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Claims for Patent: 5,591,762

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Claims for Patent: 5,591,762

Title: Benzimidazoles useful as angiotensin-11 antagonists
Abstract: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.
Inventor(s): Hauel; Norbert (Schemmerhofen, DE), Narr, deceased; Berthold (late of Biberach, DE), Ries; Uwe (Biberch, DE), van Meel; Jacobus C. A. (Mittelbiberach, DE), Wienen; Wolfgang (Biberach/Rissegg, DE), Entzeroth; Michael (Warthausen, DE)
Assignee: Dr. Karl Thomae GmbH (Biberach an der Riss, DE)
Application Number:08/457,204
Patent Claims: 1. A compound of the formula I ##STR30## wherein R.sub.1 is in the 4-position and represents a C1-4-alkyl, C.sub.3-7 -cycloalkyl or trifluoromethyl group,

R.sub.2 represents a benzimidazol-2-yl group optionally substituted in the 1-position by C.sub.1-6 -alkyl or C.sub.3-7 -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,

R.sub.3 represents a C.sub.1-5 -alkyl group or cyclopropyl, and

R.sub.4 denotes a 1H-tetrazolyl group or an R.sub.a O--CO-- group, wherein

R.sub.a denotes a hydrogen atom or a straight-chained or branched C.sub.1-4 -alkyl group,

or a pharmaceutically acceptable salt thereof.

2. In accordance with claim 1, a compound of the formula I, wherein

R.sub.2 is in the 6-position,

or a pharmaceutically acceptable salt thereof.

3. In accordance with claim 2, a compound of the formula I, wherein

R.sub.1 represents a methyl group,

R.sub.2 represents a benzimidazol-2-yl group optionally substituted in the 1-position by a C.sub.1-3 -alkyl group, whilst the phenyl nucleus of one of the above-mentioned benzimidazole groups may additionally be substituted by a fluorine atom,

R.sub.3 represents a C.sub.1-5 -alkyl group, and

R.sub.4 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)-benzimida zol-1-yl)-methyl]-biphenyl-2-carboxylic acid,

(d) 4'-[[2-n-butyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl]-m ethyl]-2-(1H-tetrazol-5-yl)-biphenyl,

(e) 4'-[[2-n-propyl-4-methyl-6-(1-methyl-6-fluoro-benzimidazol-2-yl)-benzimida zol-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-methylbenzimi dazole-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-methylben zimidazol-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.
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