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    Indazole-3-carboxylic acid derivatives
    3.
    发明授权
    Indazole-3-carboxylic acid derivatives 失效
    吲唑-3-羧酸衍生物

    公开(公告)号：US5017573A

    公开(公告)日：1991-05-21

    申请号：US384766

    申请日：1989-07-25

    申请人： Tatsuya Kon ,  Shiro Kato ,  Toshiya Morie ,  Tadahiko Karasawa ,  Naoyuki Yoshida

    发明人： Tatsuya Kon ,  Shiro Kato ,  Toshiya Morie ,  Tadahiko Karasawa ,  Naoyuki Yoshida

    IPC分类号： A61K31/55 ,  A61P1/00 ,  A61P1/08 ,  A61P9/00 ,  A61P25/00 ,  A61P25/04 ,  A61P43/00 ,  C07D243/08 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D471/04

    CPC分类号： C07D401/14 ,  C07D243/08 ,  C07D403/12 ,  C07D405/14

    摘要： An indazole-3-carboxylic acid derivative represented by the following general formula (I) or its physiologically acceptable acid addition salt or quaternary ammonium salt, ##STR1## wherein Y represents --NH-- or --O--; R.sub.1 and R.sub.2 are identical or different and each represents a hydrogen atom, a lower alkyl group, a substituted lower alkyl group, a cycloalkyl group, a lower alkenyl group, a cycloalkenyl group, a lower alkynyl group, an unsubstituted or substituted aryl-lower alkyl group, a lower alkoxycarbonyl group, an unsubstituted or substituted aralkyloxycarbonyl group or an acyl group, or R.sub.1 and R.sub.2, taken together, form a lower alkylene group; R.sub.3 represents a hydrogen atom, a lower alkyl group, or a phenyl group; R.sub.4 represents a hydrogen atom, a lower alkyl group, a substituted lower alkyl group, a cycloalkyl group, a lower alkenyl group, a cycloalkenyl group, a lower alkynyl group, an unsubstituted or substituted aryl-lower alkyl group, a lower alkoxycarbonyl group, an unsubstituted or substituted aralkyloxycarbonyl group or an acyl group; R.sub.5 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a trifluoromethyl group, a nitro group, an amino group or an acylamino group; m represents a number of 1, 2, 3 or 4; n represents a number of 1, 2 or 3; and p represents a number of 1, 2, 3 or 4.This compound is useful as a potent and selective antagonist of serotonin 3 (5--HT.sub.3) receptor.

    Medicament for treating cerebral insufficiency diseases, novel 2-(1-piperazinyl)-4-phenylcycloalkanopyrimidine derivatives, and process for the production thereof
    7.
    发明授权
    Medicament for treating cerebral insufficiency diseases, novel 2-(1-piperazinyl)-4-phenylcycloalkanopyrimidine derivatives, and process for the production thereof 失效
    治疗脑功能不全疾病的药物，新型2-（1-哌嗪基）-4-苯基环烷基嘧啶衍生物及其制备方法

    公开(公告)号：US5185338A

    公开(公告)日：1993-02-09

    申请号：US711894

    申请日：1991-06-07

    申请人： Katsuhiko Hino ,  Naoki Kai ,  Masato Sakamoto ,  Tatsuya Kon ,  Makoto Oka ,  Kiyoshi Furukawa ,  Yoshiaki Ochi

    发明人： Katsuhiko Hino ,  Naoki Kai ,  Masato Sakamoto ,  Tatsuya Kon ,  Makoto Oka ,  Kiyoshi Furukawa ,  Yoshiaki Ochi

    IPC分类号： A61K31/505 ,  C07D239/70

    CPC分类号： C07D239/70 ,  A61K31/505

    摘要： Medicament for the treatment of cerebral insufficiency diseases comprising as an active ingredient a compound of the formula: ##STR1## wherein n is 3, 4, 5 or 6; R.sup.1 is hydrogen atom, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, hydroxy-C.sub.2 -C.sub.6) alkyl, unsubstituted or substituted aryl, heteroaryl, unsubstituted or substituted aryl-(C.sub.1 -C.sub.6) alkyl, unsubstituted or substituted aryl-carbonyl-(C.sub.1 -C.sub.6) alkyl, or acyl; R.sup.2 is hydrogen atom, halogen atom, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, or trifluoromethyl; and R.sup.3 is hydrogen atom or C.sub.1 -C.sub.6 alkyl, or an acid addition salt thereof, novel 2-(1-piperazinyl)-4-phenyl-cycloalkanopyrimidine derivatives having excellent cerebral function improving activity, processes for the preparation thereof.

    摘要翻译： 用于治疗脑功能不全疾病的药物，其包含下式的化合物作为活性成分：其中n为3,4,5或6;其中n为3,4,5或6; R 1是氢原子，C 1 -C 6烷基，C 3 -C 8环烷基，羟基-C 2 -C 6）烷基，未取代或取代的芳基，杂芳基，未取代或取代的芳基 - （C 1 -C 6）烷基，未取代或取代的芳基 - 羰基 - （ C 1 -C 6）烷基或酰基; R2是氢原子，卤素原子，C1-C6烷基，C1-C6烷氧基或三氟甲基; 和R3是氢原子或C1-C6烷基或其酸加成盐，具有优异的脑功能改善活性的新型2-（1-哌嗪基）-4-苯基 - 环烷基嘧啶衍生物，其制备方法。