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Generated: September 23, 2017

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Title: (Alkanesultam-1-yl)-benzimidazol-1-yl)-1yl)-methyl-biphenyls useful as angiotensin-II antagonists
Abstract: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: 4'-[(2-n-propyl-4-methyl-6-(butanesultam-1-yl)benzimidazol-1-yl)-methyl]-b iphenyl-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: Karl Thomae GmbH (Biberach an der Riss, DE)
Filing Date:Jun 01, 1995
Application Number:08/456,978
Claims:1. A compound of the formula I ##STR30## wherein R.sub.1 is in the 4-position and represents a C.sub.1-4 -alkyl, C.sub.3-7 -cycloalkyl or trifluoromethyl group,

R.sub.2 represents a 5-, 6- or 7-membered alkyleneimino group in which a methylene group is replaced by a sulphonyl, or R.sub.2 represents a 5-, 6- or 7-membered alkyleneimino group which is substituted by one or two C.sub.1-3 -alkyl groups and in which alkyleneimino group a methylene group is replaced by a sulphonyl,

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. A compound of formula I, in accordance with claim 1, wherein

R.sub.2 is the 6-position,

or a pharmaceutically acceptable salt thereof.

3. A compound of formula I, in accordance with claim 2, wherein

R.sub.4 is a 1H-tretazolyl or carboxy group,

or a pharmaceutically acceptable salt thereof.

4. A compound of formula I, in accordance with claim 3, wherein

R.sub.2 is a propanesultam-1-yl or butanesultam-1-yl group,

or a pharmaceutically acceptable salt thereof.

5. A compound of formula I, in accordance with claim 4, wherein

R.sub.2 is a butanesultam-1-yl group,

or a pharmaceutically acceptable salt thereof.

6. 4'-[[2-n-Propyl-4-methyl-6-(butanesultam-1- yl)-benzimidazol-1-yl]-methyl]-2-(1H-tetrazol-5-yl)-biphenyl or a pharmaceutically acceptable salt thereof.

7. A pharmaceutical composition comprising a compound as in any one 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 as in any one of claims 1, 2, 3, 4, 5 or 6.
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