申请人:Dr. Karl Thomae GmbH
公开号:US05591762A1
公开(公告)日:1997-01-07
Disclosed herein are angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl. An exemplary compound is: (a) 4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazole-2-yl)-benzimidazol-1-yl] methyl]-biphenyl-2-carboxylic acid.
本文披露了以下结构的血管紧张素II拮抗剂##STR1##其中R.sub.1是氢以外的其他官能团,包括卤素、较低的烷基或环烷基;R.sub.2是可选择地取代的苯并咪唑-2-基、5,6,7,8-四氢咪唑并[1,2-a]吡啶-2-基、丁磺酰胺-1-基、咪唑-4-基和四氢苯并咪唑-2-基等;R.sub.3是较低的烷基;R.sub.4是酸性基团,如羧基或四唑基。一个示例化合物是:(a) 4'-[[2-正丙基-4-甲基-6-(1-甲基苯并咪唑-2-基)-苯并咪唑-1-基] 甲基]-联苯-2-羧酸。