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    Substituted pyrazolyl benzenesulfonamides for the treatment of inflammation
    8.
    发明授权
    Substituted pyrazolyl benzenesulfonamides for the treatment of inflammation 失效
    用于治疗炎症的取代的吡唑基苯磺酰胺

    公开(公告)号：US06492411B1

    公开(公告)日：2002-12-10

    申请号：US10125325

    申请日：2002-04-17

    申请人： John J Talley ,  Thomas D Penning ,  Paul W Collins ,  Donald J Rogier, Jr. ,  James W Malecha ,  Julie M Miyashiro ,  Stephen R Bertenshaw ,  Ish K Khanna ,  Matthew J Graneto ,  Roland S Rogers ,  Jeffery S Carter ,  Stephen H. Docter ,  Stella S Yu

    发明人： John J Talley ,  Thomas D Penning ,  Paul W Collins ,  Donald J Rogier, Jr. ,  James W Malecha ,  Julie M Miyashiro ,  Stephen R Bertenshaw ,  Ish K Khanna ,  Matthew J Graneto ,  Roland S Rogers ,  Jeffery S Carter ,  Stephen H. Docter ,  Stella S Yu

    IPC分类号： A61P2900

    CPC分类号： C07D403/04 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D231/54 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  C07D495/04

    摘要： A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: wherein R2 is selected from hydrido, alkyl, haloalkyl, alkoxycarbonyl, cyano, cyanoalkyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, cycloalkylaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, aminocarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R3 is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein R4 is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R4 is optionally substituted at a substitutable position with one or more radicals selected from halo, alkylthio, alkylsulfonyl, cyano, nitro, haloalkyl, alkyl, hydroxyl, alkenyl, hydroxyalkyl, carboxyl, cycloalkyl, alkylamino, dialkylamino, alkoxycarbonyl, aminocarbonyl, alkoxy, haloalkoxy, sulfamyl, heterocyclic and amino; provided R2 and R3 are not both hydrido; further provided that R2 is not carboxyl or methyl when R3 is hydrido and when R4 is phenyl; further provided that R4 is not triazolyl when R2 is methyl; further provided that R4 is not aralkenyl when R2 is carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that R4 is not phenyl when R2 is methyl and R3 is carboxyl; and further provided that R4 is not unsubstituted thienyl when R2 is trifluoromethyl; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 描述了一类吡唑基苯磺酰胺化合物用于治疗炎症和炎症相关疾病。 特别感兴趣的化合物由式II定义：其中R2选自氢化，烷基，卤代烷基，烷氧基羰基，氰基，氰基烷基，羧基，氨基羰基，烷基氨基羰基，环烷基氨基羰基，芳基氨基羰基，羧基烷基氨基羰基，羧基烷基，芳烷氧基羰基烷基氨基羰基，氨基羰基烷基，烷氧基羰基氰基烯基和羟烷基。 其中R 3选自氢，烷基，氰基，羟基烷基，环烷基，烷基磺酰基和卤素; 并且其中R 4选自芳烯基，芳基，环烷基，环烯基和杂环; 其中R 4在可取代位置任选被一个或多个选自卤素，烷硫基，烷基磺酰基，氰基，硝基，卤代烷基，烷基，羟基，烯基，羟基烷基，羧基，环烷基，烷基氨基，二烷基氨基，烷氧基羰基，氨基羰基，烷氧基， 卤代烷氧基，氨磺酰基，杂环和氨基; 只要R2和R3都不是氢的; 进一步提供当R 3是氢的时，当R 4是苯基时，R 2不是羧基或甲基; 进一步提供当R 2是甲基时，R 4不是三唑基; 进一步提供当R 2是羧基时，R 4不是芳烯基，氨基羰基或乙氧基羰基; 进一步提供，当R 2是甲基且R 3是羧基时，R 4不是苯基; 并且进一步提供当R 2是三氟甲基时，R 4不是未取代的噻吩基; 或其药学上可接受的盐。

    Process for preparing a substituted pyrazolyl benzenesulfonamide for the treatment of inflammation
    10.
    发明授权
    Process for preparing a substituted pyrazolyl benzenesulfonamide for the treatment of inflammation 失效
    制备用于治疗炎症的取代的吡唑基苯磺酰胺的方法

    公开(公告)号：US06716991B1

    公开(公告)日：2004-04-06

    申请号：US10378781

    申请日：2003-03-04

    申请人： John J Talley ,  Thomas D Penning ,  Paul W Collins ,  Donald J Rogier, Jr. ,  James W Malecha ,  Julie M Miyashiro ,  Stephen R Bertenshaw ,  Ish K Khanna ,  Matthew J Graneto ,  Roland S Rogers ,  Jeffery S Carter ,  Stephen H. Doctor ,  Stella S Yu

    发明人： John J Talley ,  Thomas D Penning ,  Paul W Collins ,  Donald J Rogier, Jr. ,  James W Malecha ,  Julie M Miyashiro ,  Stephen R Bertenshaw ,  Ish K Khanna ,  Matthew J Graneto ,  Roland S Rogers ,  Jeffery S Carter ,  Stephen H. Doctor ,  Stella S Yu

    IPC分类号： C07D23112

    CPC分类号： C07D409/04 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D231/54 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D495/04

    摘要： A class of pyrazolyl benzenesulfonamide compounds is descrbed for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: wherein R2 is selected from hydrido, alkyl, haloalkyl, alkoxycarbonyl, cyano, cyanoalkyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, cycloalkylaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, aminocarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R3 is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulforyl and halo; and wherein R4 is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R4 is optionally substituted at a substitutable position with one or more radicals selected from halo, alkylthio, alkylsulfonyl, cyano, nitro, haloalkyl, alkyl, hydroxyl, alkenyl, hydroxyalkyl, carboxy, cycloalkyl, alkylamino, dialkylamino, alkoxycarbonyl, aminocarbonyl, alkoxy, haloalkoxy, sulfamyl, heterocyclic and amino; provided R2 and R3 are not both hydrido; further provided that R2 is not carboxyl or methyl when R3 is hydrido and when R4 is phenyl; further provided that R4 is not triazolyl when R2 is methyl; further provided that R4 is not aralkenyl when R2 is carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that R4 is not phenyl when R2 is methyl and R3 is carboxyl; and further provided that R4 is not unsubstituted thienyl when R2 is trifluoromethyl; or a pharmceutically-acceptable salt thereof.

    摘要翻译： 描述了一类吡唑基苯磺酰胺化合物用于治疗炎症和炎症相关疾病。 特别感兴趣的化合物由式II定义：其中R 2选自氢化，烷基，卤代烷基，烷氧基羰基，氰基，氰基烷基，羧基，氨基羰基，烷基氨基羰基，环烷基氨基羰基，芳基氨基羰基，羧基烷基氨基羰基，羧基烷基，芳烷氧基羰基烷基氨基羰基，氨基羰基烷基，烷氧羰基氰基烯基和 羟烷基 其中R 3选自氢，烷基，氰基，羟基烷基，环烷基，烷基磺酰基和卤素; 其中R 4选自芳烯基，芳基，环烷基，环烯基和杂环; 其中R 4在可取代的位置任选被一个或多个选自卤素，烷硫基，烷基磺酰基，氰基，硝基，卤代烷基，烷基，羟基，烯基，羟基烷基，羧基，环烷基，烷基氨基，二烷基氨基，烷氧基羰基，氨基羰基 ，烷氧基，卤代烷氧基，氨磺酰基，杂环和氨基; 条件是R 2和R 3都不是氢的; 进一步提供当R 3是氢的时，当R 4是苯基时，R 2不是羧基或甲基; 进一步提供当R 2是甲基时，R 4不是三唑基; 进一步提供当R 2是羧基时，R 4不是芳烯基，氨基羰基或乙氧基羰基; 进一步提供当R 2是甲基且R 3是羧基时，R 4不是苯基; 并且进一步提供当R 2为三氟甲基时R 4为未取代的噻吩基; 或其药学上可接受的盐。