH?2#191 may be replaced with a...

20060199803 - Compounds: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof one of X1, X2 and X3 is N, and the others are CH; RN1 and RN2 together with the nitrogen atom to which they are attached form a nitrogen-containing heterocyclic ring having from 4 to 8 ring atoms; RN3 and...

20060199804 - Compounds: d

20060199801 - Heterobicyclic compounds used as fungicides: R2 is halogen, cyano, C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-haloalkenyl, C2-C6-alkynyl, C3-C8-cycloalkyl, C5-C8-cycloalkenyl, OR6, SR6 or NR7R8; and the agriculturally acceptable salts of the compounds I, crop protection compositions comprising at least one compound of the formula I and/or an agriculturally acceptable salt of I and at least one solid or liquid...

20060199802 - Pyridyl derivatives and their use as therapeutic agents: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (1): wherein: W is —O—, —N(R1)—, C(O), S(O)t ; (where t is 0, 1 or 2), N(R1)S(O)2, S(O)2N(R1) ,...

20060199808 - Method of synthesis and isolation of solid n-desmethylclozapine and crystalline forms thereof: Disclosed herein are crystalline Forms A, B, C, D, and E of N-desmethylclozapine, methods of preparing the same, pharmaceutical compositions comprising the same, and methods of therapeutic treatment involving N-desmethylclozapine polymorphic forms....

20060199805 - Pharmaceutical compositions for the treatment and/or prevention of anxiety disorders: The invention relates to new pharmaceutical compositions for the treatment and/or prevention of anxiety disorders and methods for the preparation thereof. In a preferred embodiment, the instant invention is directed to pharmaceutical combinations comprising flibanserin as one active ingredient in combination with at least one additional active ingredient for the...

20060199806 - Pyrrolobenzodiazepine arylcarboxamides and derivatives thereof as follicle-stimulating hormone receptor antagonists: This invention provides pyrrolobenzodiazepine arylcarboxamides selected from those of Formula (1), which act as follicle stimulating hormone receptor antagonists, as well as pharmaceutical compositions and methods of treatment...

20060199807 - Use of n-desmethylclozapine to treat human neuropsychia tric disease: Disclosed herein is a method to treat neuropsychiatric diseases including psychosis, affective disorders, dementia, neuropathic pain, and glaucoma. Treatment is carried out by administering a therapeutically effective amount of N-desmethylclozapine to a patient suffering from a neuropsychiatric disease....

20060199809 - Factor xa compounds: s

20060199810 - Muscarinic agonists: The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment...

20060199811 - Method of treatment for preventing or reducing tumor growth in the liver of patient: A method of treatment for preventing or reducing tumor growth in liver of a patient includes administering to the patient an effective about of taurolidine, taurultam or a mixture thereof, so as to prevent or reduce the tumor growth in the patient....

20060199812 - Method of conjugating aminothiol containing molecules to vehicles: The present invention relates to a novel chemical process that provides novel vehicle derivatives that are exceptional 1,2- or 1,3-aminothiol specific reagents for conjugation to unprotected targeted compounds (e.g., polypeptides, peptides, or organic compounds) having or modified to have a 1,2- or 1,3 aminothiol group. The invention further relates to...

20060199813 - Tetrahydroquinoline analogues as muscarinic agonists: The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment...

20060199816 - Aryl sulfonyl piperidines: e

20060199814 - Chemical intermediate: Compounds of Formula I, wherein R2 represents C1-6 alkyl (optionally substituted by one or more substituents selected from —OH, halo, cyano, nitro and aryl) or aryl, wherein each aryl and aryloxy group, unless otherwise specified, is optionally substituted, and methods of preparation thereof are disclosed....

20060199815 - Nk1 antagonists: wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough....

20060199817 - Phthalazine, aza- and diaza-phthalazine compounds and methods of use: wherein A1, A2, B, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates...

20060199819 - Inhibition of cyclooxygenase-2 activity: The present invention provides new methods for inhibiting the activity of the enzyme cycloxygenase-2 (or COX-2). Inhibitors of COX-2 are known to be useful anti-inflammatory, analgesic and anti-angiogenic agents. The compounds in the present case are heterocyclic substituted 4-aminoglutarimides. Methods of using the compounds to inhibit prostaglandin synthesis are claimed....

20060199818 - 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...

20060199821 - Heterocyclic amides and sulfonamides: The invention is directed to compounds and methods to inhibit p38 kinase wherein the compounds are a pyrimidine or pyridine coupled to two mandatory substituents....

20060199820 - Human adam-10 inhibitors: The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to...

20060199822 - Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors: e

20060199823 - Heteroaryl fused pyridines, pyrazines and pyrimidines as crf1 receptor ligands: Substituted heteroaryl fused pyridine, pyrazine, and pyrimidine compounds that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and...

20060199824 - Therapeutic agents useful for treating pain: b

20060199825 - Inhibitors of macrophage migration inhibitory factor and methods for identifying the same:

20060199826 - Cyclopropane compounds and pharmaceutical use thereof: wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X1 is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom,...

20060199827 - Inhibitors of macrophage migration inhibitory factor and methods for identifying the same: e

20060199828 - Pyrazine-2-carboxyamide derivatives:

20060199829 - Inhibitors of histone deacetylase: Disclosed are compounds of formula I that inhibit histone deacetylase (HDAC) enzymatic activity, pharmaceutical compositions comprising such compounds, as well as methods to treat conditions, particularly proliferative conditions, mediated at least in part by HDAC, wherein A, W, W1, W2, Ar2, and G are described herein....

20060199830 - N-(4-(4-methylthiazol-5-yl) pyrimidin-2-yl)-n-phenylamines as antiproliferative compounds: The present invention relates to 2-substituted 4-heteroaryl-pyrimidines, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders such as cancer, leukaemia, psoriasis and the like....

20060199831 - Injectable pharmaceutical compositions of an anthracenedione derivative with anti-tumoral activity: Injectable pharmaceutical compositions containing 6,9-bis[(2-aminoethyl)amino]benzo[g]isoquinoline-5,10-dione dimalcate as active ingredient in the form of a lyophilised powder with a carrier selected from lactose and dextran, mixed with sodium chloride....

20060199833 - Novel chemiluminescent compounds and their use: The present invention relates to novel chemiluminescent compounds, to a method for synthesizing these compounds, to derivatives and conjugates comprising these compounds, to the use of these compounds or conjugates thereof in chemiluminescence based assays, especially in immunoassays....

20060199834 - Oxepane isomer of 42-o-(2-hydroxy)ethyl-rapamycin: The invention provides a purified oxepane isomer of 42-O-(2-hydroxy)ethyl-rapamycin (SDZ-RAD Isomer C), a chemical process for its preparation, as well as pharmaceutical compositions and packs containing SDZ-RAD Isomer C and methods for its use as an immunosuppressive, anti-inflammatory, antifungal, antiproliferative and antitumor agent....

20060199832 - Use of non-immunosupressive pipecolic acid derivatives for inducing chondrogenic differentiation: A non-immunosuppressive pipecolic acid derivative having an affinity for FKBP-type immunophilins is provided for inducing chondrogenic differentiation. Composition containing such compounds is also disclosed....

20060199835 - Neuroprotective and anti-proliferative compounds: This invention features compounds of formula (I), (II) and (III), which are useful in the treatment of proliferative disorders characterized by loss of growth or cellular differentiation control including, but not limited to, cancer and inflammation. Formulas (I), (II), (III) have functional groups designated as A1, A2, B1, B2, X1—X9...

20060199836 - Novel thienopyridine compounds, and methods of use thereof: The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF)....

20060199837 - Substituted tetrahydro-1h-pyrazolo [3,4-c]pyridines compositions comprising them, and use: Substituted tetrahydro-1H-pyrazolo[3,4-c]pyridines, compositions comprising them and use. The present invention relates in particular to novel substituted tetrahydro-1H-pyrazolo[3,4-c]pyridines having therapeutic activity, which can be used in particular in oncology....

20060199839 - Quinolinone compounds as 5-ht4 receptor agonists: 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....

20060199838 - Substituted n-aryl benzamides and related compounds for treatment of amyloid diseases and synucleinopathies: Substituted n-aryl benzamides, related compounds and their pharmaceutically acceptable derivatives, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, including Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's...

20060199840 - Chemical derivatives and their application as antitelomerase agent: The present invention relates to cancer therapy and to novel anticancer agents having a mechanism of action which is quite specific. It also relates to novel chemical compounds as well as their therapeutic application in humans....

20060199841 - Pharmaceutical combination for the treatment of spasticity and/or pain: The present invention relates to a pharmaceutical combination for the treatment of spasticity and/or pain characterized by that the combination contains as active ingredient 70-95% w/w compound of formula (I), wherein R represents a methyl or ethyl group, and 5-30% w/w dextromethorphan (chemical name: (+/−)-3-methoxi-17-methylmorphinan)....

20060199842 - Selective serotonin 2a/2c receptor inverse agonists as therapeutics for neurodegenerative diseases: Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP...

20060199843 - Methods for treatment and management of brain cancer using 1-oxo-2-(2,6-dioxopiperidin-3-yl)-4-methylisoindoline: 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...

20060199844 - Methylene urea derivatives: The present invention relates to methylene urea derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a...

20060199845 - Thiophene compounds for inflammation and immune-related uses: e

20060199846 - Certain substituted ureas as modulators of kinase activity: Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non-covalent complexes, prodrugs, and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are also provided...

20060199847 - Stable ammonium salts of alpha-liponic acid, the production thereof and the use of the same: The invention relates to ammonium salts of α-liponic acid of general formula (I): (Lp) (A), formed from α-liponic acid (Lp) and amino compounds (A)=of general formula (II) or general formula (III). The invention also relates to a method for producing said salts, and to the use of said salts as...

20060199848 - Ion channel modulating activity ii: Methods, compositions, dosing regimes, and routes of administration for the treatment or prevention of arrhythmias. In these methods, arrythmias (e.g. atrial fibrillation, atrial flutter, early afterdepolarizations and prolongation of QT interval) may be reduced or eliminated by administering ion channel modulating compounds to a subject in need thereof. The ion...

20060199849 - Solid lercanidipine free base: The invention provides substantially pure lercanidipine free base, having a purity of at least 95%, preferably at least 97%, more preferably at least 99%, and still more preferably at least 99.5%. The lercanidipine free base of the present invention is formed as an amorphous solid that is easily handled and...

20060199850 - Insecticidal, acaricidal, and fungicidal nitromethylene compounds: e

20060199851 - Novel compounds that are useful for improving pharmacokinetics:

20060199852 - Process for the preparation of substituted benzoxazole compounds: The present invention relates to processes for the preparation of substituted benzoxazole compounds, and in particular 2-(3-fluoro-4-hydroxy-phenyl)-7-vinyl-benzoxazol-5-ol. The processes include the vinylation of a substituted benzoxazole compound having an appropriate substitutable moiety....

20060199853 - Analogs of 4-hydroxyisoleucine and uses thereof: The invention relates to analogs of 4-hydroxyisoleucine, and to lactones, pharmaceutically acceptable salts, and prodrugs thereof, to processes for their preparation, and to pharmaceutical compositions comprising the same. The analogs of the invention stimulate both glucose uptake and insulin secretion, and may thus be useful for the prevention and treatment...

20060199856 - Novel compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents: The present invention relates to a novel compounds that can be used as anti-inflammatory, immunomodulatory and antiproliferatory agents. In particular, the invention refers to new compounds which inhibit dihydroorotate dehydrogenase (DHODH), a process for their manufacture, pharmaceutical compositions containing them and to their use for the treatment and prevention of...

20060199855 - Process for producing atorvastatin hemicalcium: (c) adding a base of formula NR1R2R3 wherein R1, R2 and R3 are independently selected from H, substituted or non-substituted C1 to C7 alkyl, C6 to C9 aryl, C8 to C10 aralkyl or aminoalkyl to form atorvastatin base salt, (d) isolating by precipitation of the above atorvastatin base salt and...

20060199854 - Process for the preparation of n-substituted 2-cyanopyrrolidines: The present invention relates to a process for the preparation of a N—(N′-substituted glycyl)-2-cyanopyrrolidine comprising at least (a) reacting, in the presence of dimethylformamide, a compound of formula (V) wherein, independently of each other, X1 and X3 are halogen; X2 is halogen, OH, O—C(═O)—CH2X3, —O—SO2—(C1-8)alkyl or —O—SO2-(aryl), with L-prolinamide, followed...

20060199857 - Therapeutic agents: Substituted 3-phenylpropionic acid derivatives, processes for preparing such compounds, their utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, methods for their therapeutic use and pharmaceutical compositions containing them....

20060199858 - Substituted benzopyrans as selective estrogen receptor-beta agonists: The present invention relates to substituted benzopyran derivatives, stereoisomers, and pharmaceutical acceptable salts thereof and processes for the preparation of the same. The compounds of the present invention are useful as Estrogen Receptor ? agonists. Such agonists are useful for the treating Estrogen Receptor ? mediated diseases such as prostate...

20060199859 - Topical medicaments and methods for photodynamic treatment of disease: New photodynamic, topically-applicable medicaments and certain medical uses of such photodynamic medicaments for treatment of human or animal tissue are described, wherein a primary active component of such medicaments is a halogenated xanthene. The halogenated xanthenes constitute a family of potent photosensitizers that become photoactivated upon illumination of the treatment...

20060199861 - Methods of using derivatives of (-)-venlafaxine: Methods of preparing, and compositions comprising, derivatives of (−)-venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depression, bipolar and manic disorders, attention deficit disorder, attention deficit disorder with hyperactivity, Parkinson's disease, epilepsy, cerebral function disorders,...

20060199860 - Salts of (-)-o-desmethylvenlafaxine: Methods of preparing, and compositions comprising, derivatives of (−)-venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depression, bipolar and manic disorders, attention deficit disorder, attention deficit disorder with hyperactivity, Parkinson's disease, epilepsy, cerebral function disorders,...

20060199862 - Method for enhancing cognitive function: t

20060199863 - Product containing prostaglandin: For the purpose of the storage in a stable manner of an aqueous liquid preparation containing a prostaglandin derivative that is liable to be adsorbed on a container and slightly soluble in water, an object of the present invention is to inhibit the decrease of the content of the prostaglandin...

20060199864 - Selection of ph-dependent compounds for in vivo therapy: This invention is in the area of improved methods for the selection of pH dependent compounds to be used before, during or after a pH-lowering event as a means to minimize or prevent tissue damage....

20060199865 - Synergistic combination comprising roflumilast and (r,r) - formoterol: The invention relates to the combined administration of roflumilast and R,R-formoterol for the treatment of respiratory tract disorders....

20060199867 - Ambroxol for the treatment of chronic pain: The invention relates to the use of ambroxol and the pharmacologically acceptable salts thereof for preparing a pharmaceutical composition for the treatment of diseases which are based on a powerful activation of voltage-dependent sodium channels, particularly for the treatment of chronic pain....

20060199866 - Combination of desoxypeganine and mecamylanine for the treatment of alcohol abuse: An active substance combination comprising deoxypeganine or of one of its pharmaceutically acceptable derivatives and mecamylamine or one of its pharmaceutically acceptable derivatives. The active substance combination serves to produce a medicament for the treatment of alcohol abuse and/or alcohol dependence....

20060199868 - Use of beta-adrenoceptor antagonists for the manufacture of a medicament for the treatment of disorders of the outer retina: Compositions and methods for treating disorders of the outer retina with β-adrenoceptor antagonists are disclosed....

20060199869 - Lipase-colipase inhibitor: The present invention relates to novel colipase-lipase inhibitors of the general formulae to be used in the treatment of prophylaxis of obesity, as well as pharmaceutical compositions containing the same, and method for treating obesity using said compounds....

20060199870 - Method for producing aqueous ortho-phthalaldehyde solutions: A method for producing aqueous ortho-phthalaldehyde solutions which comprises introducing an acetal of the o-phthalaldehyde into water and subsequently setting a pH <7 by adding an acid, whereupon, then at a temperature between 10° C. and 90° C., the acetal is converted into the o-phthalaldehyde by eliminating the corresponding alcohol,...

20060199758 - Antimicrobial surfaces: V+2 represents a doubly positively charged moiety having the formula —+NR2-T-NR2+—, or 1,4-diazoniabicyclo[2.2.2]octane; T represents a saturated or unsaturated straight-chain hydrocarbon having 1-24 carbon atoms; R represents a saturated or unsaturated hydrocarbon group having 1-24 carbon atoms; phenyl; or benzyl; W represents a saturated or unsaturated straight-chain hydrocarbon having 10-24...

20060199759 - Mixtures of insulin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same: A mixture of conjugates in which each conjugate in the mixture comprises an insulin drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed. The mixture may exhibit higher in vivo activity than a polydispersed mixture of similar conjugates. The mixture may also be more effective at...

20060199760 - 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...

20060199767 - Cardiac muscle function and manipulation: A method of causing cardiomyocyte growth and/or differentiation, the method comprising exposing a cardiomyocyte to neuregulin (NRG) thereby activating the MAP kinase pathway in the cardiomyocyte and causing growth and/or differentiation of the cardiomyocyte. Use of neuregulin, neuregulin polypeptide, neuregulin derivatives, or compounds which mimic the activities of neuregulins in...

20060199763 - Derivatives of glp-1 analogs: The present invention relates to a pharmaceutical composition comprising a GLP-1 derivative having a lipophilic substituent; and a surfactant....

20060199764 - Fgf growth factor analogs: e

20060199761 - Insulin resistance improving agent: The invention provides an insulin resistance improving agent which contains, as an active component, a C-terminal globular domain of adiponectin, adiponectin, or a gene for the domain or adiponectin. The invention also provides a therapeutic agent for type 2 diabetes, which contains, as an active component, a C-terminal globular domain...

20060199766 - Pharmaceutical composition comprising a factor viia and a factor xiii: The present invention relates to the use of a factor VIIa and a factor XIII in the treatment or pro-phylaxis of bleeding episodes....

20060199765 - Pth functional domain conjugate peptides, derivatives thereof and novel tethered ligand-receptor molecules: Novel parathyroid hormone (PTH) peptides and analogs thereof of the PTH(1-34) fragment are disclosed that combine the N-terminal signaling domain (residues 1-9) and the C-terminal binding domain (residues 15-31) via a linker. Nucleic acid molecules and peptides for PTH(1-9)-(Gly)5-PTH(15-31) (PG5) and PTH(1-9)-(Gly)7-PTH(15-31) and a novel PTH receptor are disclosed. Additionally,...

20060199762 - Skin ulcer preventive curative agent containing human recombinant hgf: A neovascularization promoting composition, a granulation formation-promoting composition and a preventive or curative composition for skin ulcer, comprising a human recombinant HGF wherein five amino acid residues are deleted in the first Kringle domain thereof. The provided compositions of the present invention are useful as a drug capable of promoting...

20060199768 - Inhibitors of reca activities for control of antibiotic-resistant bacterial pathogens: Compounds for modulating RecA protein activity are provided. In some embodiments, the compounds modulate RecA activity by interfering with assembly of monomeric RecA protein subunits into a nucleoprotein filament. In some embodiments, the compounds modulate RecA activity by interfering with adenosine triphosphate hydrolysis by the RecA protein. Methods of screening...

20060199769 - Alpha-fetoprotein peptides and uses thereof: Therapeutic compounds which are cell proliferation modulators, preferably inhibitors. These modulators contain amino acid structures that are arranged as a hydrophilic analog of an alpha-fetoprotein. The modulator may be a peptide itself, e.g., an octapeptide like that of SEQ ID NO: 5; a peptidomimetic; or may be in the form...

20060199770 - Functionalized carbon nanotubes, a process for preparing the same and their use in medicinal chemistry: The present invention relates to functionalized carbon nanotubes, a process for preparing the same and their use, in particular in medicinal chemistry and more particularly in immunology....

20060199771 - Stereoselective antifibrillogenic peptides and peptidomimetics thereof: The present invention relates to antifibrillogenic agents for inhibiting amyloidosis and/or for cytoprotection for the treatment of amyloidosis disorders. These agents include peptides, isomers thereof and peptidomimetic compounds thereof. These agents comprise a peptide having a sequence identified from the glycosaminoglycan (GAG) binding region and the prot-prot interaction region of...

20060199773 - Crystalline forms of (1r,2s)-n-[(1,1-dimethylethoxy)carbonyl]-3-methyl-l-valyl-(4r)-4-[(6-methoxy-1-isoquinolinyl)oxy]-l-prolyl-1-amino-n-(cyclopropylsulfonyl)-2-ethenyl-cyclopropanecarboxamide, monopotassium salt: The present disclosure generally relates to crystalline forms of (1R,2S)-N-[(1,1 -dimethylethoxy)carbonyl]-3-methyl-L-valyl-(4R)-4-[(6-methoxy-1-isoquinolinyl)oxy]-L-prolyl-1-amino-N-(cyclopropylsulfonyl)-2-ethenyl-cyclopropanecarboxamide. The present disclosure also generally relates to a pharmaceutical composition comprising a crystalline form, as well of methods of using a crystalline form in the treatment of Hepatitis C and methods for obtaining such crystalline form....

20060199772 - Use of a proteasome inhibitor in the treatment of endothelial dysfunction and/or in a low-dose proteasome inhibitor therapy: The present invention relates to the use of a proteasome inhibitor for the manufacture of a medicament for the prevention, onset therapy, acute therapy and/or regression of diseases associated with endothelial dysfunction. The present invention also relates to the use of a proteasome inhibitor as a low-dose treatment....

20060199774 - Remedies: The present invention relates to a medicament, a food, a beverage or a feed, each comprising as an effective ingredient a compound having an enhancing action for NGF production, which is effective for a treatment, an amelioration of symptom, prevention or the like of a disease requiring enhancement of NGF...

20060199775 - Use of pkc-activating compounds as cardioprotectants and as apoptosis-inducing anti-tumor agents: Compounds for the inducing apoptosis in cancer cells are described. The described compounds induce the translocation of protein kinase C-δ to the mitochondria and the phosphorylation of mitochondrial phospholipid scramblase 3. The compounds also provide cardioprotection through the translocation and activation of protein kinase C-ε in cardiomyocytes, thereby inhibiting apoptosis...

20060199776 - Novobiocin analogues as anticancer agents: Novel analogues and derivatives of novobiocin are provided, including compounds having modifications to the amide side chain, coumarin ring, and sugar moieties. The compounds of the present invention are useful as heat shock protein 90 inhibitors, and may be used as anticancer and neuroprotective agents....

20060199781 - Assays based on btf3 activity: This invention pertains to the discovery that BTF3 plays a critical, negative-regulatory role in programmed cell death (PCD) in C. elegans and other species. Overexpression of BTF3 leads to decreased programmed cell death, while inactivation of BTF3 leads to increased programmed cell death. Methods of modulating (upregulating or downregulating) programmed...

20060199779 - Compositions and methods for short interfering nucleic acid inhibition of nav1.8: The invention provides short interfering nucleic acids, either single-stranded or double-stranded, that cause RNAi-induced degradation of mRNA from the Nav1.8 sodium channel gene; to pharmaceutical compositions comprising such short interfering nucleic acids; recombinant vectors comprising such short interfering nucleic acids; a method for inhibiting translation of an mRNA; a method...

20060199782 - Compositions and methods for therapeutic use: n is an integer from 2-8; X1 is a cholic acid group or deoxycholic acid group; and X2 and X3 are each independently selected from the group consisting of a cholic acid group, a deoxycholic acid group, and a saccharide group, wherein the saccharide group is selected from the group...

20060199778 - Methods and products related to non-viral transfection: The invention relates to compositions and methods for the non-viral delivery of nucleic acid molecules and/or organelles to cells in vitro and in vivo. The non-viral delivery complexes provided by the invention comprise cholera toxin B subunit or functional equivalents thereof and preferably cyclodextrin....

20060199780 - Methods for modulating t cell survival by modulating bcl-xl protein level: Methods for protecting a T cell from cell death are described. The methods involve contacting the T cell with an agent which augments the bcl-XL protein level in the T cell such that it is protected from cell death. The invention further pertains to methods for increasing the susceptibility of...

20060199777 - Novel technology of intracellular delivery of dna oligonucleotides to improve drug activity: The present invention relates to methods of intracellular delivery of oligonucleotides. More particularly, the present invention relates to the use of the delivery system to deliver G-quartet oligonucleotides as a cancer therapy or an anti-viral therapy....

20060199783 - Preparation of alkyl-substituted 2-deoxy-2-fluoro-d-ribofuranosyl pyrimidines and purines and their derivatives: The present invention provides (i) a process for preparing a 2-deoxy-2-fluoro-2-methyl-D-ribonolactone derivative, (ii) conversion of the lactone to nucleosides with potent anti-HCV activity, and their analogues, and (iii) a method to prepare the anti-HCV nucleosides containing the 2-deoxy-2-fluoro-2-C-methyl-o-D-ribofuranosyl nucleosides from a preformed, preferably naturally-occurring, nucleoside....

20060199784 - Compound selected from sulfated cellulose and salts thereof and dermatitis therapeutic agent: The present invention provides a compound selected from sulfated cellulose and salts thereof which can be used as an active ingredient for a cutaneous external preparation produced intending to prevent, soften, improve or cure atopic cutaneous symptoms and the like and which are excellent in a hydrolytic resistance, and dermatitis...

20060199785 - Beta-cyclodextrin derivatives as antibacterial agents: The invention provides a new class of antibiotics to which pathogenic bacteria have not been exposed, and thus should not have developed resistance. This new class of antibiotics are derivatives of β-cyclodextrin (β-CD), which is a cyclic molecule comprising seven D-glucose units....

20060199786 - Process and methods for the preparation of optically active cis-2-hydroxymethyl-4- (cytosin-1'-yl) -1,3-oxathiolane or pharmaceutically acceptable salts thereof: e

20060199787 - Compositions comprising oxophosphonate-based metalloproteinase inhibitors: The present invention relates to compositions useful for treating or controlling disease states or conditions associated with zinc containing proteinases, especially metalloproteinases. The active ingredient in these compositions is an alpha-oxo- or alpha-thioxophosphonate of formula (I). Out of the phosphonates of formula (I), some are known and others are new....

20060199788 - Anti-inflammatory phosphonate compounds: The invention is related to phosphorus substituted anti-inflammatory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds....

20060199789 - Medical composition: The present invention provides a pharmaceutical composition, which comprises 7-[2-(3,5-dichloro-4-pyridyl)-1-oxoethyl]-4-methoxy-spiro[1,3-benzodioxol-2,1′-cyclopentane] or a pharmaceutically acceptable salt thereof and a steroid agent; an agent for treating and/or preventing a pulmonary disease; the agent which comprises 7-[2-(3,5-dichloro-4-pyridyl)-1-oxoethyl]-4-methoxy-spiro[1,3-benzodioxol-2,1′-cyclopentane] or a pharmaceutically acceptable salt thereof and a steroid agent which are simultaneously or separately with...

20060199790 - Use of 3-methoxy-pregnenolone in the production of a medicament for treating neurodegenerative diseases: The invention relates to a novel use of derivatives of neurosteroids, particularly pregnenolone, for the treatment of acute or chronic lesions of the nervous system, especially certain neurodegenerative diseases, related in particular to the ability thereof to stabilize and/or increase the polymerization of neuronal microtubules....

20060199791 - Anti-microbial composition comprising a metal ion chelating agent: The present invention relates to compositions suitable for use as topical pharmaceutical compositions for use in the treatment or prophylaxis of a superficial microbial species infection, and/or as anti-microbial cleansing compositions for use in the sanitary cleaning of animate or inanimate surfaces. The pharmaceutical compositions comprise a physiologically acceptable metal...

20060199792 - Peroxynitrite decomposition catalysts and methods of use thereof: This invention provides a novel class of substituted macrocyclic metallic complexes. The complexes are useful as peroxynitrite decomposition catalysts. Pharmaceutical compositions, and methods of making and using the compounds, or a pharmaceutically acceptable salt, hydrate, prodrug, or mixture thereof are also described....

20060199793 - Sterol absorption inhibitor compounds: The present invention provides compositions, therapeutic combinations and methods including: (a) at least one peroxisome proliferator-activated receptor activator; and (b) at least one substituted azetidinone or substituted β-lactam sterol absorption inhibitor which can be useful for treating vascular conditions, diabetes, obesity and lowering plasma levels of sterols....

20060199794 - Spiroazacyclic compounds as monoamine receptor modulators: The present invention relates to spiroazacyclic compounds as monoamine receptor modulators; compositions comprising the same; methods of inhibiting an activity of a monoamine receptor with said compounds; methods of treating a disease condition associated with a monoamine receptor using said compounds; and methods for identifying a subject suitable for treatment...

20060199795 - Receptor agonists: e

20060199796 - Substituted benzofused heterocycles: The present invention relates to the compounds of Formula I, their preparation and pharmaceutical compositions comprising them. The compounds and pharmaceutical compositions are useful, for example, for the treatment and prevention of obesity, obesity-related disorders and eating disorders....

20060199797 - Use of an ibat inhibitor for the treatment of prophylaxis of constipation: The use of an IBAT inhibitor in the treatment and/or prophylaxis of constipation, in a warm-blooded animal, such as man is described....

20060199798 - Amino bustituted diaryl[a,d]cycloheptene analogs as muscarinic agonists and methods of treatment of neuropsychiatric disorders: Disclosed herein are analogs of clozapine and pharmaceutically acceptable salts, esters, amides, or prodrugs thereof; methods of synthesizing the analogs; and methods of using the analogs for treating neuorpsychiatric disorders. In some embodiments, the analogs are amino substituted diaryl[a,d]cycloheptenes....

20060199799 - Benzimidazolidinone derivatives as muscarinic agents: Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed....

20060199800 - Pyrimidine compounds and pests controlling composition containing the same: The present invention relates to a pyrimidine compound of the formula (I): wherein R1? represents a hydrogen atom, halogen atom or C1-C4 alkyl; R2? represents C3-C7 alkynyloxy; R3? represents a hydrogen atom, halogen atom or C1-C3 alkyl; X represents C4-C7 polymethylene, in which a CH?2#191-CH?2#191 may be replaced with a...

20060199803 - Compounds: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof one of X1, X2 and X3 is N, and the others are CH; RN1 and RN2 together with the nitrogen atom to which they are attached form a nitrogen-containing heterocyclic ring having from 4 to 8 ring atoms; RN3 and...

20060199804 - Compounds: d

20060199801 - Heterobicyclic compounds used as fungicides: R2 is halogen, cyano, C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-haloalkenyl, C2-C6-alkynyl, C3-C8-cycloalkyl, C5-C8-cycloalkenyl, OR6, SR6 or NR7R8; and the agriculturally acceptable salts of the compounds I, crop protection compositions comprising at least one compound of the formula I and/or an agriculturally acceptable salt of I and at least one solid or liquid...

20060199802 - Pyridyl derivatives and their use as therapeutic agents: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (1): wherein: W is —O—, —N(R1)—, C(O), S(O)t ; (where t is 0, 1 or 2), N(R1)S(O)2, S(O)2N(R1) ,...

20060199808 - Method of synthesis and isolation of solid n-desmethylclozapine and crystalline forms thereof: Disclosed herein are crystalline Forms A, B, C, D, and E of N-desmethylclozapine, methods of preparing the same, pharmaceutical compositions comprising the same, and methods of therapeutic treatment involving N-desmethylclozapine polymorphic forms....

20060199805 - Pharmaceutical compositions for the treatment and/or prevention of anxiety disorders: The invention relates to new pharmaceutical compositions for the treatment and/or prevention of anxiety disorders and methods for the preparation thereof. In a preferred embodiment, the instant invention is directed to pharmaceutical combinations comprising flibanserin as one active ingredient in combination with at least one additional active ingredient for the...

20060199806 - Pyrrolobenzodiazepine arylcarboxamides and derivatives thereof as follicle-stimulating hormone receptor antagonists: This invention provides pyrrolobenzodiazepine arylcarboxamides selected from those of Formula (1), which act as follicle stimulating hormone receptor antagonists, as well as pharmaceutical compositions and methods of treatment...

20060199807 - Use of n-desmethylclozapine to treat human neuropsychia tric disease: Disclosed herein is a method to treat neuropsychiatric diseases including psychosis, affective disorders, dementia, neuropathic pain, and glaucoma. Treatment is carried out by administering a therapeutically effective amount of N-desmethylclozapine to a patient suffering from a neuropsychiatric disease....

20060199809 - Factor xa compounds: s

20060199810 - Muscarinic agonists: The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment...

20060199811 - Method of treatment for preventing or reducing tumor growth in the liver of patient: A method of treatment for preventing or reducing tumor growth in liver of a patient includes administering to the patient an effective about of taurolidine, taurultam or a mixture thereof, so as to prevent or reduce the tumor growth in the patient....

20060199812 - Method of conjugating aminothiol containing molecules to vehicles: The present invention relates to a novel chemical process that provides novel vehicle derivatives that are exceptional 1,2- or 1,3-aminothiol specific reagents for conjugation to unprotected targeted compounds (e.g., polypeptides, peptides, or organic compounds) having or modified to have a 1,2- or 1,3 aminothiol group. The invention further relates to...

20060199813 - Tetrahydroquinoline analogues as muscarinic agonists: The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment...

20060199816 - Aryl sulfonyl piperidines: e

20060199814 - Chemical intermediate: Compounds of Formula I, wherein R2 represents C1-6 alkyl (optionally substituted by one or more substituents selected from —OH, halo, cyano, nitro and aryl) or aryl, wherein each aryl and aryloxy group, unless otherwise specified, is optionally substituted, and methods of preparation thereof are disclosed....

20060199815 - Nk1 antagonists: wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough....

20060199817 - Phthalazine, aza- and diaza-phthalazine compounds and methods of use: wherein A1, A2, B, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates...

20060199819 - Inhibition of cyclooxygenase-2 activity: The present invention provides new methods for inhibiting the activity of the enzyme cycloxygenase-2 (or COX-2). Inhibitors of COX-2 are known to be useful anti-inflammatory, analgesic and anti-angiogenic agents. The compounds in the present case are heterocyclic substituted 4-aminoglutarimides. Methods of using the compounds to inhibit prostaglandin synthesis are claimed....

20060199818 - 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...

20060199821 - Heterocyclic amides and sulfonamides: The invention is directed to compounds and methods to inhibit p38 kinase wherein the compounds are a pyrimidine or pyridine coupled to two mandatory substituents....

20060199820 - Human adam-10 inhibitors: The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to...

20060199822 - Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors: e

20060199823 - Heteroaryl fused pyridines, pyrazines and pyrimidines as crf1 receptor ligands: Substituted heteroaryl fused pyridine, pyrazine, and pyrimidine compounds that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and...

20060199824 - Therapeutic agents useful for treating pain: b

20060199825 - Inhibitors of macrophage migration inhibitory factor and methods for identifying the same:

20060199826 - Cyclopropane compounds and pharmaceutical use thereof: wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X1 is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom,...

20060199827 - Inhibitors of macrophage migration inhibitory factor and methods for identifying the same: e

20060199828 - Pyrazine-2-carboxyamide derivatives:

20060199829 - Inhibitors of histone deacetylase: Disclosed are compounds of formula I that inhibit histone deacetylase (HDAC) enzymatic activity, pharmaceutical compositions comprising such compounds, as well as methods to treat conditions, particularly proliferative conditions, mediated at least in part by HDAC, wherein A, W, W1, W2, Ar2, and G are described herein....

20060199830 - N-(4-(4-methylthiazol-5-yl) pyrimidin-2-yl)-n-phenylamines as antiproliferative compounds: The present invention relates to 2-substituted 4-heteroaryl-pyrimidines, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders such as cancer, leukaemia, psoriasis and the like....

20060199831 - Injectable pharmaceutical compositions of an anthracenedione derivative with anti-tumoral activity: Injectable pharmaceutical compositions containing 6,9-bis[(2-aminoethyl)amino]benzo[g]isoquinoline-5,10-dione dimalcate as active ingredient in the form of a lyophilised powder with a carrier selected from lactose and dextran, mixed with sodium chloride....

20060199833 - Novel chemiluminescent compounds and their use: The present invention relates to novel chemiluminescent compounds, to a method for synthesizing these compounds, to derivatives and conjugates comprising these compounds, to the use of these compounds or conjugates thereof in chemiluminescence based assays, especially in immunoassays....

20060199834 - Oxepane isomer of 42-o-(2-hydroxy)ethyl-rapamycin: The invention provides a purified oxepane isomer of 42-O-(2-hydroxy)ethyl-rapamycin (SDZ-RAD Isomer C), a chemical process for its preparation, as well as pharmaceutical compositions and packs containing SDZ-RAD Isomer C and methods for its use as an immunosuppressive, anti-inflammatory, antifungal, antiproliferative and antitumor agent....

20060199832 - Use of non-immunosupressive pipecolic acid derivatives for inducing chondrogenic differentiation: A non-immunosuppressive pipecolic acid derivative having an affinity for FKBP-type immunophilins is provided for inducing chondrogenic differentiation. Composition containing such compounds is also disclosed....

20060199835 - Neuroprotective and anti-proliferative compounds: This invention features compounds of formula (I), (II) and (III), which are useful in the treatment of proliferative disorders characterized by loss of growth or cellular differentiation control including, but not limited to, cancer and inflammation. Formulas (I), (II), (III) have functional groups designated as A1, A2, B1, B2, X1—X9...

20060199836 - Novel thienopyridine compounds, and methods of use thereof: The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF)....

20060199837 - Substituted tetrahydro-1h-pyrazolo [3,4-c]pyridines compositions comprising them, and use: Substituted tetrahydro-1H-pyrazolo[3,4-c]pyridines, compositions comprising them and use. The present invention relates in particular to novel substituted tetrahydro-1H-pyrazolo[3,4-c]pyridines having therapeutic activity, which can be used in particular in oncology....

20060199839 - Quinolinone compounds as 5-ht4 receptor agonists: 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....

20060199838 - Substituted n-aryl benzamides and related compounds for treatment of amyloid diseases and synucleinopathies: Substituted n-aryl benzamides, related compounds and their pharmaceutically acceptable derivatives, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, including Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's...

20060199840 - Chemical derivatives and their application as antitelomerase agent: The present invention relates to cancer therapy and to novel anticancer agents having a mechanism of action which is quite specific. It also relates to novel chemical compounds as well as their therapeutic application in humans....

20060199841 - Pharmaceutical combination for the treatment of spasticity and/or pain: The present invention relates to a pharmaceutical combination for the treatment of spasticity and/or pain characterized by that the combination contains as active ingredient 70-95% w/w compound of formula (I), wherein R represents a methyl or ethyl group, and 5-30% w/w dextromethorphan (chemical name: (+/−)-3-methoxi-17-methylmorphinan)....

20060199842 - Selective serotonin 2a/2c receptor inverse agonists as therapeutics for neurodegenerative diseases: Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP...

20060199843 - Methods for treatment and management of brain cancer using 1-oxo-2-(2,6-dioxopiperidin-3-yl)-4-methylisoindoline: 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...

20060199844 - Methylene urea derivatives: The present invention relates to methylene urea derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a...

20060199845 - Thiophene compounds for inflammation and immune-related uses: e

20060199846 - Certain substituted ureas as modulators of kinase activity: Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non-covalent complexes, prodrugs, and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are also provided...

20060199847 - Stable ammonium salts of alpha-liponic acid, the production thereof and the use of the same: The invention relates to ammonium salts of α-liponic acid of general formula (I): (Lp) (A), formed from α-liponic acid (Lp) and amino compounds (A)=of general formula (II) or general formula (III). The invention also relates to a method for producing said salts, and to the use of said salts as...

20060199848 - Ion channel modulating activity ii: Methods, compositions, dosing regimes, and routes of administration for the treatment or prevention of arrhythmias. In these methods, arrythmias (e.g. atrial fibrillation, atrial flutter, early afterdepolarizations and prolongation of QT interval) may be reduced or eliminated by administering ion channel modulating compounds to a subject in need thereof. The ion...

20060199849 - Solid lercanidipine free base: The invention provides substantially pure lercanidipine free base, having a purity of at least 95%, preferably at least 97%, more preferably at least 99%, and still more preferably at least 99.5%. The lercanidipine free base of the present invention is formed as an amorphous solid that is easily handled and...

20060199850 - Insecticidal, acaricidal, and fungicidal nitromethylene compounds: e

20060199851 - Novel compounds that are useful for improving pharmacokinetics:

20060199852 - Process for the preparation of substituted benzoxazole compounds: The present invention relates to processes for the preparation of substituted benzoxazole compounds, and in particular 2-(3-fluoro-4-hydroxy-phenyl)-7-vinyl-benzoxazol-5-ol. The processes include the vinylation of a substituted benzoxazole compound having an appropriate substitutable moiety....

20060199853 - Analogs of 4-hydroxyisoleucine and uses thereof: The invention relates to analogs of 4-hydroxyisoleucine, and to lactones, pharmaceutically acceptable salts, and prodrugs thereof, to processes for their preparation, and to pharmaceutical compositions comprising the same. The analogs of the invention stimulate both glucose uptake and insulin secretion, and may thus be useful for the prevention and treatment...

20060199856 - Novel compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents: The present invention relates to a novel compounds that can be used as anti-inflammatory, immunomodulatory and antiproliferatory agents. In particular, the invention refers to new compounds which inhibit dihydroorotate dehydrogenase (DHODH), a process for their manufacture, pharmaceutical compositions containing them and to their use for the treatment and prevention of...

20060199855 - Process for producing atorvastatin hemicalcium: (c) adding a base of formula NR1R2R3 wherein R1, R2 and R3 are independently selected from H, substituted or non-substituted C1 to C7 alkyl, C6 to C9 aryl, C8 to C10 aralkyl or aminoalkyl to form atorvastatin base salt, (d) isolating by precipitation of the above atorvastatin base salt and...

20060199854 - Process for the preparation of n-substituted 2-cyanopyrrolidines: The present invention relates to a process for the preparation of a N—(N′-substituted glycyl)-2-cyanopyrrolidine comprising at least (a) reacting, in the presence of dimethylformamide, a compound of formula (V) wherein, independently of each other, X1 and X3 are halogen; X2 is halogen, OH, O—C(═O)—CH2X3, —O—SO2—(C1-8)alkyl or —O—SO2-(aryl), with L-prolinamide, followed...

20060199857 - Therapeutic agents: Substituted 3-phenylpropionic acid derivatives, processes for preparing such compounds, their utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, methods for their therapeutic use and pharmaceutical compositions containing them....

20060199858 - Substituted benzopyrans as selective estrogen receptor-beta agonists: The present invention relates to substituted benzopyran derivatives, stereoisomers, and pharmaceutical acceptable salts thereof and processes for the preparation of the same. The compounds of the present invention are useful as Estrogen Receptor ? agonists. Such agonists are useful for the treating Estrogen Receptor ? mediated diseases such as prostate...

20060199859 - Topical medicaments and methods for photodynamic treatment of disease: New photodynamic, topically-applicable medicaments and certain medical uses of such photodynamic medicaments for treatment of human or animal tissue are described, wherein a primary active component of such medicaments is a halogenated xanthene. The halogenated xanthenes constitute a family of potent photosensitizers that become photoactivated upon illumination of the treatment...

20060199861 - Methods of using derivatives of (-)-venlafaxine: Methods of preparing, and compositions comprising, derivatives of (−)-venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depression, bipolar and manic disorders, attention deficit disorder, attention deficit disorder with hyperactivity, Parkinson's disease, epilepsy, cerebral function disorders,...

20060199860 - Salts of (-)-o-desmethylvenlafaxine: Methods of preparing, and compositions comprising, derivatives of (−)-venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depression, bipolar and manic disorders, attention deficit disorder, attention deficit disorder with hyperactivity, Parkinson's disease, epilepsy, cerebral function disorders,...

20060199862 - Method for enhancing cognitive function: t

20060199863 - Product containing prostaglandin: For the purpose of the storage in a stable manner of an aqueous liquid preparation containing a prostaglandin derivative that is liable to be adsorbed on a container and slightly soluble in water, an object of the present invention is to inhibit the decrease of the content of the prostaglandin...

20060199864 - Selection of ph-dependent compounds for in vivo therapy: This invention is in the area of improved methods for the selection of pH dependent compounds to be used before, during or after a pH-lowering event as a means to minimize or prevent tissue damage....

20060199865 - Synergistic combination comprising roflumilast and (r,r) - formoterol: The invention relates to the combined administration of roflumilast and R,R-formoterol for the treatment of respiratory tract disorders....

20060199867 - Ambroxol for the treatment of chronic pain: The invention relates to the use of ambroxol and the pharmacologically acceptable salts thereof for preparing a pharmaceutical composition for the treatment of diseases which are based on a powerful activation of voltage-dependent sodium channels, particularly for the treatment of chronic pain....

20060199866 - Combination of desoxypeganine and mecamylanine for the treatment of alcohol abuse: An active substance combination comprising deoxypeganine or of one of its pharmaceutically acceptable derivatives and mecamylamine or one of its pharmaceutically acceptable derivatives. The active substance combination serves to produce a medicament for the treatment of alcohol abuse and/or alcohol dependence....

20060199868 - Use of beta-adrenoceptor antagonists for the manufacture of a medicament for the treatment of disorders of the outer retina: Compositions and methods for treating disorders of the outer retina with β-adrenoceptor antagonists are disclosed....

20060199869 - Lipase-colipase inhibitor: The present invention relates to novel colipase-lipase inhibitors of the general formulae to be used in the treatment of prophylaxis of obesity, as well as pharmaceutical compositions containing the same, and method for treating obesity using said compounds....

20060199870 - Method for producing aqueous ortho-phthalaldehyde solutions: A method for producing aqueous ortho-phthalaldehyde solutions which comprises introducing an acetal of the o-phthalaldehyde into water and subsequently setting a pH <7 by adding an acid, whereupon, then at a temperature between 10° C. and 90° C., the acetal is converted into the o-phthalaldehyde by eliminating the corresponding alcohol,...