Claims for Patent: 5,591,762

Summary for Patent: 5,591,762

Title:	Benzimidazoles useful as angiotensin-11 antagonists
Abstract:	Disclosed herein are angiotensin-II antagonists of the formula wherein R1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R2 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; R3 is, inter alia, lower alkyl; and, R4 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.
Inventor(s):	Norbert Hauel, Berthold Narr, deceased, Uwe Ries, Jacobus C. A. van Meel, Wolfgang Wienen, Michael Entzeroth
Assignee:	Boehringer Ingelheim Pharma GmbH and Co KG
Application Number:	US08/457,204
Patent Claims:	1. A compound of the formula I ##STR30## wherein R1 is in the 4-position and represents a C1-4-alkyl, C3-7 -cycloalkyl or trifluoromethyl group,R2 represents a benzimidazol-2-yl group optionally substituted in the 1-position by C1-6 -alkyl or C3-7 -cycloalkyl group, whilst the phenyl nucleus of the above-mentioned benzimidazole groups may additionally be substituted by a fluorine atom or by a methyl or trifluoromethyl group, R3 represents a C1-5 -alkyl group or cyclopropyl, and R4 denotes a 1H-tetrazolyl group or an Ra O--CO-- group, whereinRa denotes a hydrogen atom or a straight-chained or branched C1-4 -alkyl group, or a pharmaceutically acceptable salt thereof. 2. In accordance with claim 1, a compound of the formula I, whereinR2 is in the 6-position, or a pharmaceutically acceptable salt thereof. 3. In accordance with claim 2, a compound of the formula I, whereinR1 represents a methyl group, R2 represents a benzimidazol-2-yl group optionally substituted in the 1-position by a C1-3 -alkyl group, whilst the phenyl nucleus of one of the above-mentioned benzimidazole groups may additionally be substituted by a fluorine atom, R3 represents a C1-5 -alkyl group, and R4 represents a carboxy or 1H-tetrazolyl group, or a pharmaceutically acceptable salt thereof. 4. A compound selected from the group consisting of:(a) 4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl]-methyl]-biphenyl-2-carboxylic acid, (b) 4'-[[2-n-propyl-4-methyl-6-(1 -methylbenzimidazol-2-yl)-benzimidazol-1-yl]-methyl]-2-(1H-tetrazol-5-yl)-biphenyl, (c) 4'-[(2-n-propyl-4-methyl-6-(1-methyl-5-fluoro-benzimidazol-2-yl)-benzimidazol-1-yl)-methyl]-biphenyl-2-carboxylic acid, (d) 4'-[[2-n-butyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl]-methyl]-2-(1H-tetrazol-5-yl)-biphenyl, (e) 4'-[[2-n-propyl-4-methyl-6-(1-methyl-6-fluoro-benzimidazol-2-yl)-benzimidazol-1-yl]-methyl]-biphenyl-2-carboxylic acid, (f) 4'-[(2-ethyl-4-methyl-6-(1-methyl-5-fluoro-benzimidazol-2-yl)-benzimidazol-1-yl)-methyl]-biphenyl-2-carboxylic acid, and pharmaceutically acceptable salts thereof. 5. 4'-[[2-n-Propyl-4-methyl-6-(1-methylbenzimidazole-2-yl)-benzimidazol-1-yl]-methyl]-biphenyl-2-carboxylic acid or a pharmaceutically acceptable salt thereof. 6. 4'-[[2-n-Propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl]-methyl]-2-(1H-tetrazol-5-yl)-biphenyl or a pharmaceutically acceptable salt thereof. 7. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claims 1, 2, 3, 4, 5, or 6. 8. A method for treating hypertension which comprises administering to a mammalian host suffering from the same an antihypertensive amount of a compound of claims 1, 2, 3, 4, 5 or 6.