首页> 外国专利> Pyrrolo 3,2-Cazepine-4-one derivatives and pyrrolo 3,4-Cazepine-4-one derivatives their preparation and pharmaceutical compositions containing them

Pyrrolo 3,2-Cazepine-4-one derivatives and pyrrolo 3,4-Cazepine-4-one derivatives their preparation and pharmaceutical compositions containing them

机译:吡咯并[3,2-C]氮杂-4-酮衍生物和吡咯并[3,4-C]氮杂-4-酮衍生物及其制备方法和含有它们的药物组合物

摘要

Disclosed is a pyrroloazepine derivative or a salt thereof. The pyrroloazepine derivative is represented by the following formula (I): CHEM wherein the ring P represented by CHEM means a pyrrole ring represented by the following structure: CHEM in which R1 represents alkyl, cycloalkyl or the like, and R2 represents H or alkyl; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present/and Z1 represents H but, when the bond is absent, Z1 and Z2 are both H; Z1 represents H and Z2 represents a group OR3 in which R3 represents H, alkyl, aralkyl or the like; Z1 and Z2 both represent groups SR4 in which R4 represents alkyl, aralkyl or the like; or Z1 and Z2 are combined together to represent O, a group NOR5 in which R5 represents H, alkyl or the like, or a C2-C3 alkylenedithio; A represents alkylene, alkenylene or alkynylene; and Y represents a group CHEM in which W represents CH, C= or N, m stands for 0 or 1, n stands for 1, 2 or 3, G represents O, S, C=O, sulfinyl, sulfonyl, alkylene, alkenylene, acetal or the like; E1 and E2 represent H or lower alkyl group; and D represents an aromatic hydrocarbon or am aromatic heterocyclic ring. The compound (I) has strong serotonin-2 receptor antagonistic action and low toxicity and less side effects, and is useful as a therapeutic for circulatory diseases such as ischemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.
机译:公开了吡咯并ze庚因衍生物或其盐。吡咯并ze庚因衍生物由下式(I)表示:,其中由表示的环P表示由以下结构表示的吡咯环:,其中R1表示烷基,环烷基等,并且R 2代表H或烷基;虚线表示存在或不存在键;当存在键时,Z2不存在/ Z1表示H,但是当不存在键时,Z1和Z2均为H; Z 1表示H,Z 2表示基团OR 3,其中R 3表示H,烷基,芳烷基等; Z 1和Z 2均代表基团SR 4,其中R 4代表烷基,芳烷基等;或Z 1和Z 2结合在一起表示O,或基团NOR 5,其中R 5表示H,烷基等,或C 2 -C 3亚烷基二硫基;或A代表亚烷基,亚烯基或亚炔基; Y代表基团,其中W代表CH,C =或N,m代表0或1,n代表1、2或3,G代表O,S,C = O,亚磺酰基,磺酰基,亚烷基,亚烯基,乙缩醛等; E1和E2代表H或低级烷基; D表示芳香族烃或芳香族杂环。化合物(I)具有强烈的5-羟色胺2受体拮抗作用,毒性低,副作用小,可用于治疗缺血性心脏病,脑血管疾病和周围循环疾病等循环系统疾病。

著录项

  • 公开/公告号IL121432A

    专利类型

  • 公开/公告日2000-09-28

    原文格式PDF

  • 申请/专利权人 SUNTORY LIMITED;

    申请/专利号IL19960121432

  • 发明设计人

    申请日1996-12-02

  • 分类号C07D487/04;C07D495/20;C12P41/00;A61K31/55;A61P7/00;A61P9/00;

  • 国家 IL

  • 入库时间 2022-08-22 01:56:04

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号