发明名称 3(5)-heteroaryl substituted pyrazoles as p38 kinase inhibitors
摘要 A compound of Formula (I), or a pharmaceutically-acceptable salt or a tautomer thereof, wherein: R1 is selected from hydrido, alkyl, cycloalkyl, alkenyl, alkynyl, cycloalkylalkyl, haloalkyl, hydroxyalkyl, arylalkyl, alkoxyalkyl, mercaptoalkyl, alkylthioalkylene, amino, alkylamino, arylamino, aminoalkyl, alkylaminoalkyl, heterocyclylalkyl, aminocarbonylalkyl, and alkylaminocarbonylalkyl; and R2 is selected from hydrido, alkyl, alkenyl, alkynyl, heterocyclyl, haloalkyl, heterocyclylalkyl, amino, alkylamino, aminoalkyl, alkoxy, alkylthio, carboxy, alkoxycarbonyl, carboxyalkyl, aminocarbonylamino, alkylaminocarbonylamino, alkylsulfonyl, aminosulfonyl, alkylsulfonylamino, aminosulfonylamino, alkylaminosulfonylamino, and alkynylamino; wherein the heterocyclyl and heterocyclylalkyl groups are optionally substituted with one or more radicals independently selected from alkylthio, alkylsulfonyl, alkylsulfonyl, halo, alkyl, alkoxy, aryloxy, arylalkoxy, heterocyclyl, haloalkyl, amino, cyano, and hydroxy ; and Ar1 is aryl optionally substituted with one or more radicals independently selected from halo, alkyl, alkenyl, alkynyl, alkoxy, alkenoxy, alkyldioxy, alkylthio, alkylsulfinyl, alkylsulfonyl, amino, aminocarbonyl, cyano, alkoxycarbonyl, formyl, aminosulfonyl, alkylamino, nitro, arylamino, alkylcarbonylamino, halosulfonyl, aminoalkyl, and haloalkyl; and HetAr2 is pyridinyl, pyrimidinyl or quinolinyl optionally substituted with one or more radicals independently selected from alkylthio, alkylsulfonyl, alkylsulfinyl, halo, alkyl, heterocyclyl, alkoxy, aralkoxy, haloalkyl, amino, cyano, arylalkyl, alkylamino, cycloalkylamino, cycloalkenylamino, arylamino, alkynylamino, and arylalkylamino. Such compounds are useful in the treatment of a p38 kinase-mediated disorders, such as bone resorption, graft v's host reaction, artherosclerosis, arthritis, osteoarthritis, rheumatoid arthritis, gout, psoriasis, topical inflammatory disease state, adult respiratory distress syndrome, asthma, chronic pulmonary inflammatory disease, cardiac reperfusion injury, renal reperfusion injury, thrombus, glomerulonephritis, Crohn's disease, ulcerative colitis, inflammatory bowel disease and cachexia.
申请公布号 NZ516318(A) 申请公布日期 2003.06.30
申请号 NZ20010516318 申请日期 2001.12.20
申请人 G 发明人 CLARE, MICHAEL;GENG, LIFENG;HANSON, GUNNAR J;PARTIS, RICHARD A;STEALEY, MICHAEL A;WEIER, RICHARD M;ANANTANARAYAN, ASHOK
分类号 C07D401/00;(IPC1-7):C07D401/00 主分类号 C07D401/00
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