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    Benz �G! indazolyl derivatives for the treatment of inflammation
    76.
    发明授权
    Benz �G! indazolyl derivatives for the treatment of inflammation 失效
    Benz [G]吲唑基衍生物用于治疗炎症

    公开(公告)号：US5696143A

    公开(公告)日：1997-12-09

    申请号：US309294

    申请日：1994-09-20

    Applicant: John J. Talley ,  Stephen R. Bertenshaw ,  Roland S. Rogers

    Inventor： John J. Talley ,  Stephen R. Bertenshaw ,  Roland S. Rogers

    IPC: C07D231/54 ,  A61K31/415

    CPC classification number: C07D231/54

    Abstract: A class of benz�g!indazolyl 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.dbd.CH--; wherein R.sup.1 is selected from lower haloalkyl, cyano, lower alkoxycarbonyl, 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.3 is one or more radicals selected from halo, lower alkylthio, lower alkylsulfinyl, lower alkyl, cyano, lower alkoxycarbonyl, aminocarbonyl, lower N-alkylaminocarbonyl, lower haloalkyl, hydroxyl, lower alkoxy, lower hydroxyalkyl, lower haloalkoxy, amino, lower N,N-dialkylamino and nitro; or a pharmaceutically-acceptable salt thereof.

    Abstract translation: 描述了一类苯并[g]吲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为-CH = CH-; 其中R 1选自低级卤代烷基，氰基，低级烷氧基羰基，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; 并且其中R 3是一个或多个选自卤素，低级烷硫基，低级烷基亚磺酰基，低级烷基，氰基，低级烷氧基羰基，氨基羰基，低级N-烷基氨基羰基，低级卤代烷基，羟基，低级烷氧基，低级羟烷基，低级卤代烷氧基，氨基，低级 N，N-二烷基氨基和硝基; 或其药学上可接受的盐。

    Pyrazolyl derivatives for the treatment of inflammation
    77.
    发明授权
    Pyrazolyl derivatives for the treatment of inflammation 失效
    吡唑基衍生物用于治疗炎症

    公开(公告)号：US5670532A

    公开(公告)日：1997-09-23

    申请号：US719501

    申请日：1996-09-25

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

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

    IPC: C07D491/04 ,  C07D491/044 ,  C07D491/048 ,  C07D491/052 ,  C07D495/04 ,  A61K31/415 ,  A61K31/435 ,  C07D487/04

    CPC classification number: C07D491/04 ,  C07D495/04

    Abstract: 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.

    Abstract translation: 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。

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