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    Benzofuran- and benzopyran-carboxamide derivatives
    2.
    发明授权
    Benzofuran- and benzopyran-carboxamide derivatives 失效
    苯并呋喃和苯并吡喃 - 甲酰胺衍生物

    公开(公告)号：US4617314A

    公开(公告)日：1986-10-14

    申请号：US591363

    申请日：1984-03-20

    申请人： Tetsuya Tahara ,  Kiyoharu Hayano ,  Michihide Setoguchi ,  Takemi Fukuda

    发明人： Tetsuya Tahara ,  Kiyoharu Hayano ,  Michihide Setoguchi ,  Takemi Fukuda

    IPC分类号： A61K31/335 ,  A61K31/34 ,  A61K31/343 ,  A61K31/35 ,  A61K31/352 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/443 ,  A61K31/445 ,  A61K31/535 ,  A61P1/08 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  C07D307/79 ,  C07D311/58 ,  C07D405/12

    CPC分类号： C07D307/79 ,  C07D405/12

    摘要： Benzofuran- and benzopyran-carboxamide derivatives of the formula: ##STR1## wherein l is 1 or 2; X is hydrogen atom, amino group or halogen atom; Y is --S(O).sub.m --R.sup.3 wherein R.sup.3 is lower alkyl group and m is 0, 1 or 2, or ##STR2## wherein R.sup.4 and R.sup.5 are the same or different and are each hydrogen atom or lower alkyl group; R.sup.1 is hydrogen atom, lower alkyl group, arylthiomethyl group, halogenomethyl group or ##STR3## wherein R.sup.6 and R.sup.7 are the same or different and are each hydrogen atom or lower alkyl group or R.sup.6 and R.sup.7 together with the adjacent nitrogen atom form a hetrocycle; R.sup.2 is hydrogen atom or lower alkyl group; and Z is ##STR4## wherein p is 2 or 3, R.sup.8 and R.sup.9 are the same or different and are each lower alkyl group or R.sup.8 and R.sup.9 together with the adjacent nitrogen atom form a heterocycle, or ##STR5## wherein q is 0 or 1, n is 1 or 2, R.sup.10 is lower alkyl group, lower alkenyl group, lower alkinyl group, aralkyl group or cycloalkyl group and R.sup.11 is hydrogen atom or lower alkyl group, their physiologically acceptable salts or their optical isomers, and a method of preparing same. These compounds are useful as psychotropic and antipsychotic agents.

    摘要翻译： 苯并呋喃和苯并吡喃 - 甲酰胺衍生物，其结构式如下：其中l为1或2; X是氢原子，氨基或卤素原子; Y是-S（O）m -R 3，其中R 3是低级烷基，m是0,1或2，或者其中R 4和R 5相同或不同，各自为氢原子或低级烷基; R 1是氢原子，低级烷基，芳基硫代甲基，卤代甲基或者其中R 6和R 7相同或不同，各自为氢原子或低级烷基，或者R 6和R 7与相邻的氮原子一起形成杂环; R2是氢原子或低级烷基; 并且Z为，其中p为2或3，R8和R9相同或不同，为低级烷基或R8和R9与相邻的氮原子一起形成杂环，或者其中q为0或 1，n为1或2，R 10为低级烷基，低级烯基，低级炔基，芳烷基或环烷基，R 11为氢原子或低级烷基，其生理学上可接受的盐或其旋光异构体， 准备相同 这些化合物可用作精神药物和抗精神病药。

    Neuroleptic indole-3-carboxamide derivatives
    3.
    发明授权
    Neuroleptic indole-3-carboxamide derivatives 失效
    神经性吲哚-3-甲酰胺衍生物

    公开(公告)号：US4616009A

    公开(公告)日：1986-10-07

    申请号：US679437

    申请日：1984-12-07

    申请人： Tetsuya Tahara ,  Takemi Fukuda ,  Michihide Setoguchi

    发明人： Tetsuya Tahara ,  Takemi Fukuda ,  Michihide Setoguchi

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/405 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/55 ,  A61P1/04 ,  A61P1/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D209/42 ,  C07D401/12 ,  C07D403/12

    CPC分类号： C07D401/12 ,  C07D209/42 ,  C07D403/12 ,  Y10S47/01

    摘要： Indole-3-carboxamide derivatives of the formula: ##STR1## inclusive of pharmaceutically acceptable acid addition salt and/or hydrate forms thereof, wherein R.sup.1 is hydrogen, C.sub.1-4 alkyl, phenyl which may be optionally substituted by halogen on the benzene ring or phenyl-C.sub.1-4 alkyl which may be optionally substituted by halogen on the benzene ring; R.sup.2 is hydrogen or C.sub.1-4 alkyl; R.sup.3 is hydrogen, halogen, C.sub.1-4 alkyl, hydroxy or C.sub.1-4 alkoxy; R.sup.4 is hydrogen, C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl, allyl or benzyl which may be optionally substituted by halogen on the benzene ring or by methyl on the .alpha.-carbon; R.sup.5 is hydrogen or C.sub.1-4 alkyl; m is 0 or 1; and n is an integer of 1 to 3, are useful as neuroleptic and anxiolytic drugs, and for the prevention and treatment of psychosomatic disturbances.

    摘要翻译： 下式的吲哚-3-甲酰胺衍生物：包括其药学上可接受的酸加成盐和/或其水合物形式，其中R 1是氢，C 1-4烷基，可任意被苯环上的卤素取代的苯基或 苯基-C 1-4烷基，其可任选被苯环上的卤素取代; R2是氢或C1-4烷基; R3是氢，卤素，C1-4烷基，羟基或C1-4烷氧基; R4是氢，C1-4烷基，C3-7环烷基，烯丙基或苄基，它们可以任选地被苯环上的卤素取代，或在α-碳上被甲基取代; R5是氢或C1-4烷基; m为0或1; n为1〜3的整数，可用作抗精神病药和抗焦虑药，用于预防和治疗心身障碍。

    Benzazine compounds and pharmaceutical uses thereof
    5.
    发明授权
    Benzazine compounds and pharmaceutical uses thereof 失效
    苯并嗪化合物及其药物用途

    公开(公告)号：US5185333A

    公开(公告)日：1993-02-09

    申请号：US721011

    申请日：1991-06-26

    申请人： Takeshi Kawakita ,  Takanobu Kuroita ,  Takemi Fukuda ,  Ryuhei Iezawa

    发明人： Takeshi Kawakita ,  Takanobu Kuroita ,  Takemi Fukuda ,  Ryuhei Iezawa

    IPC分类号： C07D265/36 ,  C07D279/16 ,  C07D413/12 ,  C07D417/12 ,  C07D451/04 ,  C07D451/14 ,  C07D453/02

    CPC分类号： C07D451/04 ,  C07D265/36 ,  C07D279/16 ,  C07D413/10 ,  C07D417/12 ,  C07D451/14 ,  C07D453/02

    摘要： A benzazine compound, a geometrical isomer of said benzazine compound, an optical isomer of said benzazine compound, and a pharmaceutically acceptable salt of said benzazine compound, said benzazine compound being represented by formula (I): ##STR1## wherein each symbol is as defined in the specification. Said benzazine compounds exhibit 5-HT.sub.3 receptor antagonistic activity, and 5-HT.sub.1A receptor and/or 5-HT.sub.2 receptor and/or dopamine D.sub.2 receptor blocking activity so that they are useful as drugs for the prophylaxis or treatment of various digestive diseases vomiting and disturbances in central nervous systems and the like. The intermediates for said benzazine compounds are also disclosed.

    摘要翻译： 苯并嗪化合物，所述苯并嗪化合物的几何异构体，所述苯并嗪化合物的光学异构体和所述苯并嗪化合物的药学上可接受的盐，所述苯并嗪化合物由式（I）表示：其中每个符号 如本说明书中所定义。 所述苯并嗪化合物显示5-HT 3受体拮抗活性和5-HT1A受体和/或5-HT2受体和/或多巴胺D2受体阻断活性，使得它们可用作预防或治疗各种消化疾病呕吐和干扰的药物 在中枢神经系统等中。 还公开了所述苯并嗪化合物的中间体。