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    Substituted isoxazole for the treatment of inflammation
    1.
    发明授权
    Substituted isoxazole for the treatment of inflammation 失效
    取代的异恶唑用于治疗炎症

    公开(公告)号：US5985902A

    公开(公告)日：1999-11-16

    申请号：US801768

    申请日：1997-02-18

    申请人： John J Talley ,  Srinivasan Nagarajan ,  Roland S Rogers

    发明人： John J Talley ,  Srinivasan Nagarajan ,  Roland S Rogers

    IPC分类号： A61K31/42 ,  A61K31/4439 ,  A61P1/00 ,  A61P1/02 ,  A61P1/04 ,  A61P3/10 ,  A61P7/00 ,  A61P7/06 ,  A61P9/10 ,  A61P11/00 ,  A61P11/02 ,  A61P11/06 ,  A61P13/12 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P19/06 ,  A61P19/08 ,  A61P21/04 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/28 ,  A61P27/02 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07D261/08 ,  C07D261/10 ,  C07D261/12 ,  C07D261/18 ,  C07D413/04 ,  A61K31/44 ,  C07D413/06 ,  C07D413/12

    CPC分类号： C07D261/10 ,  C07D261/08 ,  C07D261/12 ,  C07D261/18 ,  C07D413/04

    摘要： A class of substituted isoxazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II ##STR1## wherein R.sup.1 is selected from hydroxyl, lower alkyl, carboxyl, lower carboxyalkyl, lower aminocarbonylalkyl, lower alkoxycarbonylalkyl, lower aralkyl, lower alkoxyalkyl, lower aralkoxyalkyl, lower alkylthioalkyl, lower aralkylthioalkyl, lower alkylaminoalkyl, lower aryloxyalkyl, lower arylthioalkyl, lower haloalkyl, lower hydroxylalkyl, cycloalkyl, cycloalkylalkyl, and aralkyl; wherein R.sup.3 is selected from cycloalkyl, cycloalkenyl, aryl, and heteroaryl; wherein R.sup.3 is optionally substituted at a substitutable position with one or more radicals independently selected from lower alkylsulfinyl, lower alkyl, cyano, carboxyl, lower alkoxycarbonyl, lower haloalkyl, hydroxyl, lower hydroxyalkyl, lower haloalkoxy, amino, lower alkylamino, lower arylamino, lower aminoalkyl, nitro, halo, lower alkoxy, aminosulfonyl, and lower alkylthio; and wherein R.sup.4 is selected from lower alkyl, hydroxyl and amino; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 描述了一类用于治疗炎症和炎症相关疾病的取代的异恶唑基化合物。 特别感兴趣的化合物由式II定义，其中R1选自羟基，低级烷基，羧基，低级羧基烷基，低级氨基羰基烷基，低级烷氧基羰基烷基，低级芳烷基，低级烷氧基烷基，低级芳烷氧基烷基，低级烷硫基烷基，低级芳烷硫基烷基，低级烷基氨基烷基，低级芳氧基烷基 低级芳基硫代烷基，低级卤代烷基，低级羟基烷基，环烷基，环烷基烷基和芳烷基; 其中R 3选自环烷基，环烯基，芳基和杂芳基; 其中R 3在可取代的位置任选被一个或多个独立地选自低级烷基亚磺酰基，低级烷基，氰基，羧基，低级烷氧基羰基，低级卤代烷基，羟基，低级羟烷基，低级卤代烷氧基，氨基，低级烷基氨基，低级芳基氨基，低级 氨基烷基，硝基，卤素，低级烷氧基，氨基磺酰基和低级烷硫基; 并且其中R 4选自低级烷基，羟基和氨基; 或其药学上可接受的盐。

    Substituted pyrazolyl benzenesulfonamides for the treatment of inflammation
    2.
    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
    4.
    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。

    Substituted pyrazolyl benzenesulfonamides for the treatment of asthma
    6.
    发明授权
    Substituted pyrazolyl benzenesulfonamides for the treatment of asthma 失效
    用于治疗哮喘的取代的吡唑基苯磺酰胺

    公开(公告)号：US06413960B1

    公开(公告)日：2002-07-02

    申请号：US09609011

    申请日：2000-05-30

    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： A61P1106

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

    Substituted pyrazolyl benzenesulfonamides for the treatment of inflammation
    7.
    发明授权
    Substituted pyrazolyl benzenesulfonamides for the treatment of inflammation 有权
    用于治疗炎症的取代的吡唑基苯磺酰胺

    公开(公告)号：US6156781A

    公开(公告)日：2000-12-05

    申请号：US449076

    申请日：1999-11-24

    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： A61K31/415 ,  A61P11/06 ,  A61P17/06 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D231/54 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D495/04 ,  A61P17/07

    CPC分类号： C07D405/04 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D231/54 ,  C07D401/04 ,  C07D403/04 ,  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: ##STR1## wherein R.sup.2 is selected from hydrido, alkyl, haloalkyl, alkoxycarbonyl, cyano, cyanoalkyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, cycloalkylaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, aminocarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R.sup.3 is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein R.sup.4 is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R.sup.4 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 R.sup.2 and R.sup.3 are not both hydrido; further provided that R.sup.2 is not carboxyl or methyl when R.sup.3 is hydrido and when R.sup.4 is phenyl; further provided that R.sup.4 is not triazolyl when R.sup.2 is methyl; further provided that R.sup.4 is not aralkenyl when R.sup.2 is carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that R.sup.4 is not phenyl when R.sup.2 is methyl and R.sup.3 is carboxyl; and further provided that R.sup.4 is not unsubstituted thienyl when R.sup.2 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。