US 7,910,568 B2 · Derivatives of 4- or 5-aminosalicylic acid

Abstract

The present invention provides new derivatives of 4- or 5-aminosalicylic acid, and a pharmaceutical composition containing these derivatives of 4- or 5-aminosalicylic acid as active ingredients, useful for the treatment of intestinal diseases such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) and for the prevention/treatment of colon cancer. More particularly, these derivatives comprise a hydrogen sulfide releasing moiety linked via an azo, an ester, an anhydride, a thioester or an amide linkage to a molecule of 4- or 5-aminosalicylic acid. Furthermore, the present invention provides a process for preparing these compounds and their use for treating IBD and IBS and the prevention/treatment of colon cancer.

Claims17

Dependent claims

A compound of general formula:

A-L-R (I)
where:
A is
where —N═is either at position 4 or 5,
where —NH is either at position 4 or 5,
where —NH2 is either at position 4 or 5,
or
where —NH2 is either at position 4 or 5;
L is either O, O—C═O, S, N or a covalent bond, to form an ester linkage, an anhydride linkage, a thioester linkage, an amide linkage or an azo linkage;
and
R is a hydrogen sulfide releasing moiety that releases hydrogen sulfide in tissue selected from the group consisting of:
or a salt thereof.

9 more elements

Dependencies are inferred from the claim text.

Facts

Application

11/915,305Filed 31 Mar 2006

Priority

CA PCT/CA2005/00081927 May 2005

Published

US 2008/0207564 A128 Aug 2008

Granted

22 Mar 2011

Term ends

Not estimatedThe source records don’t support an estimate.

Classification16 codes

C07C 327/42
Having carbon atoms of thiocarboxamide groups bound to hydrogen atoms or to acyclic carbon atoms: to hydrogen atoms or to carbon atoms of a…
A61P 1/00
Drugs for disorders of the alimentary tract or the digestive system
A61P 1/04
Drugs for disorders of the alimentary tract or the digestive system: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of…
A61P 29/00
Non-central analgesic, antipyretic or antiinflammatory agents

Derivatives of 4- or 5-aminosalicylic acid

Life of this patent

Derivatives of 4- or 5-aminosalicylic acid

Life of this patent

Abstract

Claims17