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    Process for preparing a substituted pyrazolyl benzenesulfonamide for the treatment of inflammation
    3.
    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。

    Heteroarylpyranopyrazolyl derivatives for the treatment of inflammation
    8.
    发明授权
    Heteroarylpyranopyrazolyl derivatives for the treatment of inflammation 失效
    异芳基吡喃并吡唑衍生物用于治疗炎症

    公开(公告)号：US5565482A

    公开(公告)日：1996-10-15

    申请号：US536925

    申请日：1995-09-29

    申请人： John J. Talley ,  Stephen R. Bertenshaw ,  Matthew J. Graneto ,  Donald J. Rogier

    发明人： John J. Talley ,  Stephen R. Bertenshaw ,  Matthew J. Graneto ,  Donald J. Rogier

    IPC分类号： C07D491/04 ,  C07D491/044 ,  C07D491/048 ,  C07D491/052 ,  C07D495/04 ,  A61K31/415 ,  C07D491/14

    CPC分类号： C07D491/04 ,  C07D495/04

    摘要： A class of benzopyranopyrazolyl derivatives is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein A is --(CH.sub.2).sub.m --X--(CH.sub.2).sub.n --; wherein X is S(O).sub.p or O; wherein m is 0 or 1; wherein n is 0 or 1; wherein p is 0 or 1; wherein B is selected from phenyl and five and six membered heteroaryl; wherein R.sup.1 is selected from lower haloalkyl, cyano, formyl, lower alkoxycarbonyl, lower alkoxy, lower N-alkylaminocarbonyl, N-phenylaminocarbonyl, lower N,N-dialkylaminocarbonyl and lower N-alkyl-N-phenylaminocarbonyl; wherein R.sup.2 is phenyl substituted at a substitutable position with a radical selected from lower alkylsulfonyl and sulfamyl; and wherein R.sup.4 is one or more radicals selected from hydrido, halo, lower alkylthio, lower alkylsulfinyl, lower alkyl, cyano, carboxyl, lower alkoxycarbonyl, aminocarbonyl, lower haloalkyl, hydroxyl, lower alkoxy, amino, lower N-alkylamino, lower N,N-dialkylamino, lower hydroxyalkyl and lower haloalkoxy; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 描述了一类苯并吡喃并吡唑基衍生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I（I）定义，其中A是 - （CH 2）m -X-（CH 2）n - ; 其中X是S（O）p或O; 其中m为0或1; 其中n为0或1; 其中p为0或1; 其中B选自苯基和五元和六元杂芳基; 其中R 1选自低级卤代烷基，氰基，甲酰基，低级烷氧基羰基，低级烷氧基，低级N-烷基氨基羰基，N-苯基氨基羰基，低级N，N-二烷基氨基羰基和低级N-烷基-N-苯基氨基羰基。 其中R2是在可取代的位置被选自低级烷基磺酰基和氨磺酰基的基团取代的苯基; 氰基，羧基，低级烷氧基羰基，氨基羰基，低级卤代烷基，羟基，低级烷氧基，氨基，低级N-烷基氨基，低级N，低级烷基氨基，低级烷基氨基，低级烷基氨基， N-二烷基氨基，低级羟烷基和低级卤代烷氧基; 或其药学上可接受的盐。

    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。