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    Benzopyran derivatives with antihypertensive activity
    6.
    发明公开
    Benzopyran derivatives with antihypertensive activity 失效
    Benzopyranderivate mit einer blutdrucksenkenden Wirkung。

    公开(公告)号：EP0359537A1

    公开(公告)日：1990-03-21

    申请号：EP89309272.6

    申请日：1989-09-12

    申请人： BEECHAM GROUP PLC

    发明人： Stemp, Geoffrey ,  Burrell, Gordon ,  Smith, David Glynn Beecham Pharmaceuticals

    IPC分类号： C07D311/68 ,  C07D405/04 ,  C07D491/04 ,  C07C247/14 ,  C07C255/59 ,  C07C279/16 ,  C07C335/14 ,  A61K31/44

    CPC分类号： C07D405/04 ,  C07C255/59 ,  C07C255/67 ,  C07C279/28 ,  C07C335/32 ,  C07C2602/08 ,  C07D311/68 ,  C07D491/04

    摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof:
    wherein
    a and b together form an -O- or -CH₂- linkage or a bond;
    either Y is N and R₂ is hydrogen; or
    Y is C-R₁
    wherein
    either one of R₁ and R₂ is hydrogen and the other is nitro, cyano, halo, CF₃, formyl, aldoxime, CF₃O, NO₂-CH=CH-, NC-CH=CH-; a group R x X- wherein R x is C₁₋₆ alkyl, aryl or heteroaryl either of which may be optionally substituted by one, two or three of C₁₋₄ alkyl, C₁₋₄ alkoxy, nitro, halo, CF₃ and cyano; and X is C=O, O.C=O, C=O.O, CHOH, SO, SO₂, O.SO, O.SO₂, CONH, O.CONH, C=S, O.C=S, C=S.O, CH.SH, SONH, SO₂NH, O.SONH, O.SO₂NH, CO-CH=CH, C=NHOH, C=NNH₂; or a group R y R z NZ- wherein R y and R z are independently hydrogen or C₁₋₆ alkyl and Z is C=O, SO or SO₂; or
    R₁ is a C₃₋₈ cycloalkyl group or a C₁₋₆ alkyl group optionally substituted by a group which is hydroxy, C₁₋₆ alkoxy, amino optionally substituted by one or two C₁₋₆ alkyl groups, C₁₋₇ alkanoylamino, C₃₋₈ cycloalkyloxy or C₃₋₈ cycloalkylamino; and R₂ is hydrogen; or
    one of R₁ and R₂ is nitro, cyano or C₁₋₃ alkylcarbonyl and the other is a different group selected from nitro, cyano, halo, C₁₋₃ alkylcarbonyl, methoxy or amino optionally substituted by one or two C₁₋₆ alkyl or by C₂₋₇ alkanoyl;
    either one of R₃ and R₄ is hydrogen or C₁₋₄ alkyl and the other is C₁₋₄ alkyl; or
    R₃ and R₄ together are C₂₋₅ polymethylene;
    either R₅ is hydrogen, hydroxy, C₁₋₆ alkoxy or C₁₋₇ acyloxy; and
    R₆ is hydrogen; or
    R₅ and R₆ together are a bond;
    either R₇ is hydrogen, C₁₋₆ alkyl, C₃₋₆ cycloalkyl, C₂₋₆ alkenyl or C₂₋₆ alkynyl; and
    R₈ is hydrogen or C₁₋₆ alkyl; or
    R₇ and R₈ together are C₂₋₄ polymethylene;
    R₉ is CN, NO₂, COR₁₀ or SO₂R₁₀ wherein R₁₀ is C₁₋₃ alkyl, NH₂, NH(C₁₋₃ alkyl), CF₃ or phenyl optionally substituted as defined for R x ; and
    the R₈N(NR₉)NHR₇ moiety is trans to the R₅ group when R₅ is hydroxy, C₁₋₆ alkoxy or C₁₋₇ acyloxy;
    having antihypertensive and/or bronchodilator activity, processes for their preparation and their use as pharmaceuticals.

    摘要翻译： 式（I）化合物及其药学上可接受的盐：其中a和b一起形成-O-或-CH 2 - 键或键; Y是N，R 2是氢; 或Y是C-R1，其中R1和R2中的任一个是氢，另一个是硝基，氰基，卤素，CF 3，甲酰基，醛肟，CF 3 O，NO 2 -CH = CH-，NC-CH = CH-; 基团RxX-，其中Rx是C 1-6烷基，芳基或杂芳基，其中任一个可以任选被C 1-4烷基，C 1-4烷氧基，硝基，卤素，CF 3和氰基中的一个，两个或三个取代; 并且X为C = O，OC = O，C = OO，CHOH，SO，SO2，O.SO，O.SO2，CONH，O.CONH，C = S，OC = S，C = SO，CH.SH ，SONH，SO2NH，O.SONH，O.SO2NH，CO-CH = CH，C = NHOH，C = NNH2; 或RyRzNZ-基团，其中R y和R z独立地为氢或C 1-6烷基，Z为C = O，SO或SO 2; 或R 1为任选被羟基，C 1-6烷氧基，任选被一个或两个C 1-6烷基取代的氨基，C 1-7烷酰基氨基，C 3-8烷基氨基， 8环烷氧基或C 3-8环烷基氨基; R2是氢; 或R 1和R 2中的一个是硝基，氰基或C 1-3烷基羰基，另一个是选自硝基，氰基，卤素，C 1-3烷基羰基，甲氧基或任选被一个或两个C 1-6烷基取代的氨基或不同的基团 C2-7烷酰基; R3和R4中的任一个是氢或C 1-4烷基，另一个是C 1-4烷基; 或R3和R4一起是C2-5聚亚甲基; R5是氢，羟基，C1-6烷氧基或C1-7酰氧基; R6为氢; 或R5和R6一起是键; R 7是氢，C 1-6烷基，C 3-6环烷基，C 2-6烯基或C 2-6炔基; R8是氢或C1-6烷基; 或R7和R8一起是C2-4聚亚甲基; R9是CN，NO2，COR10或SO2R10，其中R10是C1-3烷基，NH2，NH（C1-3烷基），CF3或如Rx所定义的任选取代的苯基; 当R 5为羟基，C 1-6烷氧基或C 1-7酰氧基时，R 8 N（NR 9）NHR 7部分为反式基团; 具有抗高血压和/或支气管扩张剂活性，其制备方法及其作为药物的用途。