# US 5,705,525 A · Thiophene compounds

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- Number: US 5,705,525 A
- Document ID: US5705525A
- Status: Granted
- Kind: A
- Application number: 08/605,537
- Filed: 1996-02-22
- Granted: 1998-01-06
- Earliest claimed: 1995-02-23
- Assignees: Adir et Compagnie
- Inventors: Michel Wierzbicki; Frederic Sauveur; Jacqueline Bonnet; Charles Tordjman
- Web page: https://patentgrep.com/patent/US5705525A

## CPC

- C07D 333/24: Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 17/00: Drugs for dermatological disorders
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The invention relates to thiophene compounds of formula: ##STR1## wherein: X.sub.1, X.sub.2, Y.sub.1 and Y.sub.2, which are identical or different, each represents hydrogen or halogen, (C.sub.1 -C.sub.5)-alkyl or alkoxy, or trifluoromethyl, R.sub.1 represents hydrogen or (C.sub.1 -C.sub.5)-alkyl, A represents a straight (C.sub.1 -C.sub.5)-hydrocarbon chain of which each carbon atom is optionally mono- or di-substituted by a (C.sub.1 -C.sub.5)-alkyl, and R.sub.2 represents hydrogen, (C.sub.1 -C.sub.6)-alkyl, cyclohexyl or benzyl; and their physiologically tolerable salts. The products of the invention may be used as anti-inflammatory agents.

## Claims

### Claim 1

A thiophene compound selected from those of formula I: ##STR53## wherein: X.sub.1, X.sub.2, Y.sub.1 and Y.sub.2, which are identical or different, each represents (C.sub.1 -C.sub.5) alkoxy each in straight or branched chain,
R.sub.1 represents hydrogen;
A represents a straight (C.sub.1 -C.sub.2) hydrocarbon chain, and
R.sub.2 represents (C.sub.1 -C.sub.5) alkyl in straight or branched chain;
and physiologically tolerable addition salts thereof with appropriate bases.

### Claim 2 (depends on 1)

A compound of claim 1 selected from the group consisting of 3-›4,5-bis(4-methoxyphenyl) thien-2-yl!-N-hydroxy-N-methylpropionamide and a calcium salt thereof.

### Claim 3 (depends on 1)

A compound of claim 1 which is 4-›4,5-bis(4-methoxyphenyl) thien-2-yl!-N-hydroxy-N-methylbutanamide.

### Claim 4 (depends on 1)

A compound of claim 1 which is 3-›4,5-bis(4-methoxyphenyl) thien-2-yl!-N-ethyl-N-hydroxypropionamide.

### Claim 5 (depends on 1)

A method for treating a living animal body afflicted with a rheumatological inflammation or inflammation of the intestinal or cutaneous type in which leukotrienes are implicated, comprising the step of administering to the living animal body an amount of a compound of claim 1 which is effective for alleviation of said condition.

### Claim 6 (depends on 1)

A pharmaceutical composition useful in the treatment of rheumatological inflammation comprising as active ingredient a compound according to claim 1, alone or in combination with one or more pharmaceutical excipients.