N-terminally modified GLP-1 receptor modulators

US7960349B2 · kind B2 · utility

Assignee

• Bristol-Myers Squibb Company · US

Inventors

• William R. Ewing · Yardley, US
• Claudio Mapelli · Princeton, US
• Douglas James Riexinger · Flemington, US
• Ving Lee · Hillsborough Township, US
• Richard B. Sulsky · Somerville, US
• Yeheng Zhu · Stockton, US

Key dates

• Filing date: May 25, 2007
• Grant date: Jun 14, 2011
• Expiry date: Dec 1, 2029

Classification

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

Abstract

The subject matter described herein provides novel human glucagon-like peptide-1 (GLP-1) receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. The described compounds include chemically modified peptides that may stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The disclosed and claimed peptides show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.