21st week of 2012 patent applcation highlights part 52 |
Patent application number | Title | Published |
20120129816 | ARYL SULFONAMIDE AMINE COMPOUNDS AND THEIR USE AS 5-HT6 LIGANDS - The present invention relates to novel aryl sulfonamide amine compounds of the formula (I), their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates described herein and pharmaceutically acceptable compositions containing them. | 2012-05-24 |
20120129817 | COMBINATION TREATMENT FOR DIABETES MELLITUS - The subject matter of this application is directed to combinations of (2R,4aR,10bR)-6-(2,6-Dimethoxy-pyridin-3-yl)-9-ethoxy-8-methoxy-1,2,3,4,4a,10b-hexahydrophenanthridin-2-ol with other active compounds for the treatment of diabetes mellitus type 2 and/or type 1. | 2012-05-24 |
20120129818 | Compositions and Methods for Treatment of Cardiovascular Disease - Ortho methoxy phenolic compounds are provided that include methylenedioxyphenyl ferulate and ferulylproline and derivatives thereof. Pharmaceutical compositions comprising the compounds and methods of using the compounds for treating cardiovascular diseases, including hypertension, atherosclerosis, coronary heart disease, angina, stroke, and myocardial infarction, are further provided. The compounds are also useful in reducing low-density lipoprotein oxidation, improving or increasing vasodilation, and reducing plaque destabilization in a subject. | 2012-05-24 |
20120129819 | GEL COMPOSITIONS FOR ADMINISTRATION OF PHARMACEUTICALLY ACTIVE COMPOUNDS - The present invention provides a pharmaceutical composition in the form of a water-based gel comprising: at least one pharmaceutically active compound; at least one gelling agent; a solubilising agent; and water, wherein said composition is free or substantially free of unsubstituted monohydric alcohols having between 1 and 6 carbon atoms. The invention also relates to methods for preparing the compositions and uses thereof. | 2012-05-24 |
20120129820 | NEW PHARMACEUTICAL COMPOSITIONS FOR TREATMENT OF RESPIRATORY AND GASTROINTESTINAL DISORDERS - The present invention provides pharmaceutical compositions comprising one or more CRTH2 antagonists 1 and one or more further active compounds 2. | 2012-05-24 |
20120129821 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 2012-05-24 |
20120129822 | COMPOSITION CONTAINING DIOSGENIN AND USE THEREOF TO IMPROVE AT LEAST ONE OF COGNITIVE DEFICITS ASSOCIATED WITH MENOPAUSAL SYNDROME - Disclosed herein is a composition for improving at least one of cognitive deficits associated with menopausal syndrome, which includes diosgenin. Also disclosed herein is a method for improving at least one of cognitive deficits associated with menopausal syndrome in a subject via administering the aforesaid composition. | 2012-05-24 |
20120129823 | CONTRACEPTION PROCESS AND ADMINISTRATION FORM FOR THE SAME - A method for hormonal contraception comprising administering at least one contraceptive hormone in a plurality of linked taking periods optionally having a sequence lasting several years. Each taking period comprises at least one taking cycle. Each taking cycle comprises a duration-constant taking phase lasting several days and a taking pause lasting several days. In each taking phase the hormonal component is administrated in a daily unit. In each taking pause either a placebo or no unit is administered. The duration of the taking phase or phases of at least the final taking period is at least 22 days. The duration of each taking phase in any taking period preceding a following taking period is shorter than that in each of the taking phases in each following taking period. | 2012-05-24 |
20120129824 | Pharmaceutical Formulations Containing Corticosteroids for Topical Administration - The potency of a topical corticosteroid in a pharmaceutical formulation is maintained even when the concentration of the corticosteroid is substantially reduced by providing the corticosteroid in a formulation containing a liquid oil component that includes a dicarboxylic acid ester and/or a monocarboxylic acid ester. | 2012-05-24 |
20120129825 | METHOD FOR ON-DEMAND CONTRACEPTION USING LEVONORGESTREL OR NORGESTREL - The invention relates to a method for contraception, which method comprises on-demand administering levonorgestrel or norgestrel in a woman, within 24 hours before an intercourse. | 2012-05-24 |
20120129826 | Method of Treating Depression - Methods for treatment of depression-related mood disorders in mammals, particularly humans are disclosed. The methods of the invention include administration of compounds capable of enhancing glutamate transporter activity in the brain of mammals suffering from depression. ATP-sensitive K | 2012-05-24 |
20120129827 | NOVEL DERIVATIVES OF 1-ALKYL-6-OXO-PIPERIDINE-3-CARBOXYLIC ACIDS AND 1-ALKYL-5-OXO-PYRROLIDINE-3-CARBOXYLIC ACIDS AND THEIR USES AS COOLING COMPOUNDS - The present invention relates to novel derivatives of 1-alkyl-6-oxo-piperidine-3-carboxylic acids and 1-alkyl-5-oxo-pyrrolidine-3-carboxylic acids represented by Formula I: | 2012-05-24 |
20120129828 | S1P1 RECEPTOR AGONISTS AND USE THEREOF - The present invention relates to compounds of Formula (I) that are have activity as S1P1 receptor modulating agents, more specifically to specifically compounds that are S1P1 receptor agonists. The invention also related to the use of such compounds to treat diseases associated with inappropriate S1P1 receptor activity such as autoimmune diseases. | 2012-05-24 |
20120129829 | NOVEL INDOLE MODULATORS OF S1P RECEPTORS - The present invention relates to novel indole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 2012-05-24 |
20120129830 | 7-AZA-SPIRO[3.5]NONANE-7-CARBOXYLATE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to compounds of the general formula (I) where: R | 2012-05-24 |
20120129831 | Substituted 3-(1,2,4-Oxadiazol-5-yl)-5-Phenylpiperidines - The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and tumour disorders. | 2012-05-24 |
20120129832 | AMIDE DERIVATIVE - Provided are a compound having an excellent hypoglycemic action, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause an increase in the blood sugar level due to abnormal sugar metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed. | 2012-05-24 |
20120129833 | CYCLIC KETOENOLS FOR THERAPY - The invention relates to 5′-biphenyl-substituted cyclic ketoenols for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of diabetes, obesity, hyperlipidaemia, fatty livers and of disorders of the cardiovascular system. | 2012-05-24 |
20120129834 | SEROTONIN RECEPTOR ANTAGONISTS FOR USE IN THE TREATMENT OF HUNTINGTON'S DISEASE - Methods are provided for the treatment and/or prophylaxis of Huntington's disease. In various embodiments the methods involve administration of one or more serotonin receptor antagonists. In certain embodiments the serotonin receptor antagonists include, but are not limited to loxapine, and/or a loxapine analogue, and/or cyproheptadine, and/or a cyproheptadine analogue (e.g., pizotifen). | 2012-05-24 |
20120129835 | SCHIZOPHRENIA METHODS AND COMPOSITIONS - Methods of preparing and using neural cells derived from human induced pluripotent stem cell (hiPSCs), particularly hiPSCs derived from subjects with schizophrenia are provided. The hiPSC-derived neural cells can be used to screen test compounds and to identify schizophrenia marker functions. The hiPSC-derived neural cells can be used to diagnose and/or assess the severity of schizophrenia in a subject. Further, may the hiPSC-derived neural cells from a subject be used as an in vitro system to identify the most effective candidate among existing drugs for that specific subject (i.e. personalized medicine). | 2012-05-24 |
20120129836 | Imidazole derivatives as PDE10A enzyme inhibitors - This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. | 2012-05-24 |
20120129837 | Derivatives of Fluorene, Anthracene, Xanthene, Dibenzosuberone and Acridine and Uses Thereof - Chemical agents, such as disulfonamide derivatives of fluorene, anthracene, xanthene, dibenzosuberone and acridine, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of the Wnt/β-catenin signaling pathway, and serve to reduce β-catenin levels present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents. | 2012-05-24 |
20120129838 | Composition for Preventing and Treating Alopecia Disorder Containing Morgalanthamine Compounds as an Active Ingredient - Provided are a pharmaceutical composition, a cosmetic composition and health foods for preventing and treating alopecia disorder, which include a norgalanthamine compound as an active ingredient. Since the norgalanthamine compound has an effect on growth and proliferation of dermal papilla cells that play an important role in hair growth, the norgalanthamine compound may be used for the pharmaceutical composition, the cosmetic composition and health foods, which are useful in preventing and treating alopecia disorder. | 2012-05-24 |
20120129839 | METHODS OF TREATING DISORDERS ASSOCIATED WITH PROTEIN POLYMERIZATION - The present invention relates to methods of treatment of clinical disorders associated with protein polymerization comprising administering, to a subject, an effective amount of carbamazepine, oxcarbazepine or another carbamazepine-like compound. It is based, at least in part, on the discovery that, in cells having a genetic defect in α1-antitrypsin, carbamazepine was able to decrease levels of the mutant protein. Furthermore, carbamazepine reduced the hepatic load of mutant α1-antitrypsin and the toxic effect of that mutant protein accumulation, hepatic fibrosis, in vivo using a mouse model of the disease. As patients having this defect in α1-antitrypsin exhibit toxic accumulations of the protein, treatment according to the invention may be used to ameliorate symptoms and signs of disease. | 2012-05-24 |
20120129840 | NOVEL VIRAL REPLICATION INHIBITORS - The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity. | 2012-05-24 |
20120129841 | CARBOLINE DERIVATIVES USEFUL IN THE TREATMENT OF CANCER AND OTHER DISEASES - In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and compositions, and methods for the administration and use of those compounds. provided. In one aspect of the invention, compounds useful in the inhibition of VEGF production, in the treatment of solid tumor cancer, and in reducing serum, plasma, and/or tumor VEGF levels, are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the treatment of cancer, and the reduction of plasma and/or tumor VEGF levels, using the compounds of the invention. | 2012-05-24 |
20120129842 | BISTHIAZOLE INHIBITORS OF PRO-MATRIX METALLOPROTEINASE ACTIVATION - This invention relates to bisthiazole I and its therapeutic and prophylactic uses, wherein the variables A, R | 2012-05-24 |
20120129843 | PYRIDYL-THIAZOLYL INHIBITORS OF PRO-MATRIX METALLOPROTEINASE ACTIVATION - This invention relates to thiazole I and its therapeutic and prophylactic uses, wherein the variables R | 2012-05-24 |
20120129844 | N-[5-[2-(3,5-DIMETHOXYPHENYL)ETHYL]-1H-PYRAZOL-3-YL]-4-(3,4-DIMETHYLPIPERA- ZIN-1-YL)BENZAMIDE AND SALTS THEREOF - There is provided a compound of formula (I): | 2012-05-24 |
20120129845 | Inhibitors of Bruton's Tyrosine Kinase - This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: | 2012-05-24 |
20120129846 | GAMMA SECRETASE MODULATORS - In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions. | 2012-05-24 |
20120129847 | COMPOSITIONS AND METHODS FOR TREATING OCULAR EDEMA, NEOVASCULARIZATION AND RELATED DISEASES - Disclosed are methods for the treatment of diseases or conditions of the eye, especially retinopathies, ocular edema and ocular neovascularization. Non-limiting examples of these diseases or conditions include diabetic macular edema, age-related macular degeneration (wet form), choroidal neovascularization, diabetic retinopathy, retinal vein occlusion (central or branch), ocular trauma, surgery induced edema, surgery induced neovascularization, cystoid macular edema, ocular ischemia, uveitis, and the like. | 2012-05-24 |
20120129848 | Benzo [E] [1,3] Oxazin-4-One Derivatives as Phosphoinositide 3-Kinase Inhibitors - Compounds of formula (I): wherein: W is O, N—H, N-alkyl, N-alkenyl, N-alkynyl, N-aryl, N-heteroaryl or S; each X is independently CH or N; R | 2012-05-24 |
20120129849 | DEUTERATED SERINE-THREONINE PROTEIN KINASE MODULATORS - The present invention provides deuterated compounds having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. The deuterated compounds of the invention can modulate casein kinase (CK) activity and/or poly(ADP-ribose)polymerase (PARP) activity. The invention also relates in part to methods for using such deuterated compounds as therapeutic agents. | 2012-05-24 |
20120129850 | IMIDAZOLOTHIAZOLE COMPOUNDS FOR THE TREATMENT OF DISEASE - Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases. | 2012-05-24 |
20120129851 | Substituted Quinazoline and Pyrido-Pyrimidine Derivatives - The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer. | 2012-05-24 |
20120129852 | AZAINDAZOLES AS KINASE INHIBITORS AND USE THEREOF - Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, (I) are useful as kinase modulators, including Btk modulation, wherein A | 2012-05-24 |
20120129853 | METHODS OF TREATMENT USING SELECTIVE BCL-2 INHIBITORS - This invention pertains to methods of treating systemic lupus erythematosus, lupus nephritis or Sjogren's Syndrome with compounds that selectively inhibit the activity of Bcl-2 anti-apoptotic proteins. Specifically, the current invention is directed to treatment with compounds that selectively inhibit the activity of Bcl-2 proteins, with a lesser affinity for inhibiting the activity of other BCL-2 family proteins, including Bcl-x | 2012-05-24 |
20120129854 | Pesticidal Arylpyrrolidines - The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the yield of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification. | 2012-05-24 |
20120129855 | PHTHALAZINONE DERIVATIVES - A compound of the formula (I): | 2012-05-24 |
20120129856 | COMPOUNDS, COMPOSITIONS AND METHODS USEFUL FOR CHOLESTEROL MOBILISATION - The invention relates to classes of pharmaceutically-active heterocyclic compounds and pharmaceutically acceptable salts, and hydrates thereof, and compositions comprising the same. The invention also relates to methods for treating or preventing a disease or disorder, which comprises administering a therapeutically or prophylactically effective amount a compound described herein. | 2012-05-24 |
20120129857 | Substituted sodium 1H-pyrazol-5-olate - The present application relates to sodium 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1 H-pyrazol-5-olate, to processes for its preparation, to its use for the treatment and/or prophylaxis of diseases and to its use for the preparation of medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular and haematological diseases and kidney diseases, and for promoting wound healing. | 2012-05-24 |
20120129858 | COMPOUNDS, COMPOSITIONS AND METHODS COMPRISING PYRIDAZINE SULFONAMIDE DERIVATIVES - The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-3 or encompassed by formula I-III) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease. | 2012-05-24 |
20120129859 | PREPARATION OF 1-(SUBSTITUTED BENZYL)-5-TRIFLUOROMETHYL-2(1H)PYRIDONE COMPOUNDS AND SALTS THEREOF AND THEIR APPLICATIONS - 1-(substituted benzyl)-5-trifluoromethyl-2(1H)pyridone compounds and their pharmaceutical acceptable salts are disclosed. The preparation methods of the compounds and their salts and the use of the same for preparing the medicaments for treating fibrosis are also disclosed. New pyridine compounds and their salts are obtained from trifluoromethyl pyridone as starting material. | 2012-05-24 |
20120129860 | STYRENYL DERIVATIVE COMPOUNDS FOR TREATING OPHTHALMIC DISEASES AND DISORDERS - The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are styrenyl derivative compounds, including but not limited to stilbene derivative compounds, and compositions comprising these compounds, that are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease. | 2012-05-24 |
20120129861 | COMPOSITIONS OF DIBROMOMALONAMIDE AND THEIR USE AS BIOCIDES - A biocidal composition comprising 2,2-dibromomalonamide and an aldehyde-based biocidal compound, and its use for the control of microorganisms in aqueous and water-containing systems. | 2012-05-24 |
20120129862 | PROKINETICIN 1 RECEPTOR ANTAGONISTS - The present invention relates to certain novel compounds of Formula (I): | 2012-05-24 |
20120129863 | CHYMASE INHIBITORS - Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving chymase. | 2012-05-24 |
20120129864 | SUBSTITUTED 1-ALKYLCINNOLIN-4(1H)-ONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATION OF SAME - The subject of the present invention is compounds corresponding to the formula (I) in which: X represents a divalent (C | 2012-05-24 |
20120129865 | CRYSTALLINE (8S,9R)-5-FLUORO-8-(4-FLUOROPHENYL)-9-(1-METHYL-1H-1,2,4-TRIAZOL-5-YL)-8,- 9-DIHYDRO-2H-PYRIDO[4,3,2-DE]PHTHALAZIN-3(7H)-ONE TOSYLATE SALT - Provided herein are (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt forms, including crystalline forms, and methods of their preparation. Pharmaceutical compositions comprising a (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt are also provided, as are methods of using (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt to treat a disease or condition, such as a cancer. | 2012-05-24 |
20120129866 | METHODS FOR PREVENTING OR TREATING METABOLIC DISEASES, INFLAMMATORY DISEASES, AUTOIMMUNE DISEASES, ALLERGIC DISEASES, CENTRAL NERVOUS SYSTEM DISEASES, CARDIOVASCULAR DISEASES, HOMEOSTASIS-RELATED DISEASES OR GLAUCOMA - A method for preventing or treating a metabolic disorder, an inflammatory disease, an autoimmune disease, an allergic disease, a central nervous system disease, a cardiovascular disease, a homeostasis-related disease or glaucoma, involving administering a compound or a salt thereof, the compound having the following formula (1) | 2012-05-24 |
20120129867 | INHIBITORS OF PROTEIN KINASES - The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. | 2012-05-24 |
20120129868 | POLY (ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS - Compounds of the following formula are provided for use with PARP: | 2012-05-24 |
20120129869 | PHOSPHORYLATION AND MUTATIONS OF ANAPLASTIC LYMPHOMA KINASE AS A DIAGNOSTIC AND THERAPEUTIC TARGET IN LUNG CANCER - The invention related to the use of high-density loss of heterozygosity (LOH) mapping in lung adenocarcinoma to identify intragenic LOH and driver mutations in different domains of ALK resulted in enhanced tumor growth in xenografted mouse. Mutant (H694R and E1384K) ALKs showed activation of Y1604 ALK and downstream AKT, STAT3 and ERK signaling pathways. Increases of oncogenic signalings resulted in enhanced cell proliferation, colony-formation, cell-migration and tumor-growth in xenografted mouse. Western blot and immunohistochemistry analysis using antibody against phospho-Y1604 ALK on 11 lung cancer cell-lines and 263 cancer specimens indicated ALK activation in all lung cancers regardless of tumor stages. Treating mutant-bearing mice with ALK inhibitor WHI-P 154 resulted in tumor shrinkage, metastasis suppression, and improved survival. Hyperphosphorylation of Y1604 ALK occurred early and continuously throughout tumor progression and could be used as a biomarker to detect lung cancer. Oncogenic ALK point mutations could be treatment targets for lung cancer. | 2012-05-24 |
20120129870 | PIPERAZINYL DERIVATIVES USEFUL AS MODULATORS OF THE NEUROPEPTIDE Y2 RECEPTOR - The present invention is directed to piperidinyl and piperazinyl derivatives of formula (II) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and/or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor. | 2012-05-24 |
20120129871 | Crystalline form of an inhibitor of MDM2/4 and p53 interaction - A crystalline form of (S)-1-(4-Chloro-phenyl)-7-isopropoxy-6-methoxy-2-(4-{methyl-[4-(4-methyl-3-oxo-piperazin-1-yl)-trans-cyclohexylmethyl]-amino}-phenyl)-1,4-dihydro-2H-isoquinolin-3-one, which is useful in the treatment of a disease or disorder associated with the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively, | 2012-05-24 |
20120129872 | FUSED HETEROARYL INHIBITORS OF PRO-MATRIX METALLOPROTEINASE ACTIVATION - This invention relates to thiazole I and its therapeutic and prophylactic uses, wherein the variables A, Q, J, R | 2012-05-24 |
20120129873 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 2012-05-24 |
20120129874 | SALT FORMS OF ORGANIC COMPOUND - The present invention relates to novel salt forms of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, a DPP-4 inhibitor and their use in pharmaceutical compositions useful in the treatment of type 2, diabetes, as well as their production. | 2012-05-24 |
20120129875 | SUBSTITUTED QUINAZOLINES AS FUNGICIDES - The present invention relates to a compound of formula (I) wherein the substituents have the definitions as defined in claim | 2012-05-24 |
20120129876 | [4-(6-FLUORO-7-METHYLAMINO-2,4-DIOXO-1,4-DIHYDRO-2H-QUINAZOLIN-3-YL)-PHENY- L]-5-CHLORO-THIOPHEN-2-YL-SULFONYLUREA SALTS, FORMS AND METHODS RELATED THERETO - The present invention provides novel sulfonylurea salts of a salt of formula (I) | 2012-05-24 |
20120129877 | USE OF QUINAZOLINE DERIVATIVES FOR NEURODEGENERATIVE DISEASES - The present invention relates to the use of a series of quinazoline-derived compounds to produce a medicament for the treatment and/or prevention of neurological and/or neurodegenerative diseases, such as Parkinson's disease or Alzheimer's disease. The present invention also relates to a method for the treatment and/prevention of neurological and/neurodegenerative diseases comprising the administration of a therapeutically effective amount of said compounds. | 2012-05-24 |
20120129878 | TABLET - Provided is a tablet having a high content of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-4-fluorobenzonitrile (compound (A)) or a salt thereof as a pharmaceutically active component. A tablet containing compound (A) or a salt thereof, and a fluidizer, which has a compound (A) content of 35-50 weight %. | 2012-05-24 |
20120129879 | Compounds and Compositions for Use in Phototherapy and in Treatment of Ocular Neovascular Disease and Cancers - The invention relates generally to anti-angiogenesis agents and related methods of using to anti-angiogenesis agents for biomedical applications including direct monotherapy and combination therapy for treatment of an angiogenesis related condition. In an embodiment, the invention provides a class of opioid compounds and structurally related opioid derivatives exhibiting anti-VEGF activity for use in therapeutic procedures, including phototherapy. Opioid compounds and structurally related opioid derivatives of the invention may be administered alone or in combination with administration of a phototherapy agent and/or other therapeutic agent. | 2012-05-24 |
20120129880 | METHOD FOR DETERMINING SENSITIVITY TO IRINOTECAN AND USE THEREOF - To provide a method for determining the sensitivity of a patient to irinotecan, SN-38, and/or a salt thereof, which method can determine the therapeutic response of the patient and to provide a novel cancer therapeutic means employing the method. | 2012-05-24 |
20120129881 | COMBINATIONS OF THERAPEUTIC AGENTS FOR TREATING CANCER - A combination of an mTOR inhibitor compound with one or more pharmaceutically active agents, for simultaneous, concurrent, separate or sequential use for preventing or treating a proliferative disease. | 2012-05-24 |
20120129882 | Method for producing benzazoloquinolium (BQs) salts, using the composition as cellular markers, and using the biological activity of the composition - A synthesis procedure for benzazolo[3,2-a]quinolinium chloride salts and the inclusion of chloro-substituent, amino-substituent, and nitro-substituent resulting in several compounds wherein said procedures provides an increment in the compounds biological activity. The compounds are further used for intra cellular binding, cytotoxicity on malignant cells through apoptosis activation mediated by mitochondrial damage, cellular organelles binding and damage, DNA fragmentation, marker of bacterial growth, antibacterial activity, cell cycle disruption, and a marker due to the auto-fluorescent properties. | 2012-05-24 |
20120129883 | BENZENESULFONYL OR SULFONAMIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO THE MODULATION OFTHE SEROTONIN 5-HT6 RECEPTOR - The present invention relates to benzenesulfonyl or sulfonamide compounds of formulae IA and IB | 2012-05-24 |
20120129884 | PHOTOCHEMOTHERAPEUTIC HETEROCYCLIC AGENTS HAVING ANTIPROLIFERATIVE AND ANTINEOPLASTIC ACTIVITY - The present invention concerns the synthesis of new analogs of angelicins, pyrrolo [3,2-h]quinoline, for the treatment of pathologies having hyperproliferative character included those having neoplastic nature. The treatment is based on the combined action of pyrrolo [3,2-h]quinolines and UV-A light, through a clinical approach defined as PUVA (psoralen-UVA light). The most important feature of these compounds is that they exert their remarkable photoxicity without any DNA damage, which is the main origin of the side effects of the PUVA therapy. | 2012-05-24 |
20120129885 | (2S,3R)-N-(2-((3-PYRIDINYL)METHYL)-1-AZABICYCLO[2.2.2]OCT-3-YL)BENZOFURN-2- -CARBOXAMIDE, NOVEL SALT FORMS, AND METHODS OF USE THEREOF - The present invention relates to (2S,3R)—N-(2-((3-pyridinyl)methyl)-1-azabicyclo[2.2.2]oct-3-yl)benzofuran-2-carboxamide, novel salt forms thereof, methods for its preparation, novel intermediates, and methods for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central and autonomic nervous systems. | 2012-05-24 |
20120129886 | METALLOENZYME INHIBITOR COMPOUNDS - The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes. | 2012-05-24 |
20120129887 | COMPOUNDS DERIVED FROM ARTESUNATE, PREPARATION PROCESS, PHARMACEUTICAL COMPOSITION AND USE OF THE RESPECTIVE MEDICINE - The present invention refers to new compounds represented by the general formula (I) where X is represented by the general formula (II) and Y is represented by the general formula (III). The relation X to Y may vary from 1:1 to 1:7. The radicals R | 2012-05-24 |
20120129888 | LIBRARIES OF N-(2-OXO-1-PHENYLPIPERIDIN-3-YL)SULFONAMIDES FOR DRUG DISCOVERY - Novel compounds are continually sought after to treat and prevent disorders. The invention relates to N-(2-oxo-1-phenylpiperidin-3-yl)sulfonamides useful for contributing to the search and identification of new lead compounds which can modulate the functional activity of a biological target. | 2012-05-24 |
20120129889 | Non-competitive NMDA receptor antagonists - Disclosed herein are non-competitive NMDA receptor antagonists having chemical structures similar to that of phencyclidine (PCP). These antagonists contain a polycyclic ring structure in place of the cycloalkyl ring of PCP. The antagonists also differ from PCP in that they include an electron withdrawing group, a hydroxyl group, or an amine group at the para position of the phenyl ring. The antagonists disclosed herein are useful for treating or ameliorating a symptom of ailments associated with over excitation of cells (e.g., neurons) that express NMDA receptors. Examples of ailments that can be treated and for which symptoms can be ameliorated include epilepsy, neurodegenerative disease (e.g., Alzheimer's and Parkinson's diseases), drug addiction, neuropathic pain, and neuronal and glutamate-dependent tumors. | 2012-05-24 |
20120129890 | INDOLE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - A compound (I) of the present invention, which has an EP | 2012-05-24 |
20120129891 | SULFONE DERIVATIVE - Provided are a compound having an excellent hypoglycemic action, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause an increase in the blood sugar level due to abnormal sugar metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed. | 2012-05-24 |
20120129892 | NOVEL PHARMACEUTICALLY ACCEPTABLE SALTS OF 4-(1H-IMIDAZOL-4-YLMETHYL)PYRIDINE AND THEIR THERAPEUTICAL USES - The present invention concerns novel pharmaceutical compositions of immethridine, in particular of novel pharmaceutically acceptable salts thereof, such as the dioxalate salt of immethridine, as well as its therapeutical uses and novel process of preparation. | 2012-05-24 |
20120129893 | Inhibition Of Raf Kinase Using Substituted Heterocyclic Ureas - Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se. | 2012-05-24 |
20120129894 | Alkoxy Compounds for Disease Treatment - The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease. | 2012-05-24 |
20120129895 | METHODS OF TREATMENT - The invention relates to combinations comprising a vascular disrupting agent (VDA) with IAP antagonists, for simultaneous, concurrent, separate or sequential use, especially for use in the treatment of proliferative diseases. | 2012-05-24 |
20120129896 | THIAZOLIDINEDIONE ANALOGUES FOR THE TREATMENT OF METABOLIC DISEASES - The present invention relates to thiazolidinedione analogues that are useful for treating hypertension, diabetes, and inflammatory diseases. | 2012-05-24 |
20120129897 | BIS HETEROARYL INHIBITORS OF PRO-MATRIX METALLOPROTEINASE ACTIVATION - This invention relates to thiazole I and its therapeutic and prophylactic uses, wherein the variables A, Q, J, R | 2012-05-24 |
20120129898 | PHARMACEUTICAL COMPOSITIONS FOR POORLY SOLUBLE DRUGS - The invention relates to solid dispersions of poorly soluble compounds formed by co-precipitation and hot melt extrusion, resulting in improved stability and bioavailability. The invention also relates to hot melt extrusion processes used to prepare such solid dispersions. | 2012-05-24 |
20120129899 | SYNERGISTIC ANTIMICROBIAL COMPOSITION OF 1,2-BENZISOTHIAZOLIN-3-ONE AND TRIS(HYDROXYMETHYL)NITROMETHANE - A synergistic antimicrobial composition containing 1,2-benzisothiazolin-3-one and tris(hydroxymethyl)nitromethane. | 2012-05-24 |
20120129900 | DUAL-ACTING ANTIHYPERTENSIVE AGENTS - The invention is directed to compounds of formula I: | 2012-05-24 |
20120129901 | TRITERPENOID DERIVATIVES USEFUL AS ANTIPROLIFERATIVE AGENTS - Formula (I) and (II). The present invention relates to the use of a new lupane derivative of general formula (I) or (II), or a pharmaceutically acceptable salt, crystal form, complex, hydrate, or hydrolysable ester thereof, for preventing and/or inhibiting tumor growth and for treating cancer and other proliferative diseases, more particularly for treating leukemia, liver, cervical, colon and prostate cancer. The present invention also relates to the synthesis of these compounds and to pharmaceutical compositions which contain them. | 2012-05-24 |
20120129902 | 4-SUBSTITUTED-3-PHENYLSULFANYLMETHYL-BICYCLO[3.1.0]HEXANE COMPOUNDS AS mGluR 2/3 ANTAGONISTS - A mGlu2/3 receptor antagonist of the formula: | 2012-05-24 |
20120129903 | POLYMORPHIC, CRYSTALLINE AND MESOPHASE FORMS OF SODIUM 2-(5-BROMO-4-(4-CYCLOPROPYLNAPHTHALEN-1-YL)-4H-1,2,4-TRIAZOL-3-YLTHIO) ACETATE, AND USES THEREOF - Crystalline polymorphs and solid mesophase forms of sodium 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetate are described. In addition, pharmaceutical compositions and uses of such compositions for the treatment of a variety of diseases and conditions are provided. | 2012-05-24 |
20120129904 | Liquid Formulations Of Bendamustine - Stable liquid formulations of bendamustine, and pharmaceutically acceptable salts thereof, and polar aprotic solvents, are described. | 2012-05-24 |
20120129905 | PHARMACEUTICAL COMPOSITION - To provide a pharmaceutical composition which can enhance the storage stability of 1-( | 2012-05-24 |
20120129906 | MODULATORS OF S1P RECEPTORS - The present invention relates to novel diphenylethyne derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 2012-05-24 |
20120129907 | HISTIDINOL DEHYDROGENASE INHIBITORS, AND USE THEREOF AS MEDICAMENTS - Compounds of general formula (I) below: | 2012-05-24 |
20120129908 | Agent For The Prophylaxis And Treatment Of Highly Pathogenic Infectious Diseases - The invention relates to an agent for the treatment and/or prophylaxis of highly pathogenic infectious diseases, such as highly pathogenic influenza A (in particular, subtypes H5 and H7) and severe acute respirator syndrome caused by the genotype IV coronavirus. The agent is in the form of glutaryl histamine or a pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition based on glutaryl histamine or a pharmaceutically acceptable salt thereof and to a method for the treatment and/or prophylaxis of highly pathogenic infectious diseases. | 2012-05-24 |
20120129909 | 2-AMINO-2-PHENYL-ALKANOL DERIVATIVES, PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME - Ester derivatives of 2-amino-2-phenyl-alkanol of general formula (I) in which: R | 2012-05-24 |
20120129910 | Inhibition of Apoptosis-Specific eIF-5A(elF-5A1") with Antisense Oligonucleotides and siRNA as Anti-Inflammatory Therapeutics - The present invention relates to apoptosis specific eucaryotic initiation factor 5A (eIF-5A), referred to as apoptosis-specific eIF-5A or eIF5A1, nucleic acids and polypeptides and methods for inhibiting or suppressing apoptosis in cells using antisense nucleotides or siRNAs to inhibit expression of apoptosis-specific eIF-5A. The invention also relates to suppressing or inhibiting expression of pro-inflammatory cytokines or inhibiting activation of NFkB by inhibiting expression of apoptosis-specific eIF-5A. | 2012-05-24 |
20120129911 | COMPOSITIONS AND METHODS OF TARGETING APOLIPOPROTEIN B FOR THE REDUCTION OF APOLIPOPROTEIN C-III - Disclosed herein are compositions and methods for lowering Apolipoprotein C-III (ApoC-III) in a subject in need thereof. Subjects in need of ApoC-III reduction include subjects with elevated ApoC-III levels, subjects with a condition associated with ApoC-III, subjects with diabetes, obese subjects and subjects with cardiovascular disease. Compositions to lower ApoC-III include compounds targeting Apolipoprotein B (ApoB) such as Mipomersen and other antisense compound targeting ApoB. | 2012-05-24 |
20120129912 | RNA Targeting in Alpha-Synucleinopathies - Therapies and assays to screen for small molecules that can have therapeutic use in the control of neurodegenerative diseases such as Parkinson's and other alpha-synucleinopathies. | 2012-05-24 |
20120129913 | dsRNA For Treating Viral Infection - The invention relates to double-stranded ribonucleic acids (dsRNAs) targeting gene expression of phosphatidylinositol 4-kinase (PI4K), in particular human phosphatidylinositol 4-kinase, catalytic, beta polypeptide (PIK4CB) or human phosphatidylinositol 4-kinase, catalytic, alpha polypeptide (PIK4CA), and their use for treating infection by positive stranded RNA viruses such as hepatitis C virus (HCV). Each dsRNA comprises an antisense strand having a nucleotide sequence which is less that 30 nucleotides in length, generally 19-25 nucleotides in length, and which is substantially complementary to at least a part of the PIK4CB or PIK4CA target mRNA. A plurality of such dsRNA may be employed to provide therapeutic benefit. The invention also relates to a pharmaceutical composition comprising the dsRNA together with a pharmaceutically acceptable carrier, and including a delivery modality such as fully encapsulated liposomes or lipid complexes. The invention further includes methods for treating diseases caused by positive stranded RNA virus infection using the pharmaceutical compositions; and methods for inhibiting the propogation of positive stranded RNA viruses in and between cells. | 2012-05-24 |
20120129914 | ORGANIC COMPOSITIONS TO TREAT HSF1-RELATED DISEASES - The present disclosure relates to methods of treating heat shock factor 1 (HSF1)-related diseases such as cancer and viral diseases, using a therapeutically effective amount of a RNAi agent to HSF. | 2012-05-24 |
20120129915 | ORGANIC COMPOSITIONS TO TREAT HSF1-RELATED DISEASES - The present disclosure relates to methods of treating heat shock factor 1 (HSF1)-related diseases such as cancer and viral diseases, using a therapeutically effective amount of a RNAi agent to HSF. | 2012-05-24 |