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    Diazabicyclo derivatives
    3.
    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

    申请人： Hiroaki Satoh ,  Haruhiko Kikuchi ,  Kazuhiko Yamada ,  Ruta Fukutomi ,  Masashi Suzuki ,  Koichiro Hagihara ,  Toru Hayakawa ,  Takeo Arai ,  Setsuko Mino

    发明人： Hiroaki Satoh ,  Haruhiko Kikuchi ,  Kazuhiko Yamada ,  Ruta Fukutomi ,  Masashi Suzuki ,  Koichiro Hagihara ,  Toru Hayakawa ,  Takeo Arai ,  Setsuko Mino

    IPC分类号： C07D471/08 ,  C07D247/02 ,  A61K31/495 ,  C07D487/08

    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。

    Indole derivatives
    10.
    发明授权
    Indole derivatives 失效
    INDOLE DORIVATIVES

    公开(公告)号：US5124324A

    公开(公告)日：1992-06-23

    申请号：US614219

    申请日：1990-11-16

    申请人： Haruhiko Kikuchi ,  Hiroaki Satoh ,  Makoto Yanai ,  Toshio Suguro ,  Koichiro Hagihara

    发明人： Haruhiko Kikuchi ,  Hiroaki Satoh ,  Makoto Yanai ,  Toshio Suguro ,  Koichiro Hagihara

    IPC分类号： C07D209/42 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14

    CPC分类号： C07D401/12 ,  C07D209/42 ,  C07D403/12 ,  C07D403/14

    摘要： Disclosed are compounds of formula I ##STR1## wherein R.sub.1 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, benzyl or an indolyl carbonyl group, R.sub.2 is a saturated or unsaturated 5- or 8-membered heterocyclic group containing as a hetero atom one or more nitrogen atoms, the heterocyclic group is optionally substituted at an N or C atom by a C.sub.1 -C.sub.6 alkyl or aralkyl group, n is an integer of 1 to 5 and one or more hydrogen atoms, in an alkylene chain --(CH.sub.2).sub.n -- are optionally substituted by a C.sub.1 -C.sub.6 alkyl, phenyl and/or hydroxyl group, physiologically acceptable salts and quaternary ammonium salts thereof. The compounds are selective antagonists of 5-HT.sub.3 receptors and are useful in the treatment of psychotic disorders, neurotic diseases, gastric stasis symptoms, gastrointestinal disorders, nausea and vomiting.