Co-agonists of the glucagon and GLP-1 receptors

US10413593B2 · kind B2 · utility

Assignee

• Merck Sharp & Dohme LLC · US

Inventors

• Elisabetta Bianchi · Pomezia, IT
• Paul E. Carrington · San Mateo, US
• Qiaolin Deng · Edison, US
• Ravi Nargund · East Brunswick Township, US
• Federica Orvieto · Roma, IT
• Anandan Palani · Bound Brook, US
• Antonello Pessi · Roma, IT
• Thomas J. Tucker · North Wales, US
• Chengwei Wu · Ambler, US

Key dates

• Filing date: Oct 22, 2015
• Grant date: Sep 17, 2019
• Expiry date: Oct 22, 2035

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07K14/605
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Described are peptide analogs of glucagon, which have been modified to be resistant to cleavage and inactivation by dipeptidyl peptidase IV (DPP-IV) and to increase in vivo half-life of the peptide analog while enabling the peptide analog to have relatively balanced agonist activity at the glucagon-like peptide 1 (GLP-1) receptor and the glucagon (GCG) receptor, and the use of such GLP-1 receptor/GCG receptor co-agonists for treatment of metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.