Abstract: Cycloalkyl acid derivatives, a preparation method thereof, and a pharmaceutical application thereof are described. In particular, a cycloalkyl acid derivative represented by general formula (I) and a medical salt thereof, a preparation method thereof, and an application of the cycloalkyl acid derivative and the medical salt thereof as URAT1 inhibitors, and particularly as therapeutic agents for diseases related to an abnormal uric acid level are described, wherein definitions of substituent groups in general formula (I) are the same as the definitions in the specification.

Abstract: Provided herein are compounds which mediate the activity of monoacyglycerol lipase (MAGL). Also provided are pharmaceutical compositions comprising a compound provided herein, and methods for treating, preventing and/or managing a MAGL mediated condition using a compound or pharmaceutical composition as provided herein.

Abstract: The present invention relates to maleate salt forms of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, methods of preparing crystalline maleate salt forms, the associated compounds, and pharmaceutical compositions containing the same. The maleate salts are useful in treating cancers, particularly those affected by kinases of the epidermal growth factor receptor family.

Abstract: The present invention relates to the biocatalyzed synthesis of enantiomerically pure (3R) and (3S)-methyl-1,2,3,4-tetrahydroquinoline. Said enantiomerically pure compounds are useful as chiral synthons in organic synthesis and, in particular, for the preparation of diastereomerically pure (21R) and (21S)-agratroban and its analogs. New compounds used as intermediates in the process of the invention are also disclosed.

Abstract: The present invention relates to a morphinan derivative represented by the following general formula (I), wherein R1 represents hydrogen, C1-6 alkyl, C6-10 aryl, etc., R2 and R3, which are the same or different, represent hydrogen, hydroxy, etc., R4 and R5 represent hydrogen, C1-6 alkyl, etc., R6 represents hydrogen, hydroxy, C1-6 alkyl, etc., X represents O or CH2, Y represents C?O, C(?O)O, etc., and m and n, which are the same or different, represent an integer of 0 to 2 (m and n are not 0 at the same time), a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof, as well as an analgesic, antianxiety drug, etc. containing the same as an active ingredient.

Abstract: The invention relates to inhibitors of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation disorders and cancers, having the Formula: where Y1, X1, X2, Y2, W1, W2, W3, and R1-R5 are described herein.

Abstract: The invention relates to inhibitors of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation disorders and cancers, having the Formula: where A, B, U, V, Z, W1, W2, W3, and R1-R6 are described herein.

Abstract: The present application provides novel compounds having anti-cancer or anti-Helicobacter pylori activity, pharmaceutical compositions and method for producing and using the novel compound.

Abstract: Disclosed are compounds having the formula: wherein R1, R2, R3 and Z are as defined herein, and methods of making and using the same.

Abstract: The present invention is directed to compounds of formula (I): pharmaceutical compositions, and methods of use for treating, reducing a symptom of or reducing the risk of macular degeneration.

Abstract: This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.

Abstract: It is intended to provide a therapeutic agent and/or a preventive agent for a respiratory disease or a therapeutic agent and/or a preventive agent for a sodium channel associated disease.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R9, R10 and R11 are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: The present disclosure describes bicyclic aromatic carboxamide derivatives, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.

Abstract: The present invention provides novel intermediates of ivacaftor and process for its preparation. The present invention also provides process for the preparation of ivacaftor and pharmaceutically acceptable salt thereof using novel intermediates.

Abstract: The present invention is directed to crystalline addition salts of (i) 8-hydroxyquinolin-2(1H)-one derivatives and (ii) a hydroxycarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvates thereof.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, A1, A2, A3, m, n and p are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: Compounds of formula (I) can modulate the activity of autotaxin (ATX).

Abstract: This invention relates to methods for preparation of chemical compound 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[(4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl]-4-oxo-3-quinolinecarboxylic acid, which comprise addition of heterocyclic amine containing protecting group, to ethyl-3-oxo-3-(2,4,5-trifluoro-3-methoxyphenyl)propanoate, followed by interaction with triethyl orthoformate, addition of cyclic amine, subsequent cyclization and formation of target product. The method for preparation claimed is technologically simple in comparison with analog and requires no special complex technical operations, which in its turn simplifies method for preparation of this chemical compound, and reduces cost of the final product, while the commercial production utilizing the method claimed has low degree of environmental threat.

Abstract: An organic carboxylic acid salt of 2-[(3S,4R)-1-{[2-chloro-6-(trifluoromethyl)phenyl]methyl}-3-{[1-(cyclohex-1-en-1-ylmethyl) piperidin-4-yl]carbamoyl}-4-methylpyrrolidin-3-yl]acetic acid and a crystal thereof.