Abstract: The present invention relates to substituted pyrimidine compounds of formula I useful as orexin receptor antagonists. The invention also relates to pharmaceutical compositions containing said compounds.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as obesity, hyperlipidemia, hypercholesterolemia and diabetes and other related disorders and diseases, and may be useful for other diseases such as NASH, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and other disorders and diseases related thereto.

Abstract: Disclosed are new dihydropteridinones of the formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings provided herein, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.

Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2 L1, L2, X, Y, Q and Z have defined meanings.

Abstract: The present invention relates to compounds that inhibit HSP90 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases such as for treatment of solid tumors.

Abstract: Provided herein are compounds of the formula where A1, A2, A3, A4, L, Q, R1, R2, R3, R4, Rx, Ry, Rz, X, Y1, Y2, Y4 and Z are as described herein, and compositions thereof that are useful in the treatment of inflammatory and immune conditions and diseases. In particular, the invention provides aryl nitrile compounds which modulate the expression and/or function of a chemokine receptor.

Abstract: Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; lipid disorders; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; fatty liver disease and cancer.

Abstract: A pyridazine compound represented by formula (1): wherein R1 and R2 are same or different and represent a C1-C4 alkyl group; R3 represents a halogen atom, a nitro group, a cyano group, a C1-C4 alkyl group optionally substituted by at least one halogen atom, a C1-C4 alkoxy group optionally substituted by at least one halogen atom or a C1-C4 alkylthio group optionally substituted by at least one halogen atom; R4 and R5 each represents a halogen atom, a nitro group, a cyano group, a C1-C4 alkyl group optionally substituted by at least one halogen atom or a C1-C4 alkoxy group optionally substituted by at least one halogen atom; and m and n each represents an integer.

Abstract: Thiazole derivatives of the formula I in which R1, R2, R3, V, W, X and B are as defined in claim 1, act as phosphodiesterase IV inhibitors and can be employed for the treatment of osteoporosis, tumors, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases and AIDS.

Abstract: The present invention provides a compound represented by the formula (I): wherein ring A is void or a benzene ring optionally having substituent(s), R1 and R2 are each independently a phenyl group optionally having substituent(s), a cyclohexyl group and the like, R3 and R4 are each independently a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group and the like, and X is a residue represented by —OR5 or —NHR6 wherein R5 and R6 are a lower alkyl group optionally having substituent(s), an aralkyl group optionally having substituent(s) and the like, a asymmetric transition metal complex containing the compound as a ligand and a production method of optically active compound using the complex as an asymmetric catalyst.

Abstract: The invention relates to 2-(pyridin-2-yl)-pyrimidine compounds of general formula (I) and their use for controlling pathogenic fungi and as plant protection products that, as an active constituent, contain compounds of this type: In general formula (I), k represents 0, 1, 2, 3; m represents 0, 1, 2, 3, 4 or 5; n represents 1, 2, 3, 4 or 5; R1, independent of one another, represents halogen, OH, CN, NO2, C1-C4 alkyl, C1-C4 alkyl halide, C1-C4 alkoxy, C1-C4 alkoxy halide, C2-C4 alkenyl, C2-C4 alkynyl, C3-C8 cycloalkyl, C1-C4 alkoxy-C1-C4 alkyl, amino, phenoxy, which is optionally substituted by halogen or C1-C4 alkyl, NHR, NR2, C(Ra)?N—ORb, S(?O)pA1 or C(?O)A2, or two radicals R1 bound to adjacent carbon atoms can, together, also represent a group —O-Alk-O—, wherein Alk represents a linear or branched C1-C4 alkylene, and 1, 2, 3 or 4 hydrogen atoms can also be replaced by halogen; R2 represents C1-C4 alkyl halide, C1-C4 alkoxy, C1-C4 alkoxy halide, hydroxy, halogen, CN or NO2; whereby R2 can also represent

Abstract: Disclosed are new dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and specification, the isomers thereof, intermediates and processes for preparing these dihydropteridinones and the use thereof as pharmaceutical compositions.

Abstract: The present invention relates to pyrimido [5,4-d] pyrimidine compounds of Formula II or a pharmaceutically acceptable salt thereof, wherein Q is and X, E1, E2, E3, R6 and p are as defined herein. The compounds of this invention are irreversible inhibitors of tyrosine kinases and are useful in the treatment of cancer, atherosclerosis, restenosis, endometriosis and psoriasis.

Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.

Abstract: The present invention provides methods of preparing substituted 2-(pyridin-2-ylamino)-pirido[2,3-d]pyrimidin-7-ones (formula 1), useful in treating cell proliferative disorders, or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to use of a pyrimidone derivative represented by formula (I) or a salt thereof as therapeutic agents: Wherein m, n, p, X, Y, R1, R2, R3, R4 R5, are as defined herein. The invention specifically relates to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3? or GSK3? and cdk5/p25, such as Alzheimer disease.

Abstract: A compound of formula I wherein m, n, A, B, D, E, G, H, Y, R1, R2, R3, R4, R5, and R8, are described herein. Said compounds being useful as inhibitors of potassium channel function and in the treatment of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.

Abstract: The invention provides novel arylamino N-heteroaryl MEK inhibitors of Formula (I): Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation. Also disclosed is the treatment of a hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds.

Abstract: 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, G, J, K, L, M, V R2, R3, R4, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.