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    DIAMINOCYCLOBUTENE-3,4-DIONES
    4.
    发明公开
    DIAMINOCYCLOBUTENE-3,4-DIONES 失效
    DIAMINOCYCLOBUTENE -3,4-二酮

    公开(公告)号：EP0796243A1

    公开(公告)日：1997-09-24

    申请号：EP95935742.0

    申请日：1995-10-03

    申请人： AMERICAN HOME PRODUCTS CORPORATION

    发明人： ANTANE, Madelene, Miyoko ,  BUTERA, John, Anthony ,  HIRTH, Bradford, Hammond ,  ANTANE, Schuyler, Adam

    IPC分类号： A61K31 ,  A61P1 ,  A61P13 ,  A61P15 ,  A61P21 ,  C07C231 ,  C07C233 ,  C07C255 ,  C07C271 ,  C07C311 ,  C07D213 ,  C07D217

    CPC分类号： C07D213/75 ,  C07C233/41 ,  C07C255/60 ,  C07C271/28 ,  C07C311/08 ,  C07C2601/04 ,  C07C2601/14 ,  C07C2602/42 ,  C07D217/02

    摘要： The compound of formula (I), wherein R1 and R2 are, independent from each other, hydrogen, C1-10 straight chain alkyl, C1-10 branched alkyl, or C3-10 cyclic or bicyclic alkyl; R3 is an acyl substituent selected from the group consisting of formyl, alkanoyl of 2 to 7 carbon atoms, alkenoyl of 3 to 7 carbon atoms, alkylsulfonyl of 1 to 7 carbon atoms, aroyl of 7 to 12 carbon atoms, arylalkenoyl of 9 to 20 carbon atoms, arylsulfonyl of 6 to 12 carbon atoms, arylalkanoyl of 8 to 12 carbon atoms or arylalkylsulfonyl of 7 to 12 carbon atoms; A is selected from the group consisting of (a), wherein R4 is hydrogen, C1-6 alkyl, C1-6 perfluoroalkyl, C1-6 alkoxy, C1-6 perfluoroalkoxy, amino, C1-6 alkylamino, C2-12 dialkylamino, C1-6 alkylsulfonamido, alkylcarboxamido containing 2 to 7 carbon atoms, nitro, cyano, carboxyl; or, A is a phenyl group of formula (b), wherein R5 and R6, independent from each other, are selected from the following: cyano, nitro, amino, C1-6 alkyl, C1-6 perfluoroalkyl, C1-6 alkoxy, C1-6 perfluoroalkoxy, C1-6 alkylamino, C2-12 dialkylamino, sulfamyl, C1-6 alkylsulfonamido, C6-12 arylsulfonamido, alkylcarboxamido containing 2 to 7 carbon atoms, arylcarboxamido containing 7 to 13 carbon atoms, C2 to C6 alkanoyl, C1-6 alkylsulfonyl, C1-6 perfluoroalkylsulfonyl, C6-12 arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl, carboxyl or hydrogen; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.

    摘要翻译： 其中R 1和R 2彼此独立地为氢，C 1-10直链烷基，C 1-10支链烷基或C 3-10环状或双环烷基的式（I）化合物; R3是选自甲酰基，2至7个碳原子的烷酰基，3至7个碳原子的烯酰基，1至7个碳原子的烷基磺酰基，7至12个碳原子的芳酰基，9至20个的芳基烯酰基 6-12个碳原子的芳基磺酰基，8-12个碳原子的芳基烷酰基或7-12个碳原子的芳基烷基磺酰基; A选自（a），其中R4是氢，C1-6烷基，C1-6全氟烷基，C1-6烷氧基，C1-6全氟烷氧基，氨基，C1-6烷基氨基，C2-12二烷基氨基，C1 -6烷基亚磺酰氨基，含2-7个碳原子的烷基甲酰胺基，硝基，氰基，羧基; 或者A是式（b）的苯基，其中R5和R6彼此独立地选自：氰基，硝基，氨基，C1-6烷基，C1-6全氟烷基，C1-6烷氧基， C1-6全氟烷氧基，C1-6烷基氨基，C2-12二烷基氨基，氨磺酰基，C1-6烷基磺酰氨基，C6-12芳基磺酰氨基，含2-7个碳原子的烷基甲酰氨基，含7-13个碳原子的芳基甲酰氨基，C2- C6烷基磺酰基，C1-6全氟烷基磺酰基，C6-12芳基磺酰基，氯，溴，氟，碘，1-咪唑基，羧基或氢; 或其药学上可接受的盐是平滑肌松弛剂。