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    Pharmaceutical composition containing bicyclic type compounds
    5.
    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。

    PHARMACEUTICAL COMPOSITION CONTAINING BICYCLIC TYPE COMPOUNDS
    7.
    发明申请
    PHARMACEUTICAL COMPOSITION CONTAINING BICYCLIC TYPE COMPOUNDS 审中-公开

    公开(公告)号：US20070088064A1

    公开(公告)日：2007-04-19

    申请号：US11611161

    申请日：2006-12-15

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

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

    IPC分类号： A61K31/424 ,  A61K31/353 ,  C07D491/02

    CPC分类号： C07D409/06 ,  C07D311/68 ,  C07D409/12 ,  C07D498/04

    摘要： A compound of formula (I) or pharmaceutically acceptable salt thereof: wherein: either Y is N and R2 is hydrogen, or Y is C—R1 where: either one of R1 and R2 is hydrogen and the other is selected from the class of hydrogen, C3-8 cycloalkyl, C1-6 alkyl optionally interrupted by oxygen or substituted by hydroxy, C1-6 alkoxy or substituted aminocarbonyl, C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyloxy, C1-6 alkoxy, nitro, cyano, halo, trifluoromethyl, CF3S, or a group CF3-A-, where A is —CF2—, —CO—, —CH2—, CH(OH), SO2, SO, CH2—O, or CONH, or a group CF2H-A′- where A′ is oxygen, sulphur, SO, SO2, CF2 or CFH; trifluoromethoxy, C1-6 alkylsulphinyl, perfluoro C2-6 alkylsulphonyl, C1-6 alkylsulphonyl, C1-6 alkoxysulphinyl, C1-6 alkoxysulphonyl, aryl, heteroaryl, arylcarbonyl, heteroarylcarbonyl, phosphono, arylcarbonyloxy, heteroarylcarbonyloxy, arylsulphinyl, heteroarylsulphinyl, arylsulphonyl, heteroarylsulphonyl in which any aromatic moiety is optionally substituted, C1-6 alkylcarbonylamino, C1-6 alkoxycarbonylamino, C1-6 alkyl-thiocarbonyl, C1-6 alkoxy-thiocarbonyl, C1-6 alkyl-thiocarbonyloxy, 1-mercapto C2-7 alkyl, formyl, or aminosulphinyl, aminosulphonyl or aminocarbonyl, any amino moiety being optionally substituted by one or two C1-6 alkyl groups, or C1-6 alkylsulphinylamino, C1-6 alkylsulphonylamino, C1-6 alkoxysulphinylamino or C1-6 alkoxysulphonylamino, or ethylenyl terminally substituted by C1-6 alkylcarbonyl, nitro or cyano, or —C(C1-6 alkyl)NOH or —C(C1-6 alkyl)NNH2, or one of R1 and R2 is nitro, cyano or C1-3 alkylcarbonyl and the other is methoxy or amino optionally substituted by one or two C1-6 alkyl or by C2-7 alkanoyl; or R1 and R2 together are —(CH2)4— or —CH═CH—CH═CH—, or form an optionally substituted triazole or oxadiazole ring; one of R3 and R4 is hydrogen or C1-4 alkyl and the other is C1-4 alkyl, CF3 or CH2 Xa where Xa is fluoro, chloro, bromo, iodo, C1-4 alkoxy, hydroxy, C1-4 alkylcarbonyloxy, —S—C1-4 alkyl, nitro, amino optionally substituted by one or two C1-4 alkyl groups; cyano or C1-4 alkoxycarbonyl or R3 and R4 together are C2-5 polymethylene optionally substituted by C1-4 alkyl; R5 is C1-6 alkylcarbonyloxy, benzoyloxy, ONO2, benzyloxy, phenyloxy or C1-6 alkoxy and R6 and R9 are hydrogen or R5 is hydroxy and R6 is hydrogen or C1-2 alkyl and R9 is hydrogen; R7 is heteroaryl or phenyl; both of which are optionally substituted one or more times independently with a group or atom selected from chloro, fluoro, bromo, iodo, nitro, amino optionally substituted once or twice by C1-4 alkyl, cyano, azido, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy and trifluoromethyl; R8 is hydrogen; C1-6 alkyl, OR9 or NHCOR10 wherein R9 is hydrogen, C1-6 alkyl, formyl, C1-6 alkanoyl, aroyl or aryl-C1-6 alkyl and R10 is hydrogen, C1-6 alkyl, C1-6 alkoxy, mono or di C1-6 alkyl amino, amino, amino-C1-6 alkyl, hydroxy-C1-6 alkyl, halo-C1-6 alkyl, C1-6 acyloxy-C1-6 alkyl, C1-6 alkoxycarbonyl-C1-6-alkyl, aryl or heteroaryl; the R8—N—CO—R7 group being cis to the R5 group; and X is oxygen or NR10 where R10 is hydrogen or C1-6 alkyl with the proviso that the compound is not racemic cis-4-benzoylamino-6-cyano-3,4-dihydro-2,2-dimethyl-2H-benzo[b]pyran-3-ol.