首页> 外国专利> Treatment of circulatory disorders using n-substituted (amp;agr;- imidazolyl-toluyl) pyrrole angiotensin II antagonists

Treatment of circulatory disorders using n-substituted (amp;agr;- imidazolyl-toluyl) pyrrole angiotensin II antagonists

机译:使用n-取代的(α-咪唑基-甲苯基)吡咯血管紧张素II拮抗剂治疗循环系统疾病

摘要

A class of N-substituted (&agr;-imidazolyltoluyl)pyrrole compounds is described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein m is one; wherein R.sup.0 is selected from CH. sub.2 OH, CO.sub.2 H, CHO, CO.sub.2 CH.sub.3, CO.sub.2 C.sub.2 H.sub.5, CH.sub.2 OCH.sub.3, CH.sub.2 OCHOCH.sub.3 and CH.sub.2 --CO.sub.2 C.sub.2 H.sub.5 ; wherein R.sup.1 is selected from Cl, CF.sub.3, CHO, n-butyl, cyano, CO. sub.2 CH.sub.3 and CO.sub.2 CH.sub.2 CH.sub.3 ; wherein R.sup. 2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, propylthio, butylthio and hydroxyalkyl; wherein each of R.sub.3, R.sub.4, R.sup.6, R. sup.7, R.sup.9 and R.sup.10 is hydrido; wherein each of R.sup.5 and R.sup. 8 is independently selected from hydrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl, methoxycarbonyl with the proviso that at least one of R.sup.5 and R.sup.8 is an acidic group selected from CO. sub.2 H and tetrazolyl; or a tautomer thereof or a pharmaceutically- acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.
机译:描述了一类N-取代的(α-咪唑基甲苯基)吡咯化合物,其用于治疗循环系统疾病。特别感兴趣的化合物是式## STR1 ##的血管紧张素II拮抗剂,其中m是1; m是1。其中R.sup.0选自CH。 sub.2 OH,CO.sub.2 H,CHO,CO.sub.2 CH.sub.3,CO.sub.2 C.sub.2 H.sub.5,CH.sub.2 OCH.sub。 3,CH.sub.2 OCHOCH.sub.3和CH.sub.2-CO.sub.2 C.sub.2 H.sub.5;其中R 1选自Cl,CF 3,CHO,正丁基,氰基,CO 2 CH 3和CO 2 CH 2 CH。 3;其中R.sup。 2选自甲基,乙基,正丙基,异丙基,正丁基,仲丁基,异丁基,叔丁基,正戊基,异戊基,新戊基,苯基,苄基,苯乙基,环己基,环己基甲基,环己基乙基,丙硫基,丁硫基和羟烷基;其中R 3,R 4,R 6,R sup 7,R 9和R 10均为氢。其中R.sup.5和R.sup。 R 8独立地选自氢,卤素,硝基,三氟甲基,羟基,烷氧基,氰基,羧基,甲氧基羰基,条件是R 5和R 8中的至少一个是选自CO 2的酸性基团。 .2 H和四唑基;或其互变异构体或其药学上可接受的盐。这些化合物在治疗或控制高血压和充血性心力衰竭中特别有用。

著录项

  • 公开/公告号US5451597A

    专利类型

  • 公开/公告日1995-09-19

    原文格式PDF

  • 申请/专利权人 G.D. SEARLE & CO.;

    申请/专利号US19930066057

  • 申请日1993-05-27

  • 分类号A61K31/415;A61K31/41;C07D233/90;C07D403/04;C07D403/14;

  • 国家 US

  • 入库时间 2022-08-22 04:04:21

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