# US 5,703,110 A · Benzimidazole derivatives, their production and use

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- Number: US 5,703,110 A
- Document ID: US5703110A
- Status: Granted
- Kind: A
- Application number: 08/715,100
- Filed: 1996-09-17
- Granted: 1997-12-30
- Earliest claimed: 1990-04-27
- Assignees: Takeda Chemical Industries, Ltd.
- Inventors: Takehiko Naka; Kohei Nishikawa; Takeshi Kato
- Web page: https://patentgrep.com/patent/US5703110A

## CPC

- C07D 235/02: condensed with carbocyclic rings or ring systems
- C07D 235/26: Oxygen atoms
- C07D 235/28: Sulfur atoms
- C07D 235/30: Nitrogen atoms not forming part of a nitro radical
- C07D 403/10: linked by a carbon chain containing aromatic rings
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

Benzimidazole derivatives of the formula (I): ##STR1## wherein the ring A is a benzene ring which may optionally contain substitution in addition to the R' group; R.sup.1 is hydrogen or an optionally substituted hydrocarbon residue; R.sup.2 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; R' is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or convertible to an anion; Y is --O--, --S(O).sub.m -- or --N(R.sup.4)-- wherein m is an integer of 0, 1 or 2 and R.sup.4 is hydrogen or an optionally substituted alkyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g. hypercardia, heart failure, cardiac infarction, etc.), strokes, cerebral apoplexy, nephritis, etc.

## Claims

### Claim 1

2-Ethoxy-1-››2'-(1H-tetrazol-5-yl) biphenyl-4-yl!methyl!benzimidazole-7-carboxylic acid or a pharmaceutically acceptable salt thereof.

### Claim 2

A pharmaceutical composition for antagonizing angiotensin II which comprises a therapeutically effective amount of 2-ethoxy-1-››2'-(1H-tetrazol-5-yl)biphenyl-4-)-methyl!benzimidazole-7-carb oxylic acid or a pharmaceutically acceptable salt thereof in admixture with a pharmaceutically acceptable carrier, excipient or diluent therefor.

### Claim 3

A method for antagonizing angiotensin II in a mammal which comprises administering to said mammal a therapeutically effective amount of 2-ethoxy-1-››(2'-(1H-tetrazol-5-yl)biphenyl-4-yl!methyl!benzimidazole-7-ca rboxylic acid or a pharmaceutically acceptable salt thereof.