Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.

Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: (Aza)indolizine derivatives represented by Formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, salts thereof or the like. In Formula (I), 0 to 2 of X1, X2, X3 and X4 are a nitrogen atom and the others are CR1; one of T1 and T2 represents cyano and the other represents a group represented by Formula (A), with the proviso that when T1 is cyano, at least one of X1 to X4 is a nitrogen atom; R1 independently represents a hydrogen atom, a halogen atom, a hydroxy group, C1-6 alkyl, C1-6 alkoxy or the like; ring U represents a benzene ring or the like; m represents integral number from 0 to 2; R2 independently represents a fluorine atom, a hydroxy group or the like.

Abstract: Substituted pyrazolophenyl-benzenesulfonamide compounds of formula (I) are described, wherein m, R1, R2, R3, and R4 are defined in the description, which modulate the activity of protein kinases, These compounds find utility in treating diseases caused by deregulated protein kinase activity, such as cancer and cell proliferative disorders.

Abstract: The present invention provides novel pyrrolo[3,2-c]pyridine derivatives or pharmaceutically acceptable salts thereof, processes for the preparation thereof, and compositions comprising the same. The pyrrolo[3,2-c]pyridine derivatives or pharmaceutically acceptable salts thereof of the present invention have excellent proton pump inhibition effects and possess the ability to attain a reversible proton pump inhibitory effect.

Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene)-heterocyclopenta[b]pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

Abstract: New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

Abstract: The present invention relates to sulfamoyl benzoic acid heterobicyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.

Abstract: The present invention relates to compounds of formula (I) wherein A is C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C2-C6-alkenyl, C2-C6-halo-alkenyl, C3-C6-cycloalkyl, aryl-C1-C4-alkyl, aryl-C2-C4-alkenyl, aryl or hetaryl; is a single or double bond; X1 and X2 are N, CRx1, NRx2 or CRx3Rx4; Rx1, Rx3 and Rx4 are H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, etc. or two geminal radicals Rx3 and Rx4 together with the carbon atom to which they are bound may form a carbonyl group or a 3- to 6-membered carbocyclic or heterocyclic spiro-annulated ring; Rx2 is hydrogen, C1-C6-alkyl, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; or two vicinal radicals Rx1, Rx2, Rx3 or Rx4 together with X1 and X2 form a five- or six-membered carbocyclic or heterocyclic fused ring; Y1, Y2 and Y3 are N or CRy; Ry is H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.

Abstract: The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.

Abstract: A method for making the compound is set forth utilizing the starting material

Abstract: Provided are compounds having an inhibitory effect on kinases including Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders that comprise the inhibition of Mixed Lineage Kinases.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, A, E, G and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful as inhibitors of hormone sensitive lipase (HSL) and may be used for the treatment of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis, obesity, cardiovascular diseases, myocardial dysfunction, inflammation, non-alcoholic fatty liver disease or non-alcoholic steatohepatitis.

Abstract: The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.

Abstract: Heterocyclic compounds, pharmaceutical agent and methods thereof, having superior pharmacological action and/or physicochemical properties, which are useful for the prophylaxis or treatment of circulatory diseases such as hypertension, cardiac diseases, arteriosclerosis, renal diseases and cerebral apoplexy and/or metabolic diseases such as hyperlipidemia, obesity and diabetes and/or central nervous disorders such as cerebral infarction, and/or mental diseases such as dementia depression and depression.

Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract: The heterocyclic alkynyl benzene compounds of formula (I), their pharmaceutically acceptable salts and stereoisomers thereof, as well as application in preparing drugs for preventing or treating tumors. The compounds can overcome the clinically induced resistance against Gleevec.

Abstract: The present invention relates to compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R7, A and HET are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Abstract: This invention relates to the use of imidazole, triazole, and tetrazole derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of imidazoles, triazoles, and tetrazoles in the treatment of cancer.

Abstract: The invention relates to compounds of Formula (1) and to processes for the preparation of intermediates used in the preparation of compositions containing and the uses of such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.

Abstract: The invention relates to an improved process for preparing pradofloxacin, in which the substituent in the 7 position is introduced by nucleophilic substitution in an N-methylpyrrolidone-ethanol solvent mixture.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, A, X1, X2, X3, X4, R1, R2, R3a, R3b, R4a and R4b are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

Abstract: The present invention is directed to alkoxy tetrahydro-pyridopyrimidine compounds of formula I, which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

Abstract: The present invention provides a compound, that is a 1-({halo-2-[(2-hydrocarbyl or substituted hydrocarbyl)oxy]phenyl}methyl)-(fused bicyclic nitrogen heteroaryl) carboxylic acid or an ester or sulfonamide thereof. The compound may be represented by the following formula Wherein R1, R2, R3, R4 A, X, W, Z and Y are as defined in the specification. The compounds may be administered to treat DP, FP, EP1, TP and/or EP4 receptor-mediated diseases or conditions.

Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.

Abstract: The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. Specially, the present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or salt thereof, and a medicament containing the compound or a prodrug thereof, which is an Smo inhibitor or an agent for the prophylaxis or treatment of cancer.

Abstract: The present invention relates to fused pyrrolidino-cyclopropane derivatives according to formulae (I) to (IV) as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11-?-HSD-1) and the use of such compounds for the treatment and/or prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.

Abstract: The present disclosure relates to compounds useful as agonists of the cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders, either alone or in combination therapy. The compounds of the invention have Formula (I).

Abstract: Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or conditions and/or c-fms-mediated diseases or conditions, and methods for the use thereof.

Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.

Abstract: The present invention provides a compound which has the effect of PDE 10A inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on.

Abstract: Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system.

Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):

Abstract: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.

Abstract: This invention provides compounds of formula IB: and also provides compounds of formulas ID, IIB, VB, and IIC: wherein HY, R1, R2, G5, G6, G7, G8, and G9 are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

Abstract: The present invention provides deuterium-enriched heteroaryl-containing urea compounds (I) and use of the same for treating conditions mediated by protein kinase such as

Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.

Abstract: The present invention relates to 7-azaindole derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD-1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.

Abstract: The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling.

Abstract: Disclosed are compounds of Formula (I): useful for treatment of autoimmune and inflammatory diseases associated with IL-2 inhibition via modulation of calcium release-activated calcium (CRAC) channels. Also disclosed are methods of making and using the compounds for treatment of diseases associated with CRAC channels.

Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.

Abstract: Disclosed are compounds of Formula (I): useful for treatment of autoimmune and inflammatory diseases associated with IL-2 inhibition via modulation of calcium release-activated calcium (CRAC) channels. Also disclosed are methods of making and using the compounds for treatment of diseases associated with CRAC channels.

Abstract: An (aza)indole derivative substituted in position 5, of formula (I) in which X, Y, Z, G1, G2, G3, R1, W, and R2 have the meanings given in the description, a pharmaceutical composition comprising it, and also intermediate compounds and a preparation process therefor.

Abstract: The present invention relates to a novel dicarboximide derivative of berbamine represented by formula I, including, but not limited to, a phthalimide derivative of berbamine and an aromatic heterocyclic dicarboximide derivative of berbamine, or a pharmaceutically acceptable salt thereof, to a process for preparation of the same, to a pharmaceutical composition comprising said compound and to use thereof in manufacture of an antitumor medicament.

Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.

Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

Abstract: The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R9, Ar, Q1, Q2 and Q3 are each as defined below. The compounds of the formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of the formula I and to the use thereof as a medicament.

Abstract: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a preventive or a remedy for allergic diseases such as asthma, atopic dermatitis and allergic rhinitis.

Abstract: A method and composition for treating cancer cells that targets fructose-1,6-biphosphataseenzymes (FBPs, type 1 and type 2) and/or their respective pathways. In one embodiment, inhibitors of FBPs or FBPs pathways are administered to a patient to treat brain cancer metastasis. In another embodiment, the present invention is particularly well suited for treating cancer cells that generally survive under glucose-independent conditions, or any other condition where cancer cells produce glucose via FBPs mediated pathways.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, A1, A2, A3, A4, A5 and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful, for example, as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.