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Generated: May 28, 2018

DrugPatentWatch Database Preview

Details for Patent: 5,594,003

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Title: Tetrahydroimidazo[1,2-a]pyridin-2-yl-(benzimidazol-1-yl)-methyl-biph enyls 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 compound is: 4'-[(2-Ethyl-4-methyl-6-(5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl)-ben zimidazol-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)
Filing Date:Jun 01, 1995
Application Number:08/456,337
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 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl 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 is in the 6-position and represents a 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl group,

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. 4'-[(2-Ethyl-4-methyl-6-(5,6,7,8-tetrahydro -imidazo[1,2-a]pyridin-2-yl)-benzimidazol-1-yl)-methyl]-biphenyl-2-carboxyl ic acid or a pharmaceutically acceptable salt thereof.

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

6. 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 or 4.

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UBS
Accenture
Healthtrust
QuintilesIMS
Cerilliant
Harvard Business School
Merck
Chinese Patent Office
Queensland Health

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