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    1,3,5 trisubstituted pyrazole compounds for treatment of inflammation
    9.
    发明授权
    1,3,5 trisubstituted pyrazole compounds for treatment of inflammation 失效
    用于治疗炎症的1,3,5三取代吡唑化合物

    公开(公告)号：US5434178A

    公开(公告)日：1995-07-18

    申请号：US160517

    申请日：1993-11-30

    申请人： John J. Talley ,  Donald J. Rogier, Jr.

    发明人： John J. Talley ,  Donald J. Rogier, Jr.

    IPC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 ,  C07D231/14

    CPC分类号： C07D231/12 ,  C07D231/16 ,  C07D405/04 ,  C07D409/04

    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 ##STR1## wherein R.sup.1 is lower alkylsulfonyl or sulfamyl; wherein R.sup.2 is aryl or heteroaryl; wherein R.sup.2 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 R.sup.3 is selected from hydrido, lower alkyl, lower haloalkyl, cyano, carboxyl, alkoxycarbonyl, amino, acyl, acylamino, halo and alkylsulfonylamino; wherein R.sup.4 is aryl or heteroaryl; wherein R.sup.4 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 R.sup.2 and R.sup.4 cannot be phenyl or substituted triazole, when R.sup.1 is sulfamyl; further provided R.sup.2 cannot be 4-methoxyphenyl or 4-methylphenyl when R.sup.4 is 4-methoxyphenyl or 4-methylphenyl and when R.sup.1 is sulfamyl; and further provided that R.sup.2 cannot be tetrazole when R.sup.4 is fluorophenyl, and when R.sup.1 is methylsulfonyl; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 描述了一类1,3,5-三芳基或杂芳基吡唑用于治疗炎症，包括治疗疼痛和疾病如关节炎。 特别感兴趣的化合物是式I的化合物，其中R 1是低级烷基磺酰基或亚磺酰基; 其中R2是芳基或杂芳基; 其中R2任选在可取代的位置被一个或多个选自卤素，低级烷氧基，低级烷基，硝基，低级烷硫基，氨基，低级卤代烷基，羟基，羧基，N-单烷基氨基，N，N-二烷基氨基，氰基，烷氧羰基 和酰氨基; 其中R 3选自氢，低级烷基，低级卤代烷基，氰基，羧基，烷氧基羰基，氨基，酰基，酰氨基，卤素和烷基磺酰基氨基; 其中R4是芳基或杂芳基; 其中R 4在可取代位置任选被一个或多个选自卤素，低级烷氧基，低级烷基，硝基，低级烷硫基，氨基，低级卤代烷基，羟基，羧基，N-单烷基氨基，N，N-二烷基氨基，氰基， 烷氧基羰基和酰氨基; 当R1是亚磺酰基时，R2和R4不能是苯基或取代的三唑; 进一步提供当R 4是4-甲氧基苯基或4-甲基苯基时，当R 1是亚磺酰基时，R 2不能是4-甲氧基苯基或4-甲基苯基; 并且进一步提供当R 4为氟苯基时，R 2不能为四唑，并且当R 1为甲基磺酰基时; 或其药学上可接受的盐。