Peptide inhibitors of hepatitis C virus NS3 protease

US6867284B1 · kind B1 · utility

Assignee

• Istituto di Recerche di Biologia Molecolare P. Angeletti S.R.L. · IT

Inventors

• Victor Giulio Matassa · Roma, IT
• Frank Narjes · Ariccia, IT
• Konrad Koehler · Huddinge, SE
• Jesus Maria Ontoria · Barcelona, ES
• Marco Poma · Grosseto, IT
• Antonella Marchetti · Norcia, IT

Key dates

• Filing date: Jun 9, 1999
• Grant date: Mar 15, 2005
• Expiry date: Jun 9, 2019

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2601/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Fluorinated oligopeptides, especially those having 4,4-difluoro-2-amino butyric acid at the C terminus, may be effective inhibitors of hepatitis C virus NS3 protease. Examples of hexapeptides of the invention, optimized for binding in the S1 specificity pocket of the enzyme, may display IC50s at the sub-micromolar level. Embodiments of tripeptides of the invention, having a keto-acid group at the C-terminus are, likewise, potent inhibitors of NS3 protease.