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    Pharmaceutical composition containing bicyclic type compounds
    2.
    发明授权
    Pharmaceutical composition containing bicyclic type compounds 失效
    含双环型化合物的药物组合物

    公开(公告)号：US5948811A

    公开(公告)日：1999-09-07

    申请号：US852890

    申请日：1997-05-08

    申请人： Wai Ngor Chan ,  John Morris Evans ,  Geoffrey Stemp ,  Neil Upton ,  Robert Nicholas Willette

    发明人： Wai Ngor Chan ,  John Morris Evans ,  Geoffrey Stemp ,  Neil Upton ,  Robert Nicholas Willette

    IPC分类号： A61K31/35 ,  A61K31/352 ,  A61K31/353 ,  A61K31/38 ,  A61K31/381 ,  A61P9/10 ,  A61P25/00 ,  A61P25/06 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/26 ,  A61P25/30 ,  C07D311/68 ,  C07D311/70 ,  C07D311/72 ,  C07D409/06 ,  C07D409/12 ,  C07D498/04 ,  C07D498/14

    CPC分类号： C07D409/06 ,  C07D311/68 ,  C07D409/12

    摘要： A compound of formula (I) or pharmaceutically acceptable salt thereof: ##STR1## wherein either Y is N and R.sub.2 is hydrogen, or Y is C--R.sub.1 ; where either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from the class of hydrogen, C.sub.3-8 cycloalkyl, C.sub.1-6 alkyl optionally interrupted by oxygen or substituted by hydroxy, C.sub.1-6 alkoxy or substituted arminocarbonyl, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkoxy, nitro, cyano, halo, trifluoromethyl, CF.sub.3 S, or a group CF.sub.3 --A--, or a group CF.sub.2 H--A'--, trifluoromethoxy, C.sub.1-6 alkylsulphinyl, perfluoro C.sub.2-6 alkylsulphonyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl, C.sub.1-6 alkoxysulphonyl, aryl, heteroaryl, arylcarbonyl, heteroarylcarbonyl, phosphono, arylcarbonyloxy, heteroarylcarbonyloxy, arylsulphinyl, heteroarylsulphinyl, arylsulphonyl, heteroarylsulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, 1-mercapto C.sub.2-7 alkyl, formyl, or aminosulphinyl, aminosulphonyl or aminocarbonyl, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino, C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino, or ethylenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl)NOH or --C(C.sub.1-6 alkyl)NNH.sub.2, or one of R.sub.1 and R.sub.2 is nitro, cyano or C.sub.1-3 alkylcarbonyl and the other is methoxy or amino optionally substituted by one or two C.sub.1-6 alkyl or by C.sub.2-7 alkanoyl; or R.sub.1 and R.sub.2 together are --(CH.sub.2).sub.4 -- or --CH.dbd.CH--CH.dbd.CH--, or form an optionally substituted triazole or oxadiazole ring; R.sub.3 to R.sub.9 represent various substituent groups; and X is oxygen or NR.sub.10 where R.sub.10 is hydrogen or C.sub.1-6 alkyl.

    摘要翻译： 式（I）化合物或其药学上可接受的盐：其中Y为N且R 2为氢，或Y为C-R 1; 其中R 1和R 2中的任一个是氢，另一个选自氢，C 3-8环烷基，任选被氧中断或被羟基取代的C 1-6烷基，C 1-6烷氧基或取代的芳基羰基，C 1-6烷基羰基 C 1-6烷氧基羰基，C 1-6烷基羰基氧基，C 1-6烷氧基，硝基，氰基，卤素，三氟甲基，CF 3 S或基团CF 3 -A-或基团CF 2 H-A'，三氟甲氧基，C 1-6烷基亚磺酰基， 全氟C 2-6烷基磺酰基，C 1-6烷基磺酰基，C 1-6烷氧基亚磺酰基，C 1-6烷氧基磺酰基，芳基，杂芳基，芳基羰基，杂芳基羰基，膦酰基，芳基羰基氧基，杂芳基羰基氧基，芳基亚磺酰基，杂芳基亚磺酰基，芳基磺酰基，杂芳基磺酰基，C 1-6烷基羰基氨基， 6烷氧基羰基氨基，C 1-6烷基 - 硫代羰基，C 1-6烷氧基 - 硫代羰基，C 1-6烷基 - 硫代羰基氧基，1-巯基C 2-7烷基，甲酰基或氨基亚磺酰基，氨基磺酰基或氨基羰基，或C 1-6烷基亚磺酰氨基，C 1-6 烷基磺酰基氨基，C 1-6烷氧基亚磺酰氨基或C 1-6烷基 或由C 1-6烷基羰基，硝基或氰基或-C（C 1-6烷基）NOH或-C（C 1-6烷基）NNH 2末端取代的亚烷基磺酰基氨基，或R 1和R 2之一是硝基，氰基或C1- 3烷基羰基，另一个是任选被一个或两个C 1-6烷基或C 2-7烷酰基取代的甲氧基或氨基; 或R 1和R 2一起为 - （CH 2）4 - 或-CH = CH-CH = CH-，或形成任选取代的三唑或恶二唑环; R3至R9表示各种取代基; 并且X是氧或NR 10，其中R 10是氢或C 1-6烷基。