# US 5,352,692 A · Thiophene-2-carboxylic acid derivatives

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- Number: US 5,352,692 A
- Document ID: US5352692A
- Status: Granted
- Kind: A
- Application number: 07/938,166
- Filed: 1993-02-04
- Granted: 1994-10-04
- Earliest claimed: 1991-04-04
- Assignees: Laevosan Gesellschaft m. b. H.
- Inventors: Gerhard Greier; Dieter Binder
- Web page: https://patentgrep.com/patent/US5352692A

## CPC

- C07D 249/08: 1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
- A61P 3/08: for glucose homeostasis (pancreatic hormones A61P5/48)
- A61P 9/08: Vasodilators for multiple indications
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 9/12: Antihypertensives
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- C07D 231/12: with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D 233/56: with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

There are described novel compounds of the general formula ##STR1## in which R in position 3 or 4 is hydrogen, methyl, chlorine or bromine and R.sup.2 is C.sub.1 -C.sub.10 -alkyl, C.sub.3 -C.sub.7 -cycloalkyl or benzyl, and the pharmaceutically acceptable addition salts thereof with weak organic acids as well as a process for the preparation thereof. The compounds of formula (I) are inhibitors of thromboxane synthetase.

## Claims

### Claim 1

A compound of formula (I) ##STR6## in which R in position 3 or 4 is hydrogen, methyl, chlorine or bromine and R.sup.2 is C.sub.1 -C.sub.10 -alkyl, C.sub.3 -C.sub.7 - cycloalkyl or benzyl, or a pharmaceutically acceptable addition salt thereof with weak organic acids.

### Claim 2

1-Ethoxycarbonyloxyethyl ester of 5-[2-(1H-imidazole-1-yl)-ethoxyl]-thiophene-2-carboxylic acid.

### Claim 3

1-Ethoxycarbonyloxyethyl ester fumarate of 5-[2-(1H-imidazole-1-yl)-ethoxy]-thiophene-2-carboxyl acid.

### Claim 4 (depends on 1)

Pharmaceutical composition for oral administration, characterized in that it comprises an effective amount compound of formula (I) as defined in claim 1, or a pharmaceutically acceptable addition salt thereof with a weak organic acid, together with a pharmaceutically acceptable carrier or diluent.

### Claim 5 (depends on 1)

A method of use of a compound of formula (I) as defined in claim 1, comprising administering a compound of formula (I) in the form of a medicament in an amount thereof effective as an inhibitor of thromboxane synthetase for treating diseases caused by thromboxane A.sub.2.