发明名称 1,3,5 trisubstituted pyrazole compounds for treatment of inflammation
摘要 A class of 1,3,5-triaryl or heteroaryl pyrazoles is described for the treatment of inflammation, including treatment of pain and disorders such as arthritis. Compounds of particular interest are of Formula I <IMAGE> I wherein R1 is lower alkylsulfonyl or sulfamyl; wherein R2 is aryl or heteroaryl; wherein R2 is optionally substituted at substitutable positions with one or more radicals selected from halo, lower alkoxy, lower alkyl, nitro, lower alkylthio, amino, lower haloalkyl, hydroxyl, carboxyl, N-monoalkylamino, N,N-dialkylamino, cyano, alkoxycarbonyl and acylamino; wherein R3 is selected from hydrido, lower alkyl, lower haloalkyl, cyano, carboxyl, alkoxycarbonyl, amino, acyl, acylamino, halo and alkylsulfonylamino; wherein R4 is aryl or heteroaryl; wherein R4 is optionally substituted at a substitutable position with one or more radicals selected from halo, lower alkoxy, lower alkyl, nitro, lower alkylthio, amino, lower haloalkyl, hydroxyl, carboxyl, N-monoalkylamino, N,N-dialkylamino, cyano, alkoxycarbonyl and acylamino; provided R2 and R4 cannot be phenyl or substituted triazole, when R1 is sulfamyl; further provided R2 cannot be 4-methoxyphenyl or 4-methylphenyl when R4 is 4-methoxyphenyl or 4-methylphenyl and when R1 is sulfamyl; and further provided that R2 cannot be tetrazole when R4 is fluorophenyl, and when R1 is methylsulfonyl; or a pharmaceutically-acceptable salt thereof.
申请公布号 US5434178(A) 申请公布日期 1995.07.18
申请号 US19930160517 申请日期 1993.11.30
申请人 G.D. SEARLE & CO. 发明人 TALLEY, JOHN J.;ROGIER, JR., DONALD J.
分类号 A61K31/415;A61K31/44;A61K31/4427;A61K31/443;A61K31/4433;A61P25/04;A61P29/00;C07D231/12;C07D231/16;C07D401/04;C07D405/04;C07D409/04;(IPC1-7):A61K31/415;C07D231/14 主分类号 A61K31/415
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