Serine protease inhibitors

US6127340A · kind A · utility

Assignee

• Trigen GmbH · GB

Inventors

• Donovan St. Clair Green · London, GB
• Said Mohammed Anwr Ahmed Elgendy · London, GB
• Geeta Patel · London, GB
• Michael Scully · Spring House, US
• Christopher Goodwin · Avon, US
• Vijay Kakkar · Stockton, GB
• John Joseph Deadman · Sutton, GB

Key dates

• Filing date: Mar 30, 1998
• Grant date: Oct 3, 2000
• Expiry date: Mar 30, 2018

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This invention is directed to peptide inhibitors of serine proteases, espcecially thrombin, in which the P1-P2 natural amide linkage is replaced by another bond. Exemplary thrombin inhibitors have the formula: X-(aa.sup.3)-(aa.sup.2)-.psi.-(aa.sup.1)-Z wherein X is H or a substituent on the N-terminal amino group, aa.sup.3 is a hydrophobic amino acid, aa.sup.23 is Pro, aa.sup.1 is Arg or an Arg analgoue, Z is --COOH or a heteroatom acid group and .psi. is a non-amide linkage.