Abstract: Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals.

Abstract: The present invention provides a compound having a glucokinase activating action being useful for prevention or treatment of diabetes mellitus, etc. being represented by the formula (I): X is nitrogen atom, etc.; Y is oxygen atom, etc.; R1 is an optionally substituted five to six-membered heteroaryl group, etc.; R2 is hydrogen atom or fluorine atom; and ring A is a monocyclic or bicyclic heteroaryl group which may have a substituent represented by the formula (II)] or a pharmaceutically acceptable salt thereof.

Abstract: The present invention is directed to the novel use of a CSBP/p38 inhibitor for the treatment, including prophylaxis of inflammation enhanced cough in a mammal in need thereof.

Abstract: Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.

Abstract: Amine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.

Abstract: The inventive subject matter relates to compounds, pharmaceutical compositions, and kits containing a heterocyclic compound represented by the formula (I) wherein R is an alkyl group optionally having substituent(s) etc., X is an amino group optionally having substituent(s), Y1 and Y2 are nitrogen atoms etc., an isomer or solvate thereof or a pharmaceutically acceptable salt thereof as an active ingredient.

Abstract: Novel substituted pyrimidol[4,5-d]pyrimidin-2-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.

Abstract: The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders.

Abstract: Compounds are provided which are antagonists of chemokine receptor activity.

Abstract: The invention describes compounds of the general formula I a process for their manufacture, compositions containing them and their manufacture as well as the use of these compounds as pharmaceutically active agents. These compounds show activity as protein kinase inhibitors, in particular src family tyrosine kinase inhibitors, and may therefore be useful for the treatment of diseases mediated by said tyrosine kinases.

Abstract: Compounds having the formula (I) or (II), are useful as p38 kinase inhibitors, wherein R is an optionally substituted alkyl, cycloalkyl, or aryl; R6 is hydrogen or lower alkyl; R7 is hydrogen or a non-interfering substituent, and Q is a non-aromatic moiety as defined in the specification.

Abstract: The invention describes compounds of the general formula I a process for their manufacture, medicaments containing them and their manufacture as well as the use of these compounds as pharmaceutically active agents. The compounds show activity as protein kinase inhibitors, in particular src family tyrosine kinase inhibitors, and may therefore be useful for the treatment of diseases mediated by said tyrosine kinases.

Abstract: Ditosylate salts of 4-quinazolineamines are described as well as methods of using the same in the treatment of disorde4rs characterized by aberrant erbB family PTK activity.

Abstract: A method of treating cancer is described including administration of a 4-quinazolineamine and at least one other anti-neoplastic agent as well as pharmaceutical combinations and compositions containing the same.

Abstract: This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5–7 membered monocyclic ring or 8–10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; R1, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3 and Aurora, for treating diseases such as diabetes, cancer, and Alzheimer's disease.

Abstract: The invention provides 5,8-dihydro-6H-pyrido[2,3-d]pyrimidin-7-one compounds that are selective inhibitors of KDR and FGFR kinases, and are useful in the treatment of cancers. The compounds have the generic structure I where Ar, Ar?, and R1 are as set forth in the present specification. The invention also provides pharmaceutical compositions containing these compounds and methods for their use.

Abstract: A pyridopyrimidine or a naphthyridine derivative of the formula (I): wherein R1 is an optionally substituted nitrogen-containing heterocyclic group, etc.; R2 is H or a lower alkyl group; R3 is H or an optionally substituted lower alkyl group, etc.; R4 is H, a lower alkyl group, COOH, etc.; R5 is a lower alkyl group which may optionally be substituted by an optionally substituted aryl etc.; one of X and Y is CH and the other is nitrogen, or both of X and Y are nitrogen; or a pharmaceutically acceptable salt thereof, these compounds exhibiting excellent PDE V inhibitory activities, and being useful in the prophylaxis or treatment of penile erectile dysfunction, etc.

Abstract: Substituted quinazolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Abstract: Disclosed are compounds of the formula wherein R2, R5, R6, R7, and R8 are as defined herein. These compounds and their pharmaceutical compositions are useful for treating cell proliferative disorders, such as cancer and restenosis. These compounds are potent inhibitors of cdks and growth factor-mediated kinases.

Abstract: This invention provides antiangiogenic compounds of the Formula (I), which are useful for treating diseases, resulting from uncontrolled cellular proliferation such as cancer, atherosclerosis, rheumatoid arthritis, and psoriasis.

Abstract: The invention provides pyrido[2,3-d]pyrimidin-7(8H)-one telomerase inhibitors of the formula where R1, R2 are as defined herein. The invention also provides methods for preparing the compounds of formula I, methods of using the compounds to treat diseases such as cancer, and pharmaceutical compositions comprising the compounds.

Abstract: This invention describes novel pyrazole compounds of formula IV: wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ring having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R2, R2?, T, and R3 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

Abstract: This invention describes novel pyrazole compounds of formula IIc: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-7 membered ring having 0-3 heteroatoms; and R2 and R2? are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

Abstract: The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders.

Abstract: The invention relates to 6- or 7-bicyclic-substituted 4-amino-subsituted pyridopyrimidines and to pharmaceutically acceptable salts, prodrugs and hydrates thereof. The invention also relates to pharmaceutical compositions containing the compounds and to methods of treating hyperproliferative disorders abnormal cell growth in a mammal by administering the compounds.

Abstract: The invention is directed to methods to inhibit TGF-? and/or p38-? kinase using compounds of the formula or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar? is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.

Abstract: The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein A, X, R1, R3 and R4 are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.

Abstract: Disorders mediated by p38 kinase inhibitors are treated with compounds of the formula: or salts thereof, wherein: R1 is hydrogen or alkyl; R2 is substituted cycloalkyl, heterosubstituted cycloalkyl, helcroalkylsubstituted cycloalkyl, heterosubstituted cycloalkyl-alkly, heterocyclyl, heterocyclyl spiro cycloalkyl, aralkoxy, alkoxy, -alkylene-S(O)n-alkyl (where is 1 or 2) or —SO2Ar2; R3 is hydrogen, amino, monoalkylamino, dialkylamino, acylamino, —NR8—C(?O)—Rb (where Ra is hydrogen or alkyl and Rh is heterocyclyl or heteroalkyl), alkyl, cycloalkyl, phthalimidoalkyl, aryl, aralkyl, haloalkyl, heteroalkyl, cyanoalkyl, -alkylene-C(O) R (where R is hydrogen, alkyl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino) or acyl; and each of Ar1 and Ar2 is independently aryl.

Abstract: The invention relates to processes for the preparation of a GARFT inhibitor containing a methyl substituted thiophene core having the following structure: 1

Abstract: Disclosed are compounds which inhibit or modulate the activity of protein kinases and pharmaceutical compositions containing such compounds. The disclosed compound contain two or more ligand moieties covalently linked together by one or more linking groups. Such compounds are useful for treating diseases or medical disorders mediated by protein kinases.

Abstract: This invention relates to compounds which are generally CRF-1 receptor antagonists and which are represented by Formula I wherein X1 is (CH2)n or CO, n is 0 to 2 and R1, R2, R3 and R4 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts thereof. The invention further relates to processes for preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for their use as therapeutic agents.

Abstract: This invention provides pyridopyrimidines and 4-aminopyrimidines that are useful for treating cell proliferatives disorders, such as cancer and restenosis. We have now discovered a group of 7,8-dihydro-2 (amino and thio)pyrido[2,3-d]pyrimidines and 2,4-diaminopyrimidines that are potent inhibitors of cyclin-dependent kinases (cdks) and growth factor-mediated kinases. The compounds are readily synthesized and can be administered by a variety of routes, including orally, and have sufficient bioavailability. This invention provides compounds of Formula (I) and Formula (II) where W is NH, S, SO, or SO2, R1 includes phenyl and substituted phenyl, R2 includes alkyl and cycloalkyl, R3 includes alkyl and hydrogen, R8 and R9 include hydrogen and alkyl, and Z is carboxy. This invention also provide pharmaceutical formulations comprising a compound of Formula (I or II) together with a pharmaceutically acceptable carrier, diluent, or excipient therefor.

Abstract: Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.

Abstract: Compounds having the formula (I) or (II), 1

Abstract: Erb inhibitors used in combination with retinoids are effective to prevent skin injury otherwise caused by retinoids alone.

Abstract: The present invention provides compounds of the formula: 1

Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory and immune conditions and diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of a chemokine receptor. The subject methods are useful for the treatment of inflammatory and immunoregulatory disorders and diseases, such as multiple sclerosis, rheumatoid arthritis and type I diabetes.

Abstract: The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof wherein the variables are as defined in the description, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).

Abstract: This invention concerns a bicyclic compound of Formula (I), wherein: G is N, CH or C(CN); ring X is a 5- or 6-membered fused heteroaryl ring which contains 1, 2, or 3 heteroatoms selected from oxygen, sulphur and nitrogen; m is 0-2; R1 is a group such as hydroxy, halo, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; each of R2 and R3 is hydrogen, halo, C1-6alkyl, C2-6alkenyl or C2-6 alkynyl; R4 is a group such as hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy, amino and N-C1-6alkylamino; R5 is a group such as hydrogen, halo, trifluoromethyl, cyano, nitro, amino and hydroxy, and q is 0-4; or a pharmaceutically acceptable salt or an in vivo cleavable ester thereof; processes for its preparation, a pharmaceutical composition containing it and its use in the treatment of diseases or medical conditions mediated by cytokines.

Abstract: The invention provides certain thiazolopyrimidine compounds of formula (1) or a pharmaceutically acceptable salt or solvate thereof: in which: A is a group of formula (a) or (b): processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: Disclosed are novel dihydropridinone compounds that are selective inhibitors of both KDR and FGFR kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon lung and prostate tumors. Also, disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer.

Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.

Abstract: A method of treating cancer is described including administration of a 4-quinazolineamine and at least one other anti-neoplastic agent as well as a pharmaceutical combination including the 4-quinazolineamines.

Abstract: This invention discloses compounds, and pharmaceutically acceptable salts thereof, useful in therapeutically and/or prophylactically treating patients with an illness. Such illnesses include cancer, and secondary infections caused by Pneumocystis carinii and Toxoplasmosis gondii in immunocompromised patients. The compounds themselves, methods of making these compounds, and methods of using these compounds are all disclosed.

Abstract: The invention provides novel pyrido[2,3-d]pyrimidin-7(8H)-ones derivatives active as telomerase inhibitors, the use of the derivatives as therapeutic agents, such as antitumoral agents, processes for preparation of the derivatives, and to pharmaceutical compositions comprising the derivatives.

Abstract: The invention concerns the use of a quinazoline derivative of Formula (I) wherein Q1 includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1 includes a direct bond and O and Q3includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2 and R3 is hydrogen or (1-6C)alkyl; Z includes O, S and NH; and Q2 includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human.

Abstract: This invention provides antiangiogenic compounds of the Formula (I), which are useful for treating diseases, resulting from uncontrolled cellular proliferation such as cancer, atherosclerosis, rheumatoid arthritis, and psoriasis.

Abstract: Ditosylate salts of 4-quinazolineamines are described as well as methods of using the same in the treatment of disorders characterized by aberrant erbB family PTK activity.

Abstract: Process for preparing 2-pyridylamino-pyrido[2,3-d]pyrimidines of Formula (II) wherein Ar is aryl, R′ and R″ are hydrogen, alkyl, alkoxy, or phenyl, and R2 is alkyl.

Abstract: The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel azolidinedione derivatives of the general formula (I), and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them.