Diazabicyclo derivatives
    4.
    发明授权
    Diazabicyclo derivatives 失效
    二氮杂双环衍生物

    公开(公告)号:US5344831A

    公开(公告)日:1994-09-06

    申请号:US10145

    申请日:1993-01-28

    CPC分类号: C07D471/08

    摘要: Diazabicyclo derivatives of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, alkoxyalkyl, oxoalkyl, alkoxycarbonylalkyl, alkoxycarbonyl, acyl, dialkylaminoalkyl, hydroxyalkyl, haloalkyl, cyanoalkyl, heterocycloalkyl, aryl, heteroarylalkyl or arylalkyl, the aryl group and the aryl moiety being optionally substituted by alkoxy, nitro, alkyl, amino or halo;R.sup.2 is hydrogen or alkyl;R.sup.3 and R.sup.4 may be the same or different and each is hydrogen, alkyl, alkenyl, acyl, alkoxyalkyl or arylalkyl wherein the aryl moiety is optionally substituted by alkoxy, nitro, alkyl, amino or halo;with the proviso that when R.sup.2 is hydrogen and both R.sup.3 and R.sup.4 are methyl, R.sup.1 does not represent hydrogen, alkyl, unsubstituted benzyl or dimethylaminoethyl; having 5-HT.sub.3 receptor antagonist activity.

    摘要翻译: 式(I)的二氮杂双环衍生物及其药学上可接受的盐:其中R是氢,烷基,烯基,炔基,环烷基,环烷基烷基,烷氧基烷基,氧代烷基,烷氧基羰基烷基,烷氧基羰基,酰基,二烷基氨基烷基,羟基烷基,卤代烷基, 氰基烷基,杂环烷基,芳基,杂芳基烷基或芳烷基,芳基和芳基部分任选被烷氧基,硝基,烷基,氨基或卤素取代; R2是氢或烷基; R 3和R 4可以相同或不同,各自为氢,烷基,烯基,酰基,烷氧基烷基或芳烷基,其中芳基部分任选被烷氧基,硝基,烷基,氨基或卤素取代; 条件是当R 2是氢并且R 3和R 4都是甲基时,R 1不代表氢,烷基,未取代的苄基或二甲基氨基乙基; 具有5-HT 3受体拮抗剂活性。