Non-peptide antagonists of GLP-1 receptor and methods of use

US6469021B1 · kind B1 · utility

Assignee

• Agouron Pharmaceuticals, Inc. · US

Inventors

• Larry Kenneth Truesdale · San Diego, US
• Richard A. Bychowski · Irvine, US
• Javier Gonzalez · Oceanside, US
• Atsuo Kuki · Encinitas, US
• Ranjan Rajapakse · San Diego, US
• Min Teng · Aliso Viejo, US
• Dan Kiel · San Diego, US
• Daljit S. Dhanoa · Wakefield, US
• Yufeng Hong · San Diego, US
• Tso-sheng Chou · San Diego, US
• Anthony Lai Ling · San Diego, US
• Michael David Johnson · Las Cruces, US
• Vlad Edward Gregor · Del Mar, US

Key dates

• Filing date: Oct 26, 2001
• Grant date: Oct 22, 2002
• Expiry date: Oct 26, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D491/14
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Non-peptide compounds that act as antagonists of the intestinal hormone glucagons-like peptide 1 (GLP-1) have a 9H-b-carboline central motif. The compounds exhibit advantageous physical, chemical and biological properties and inhibit GLP-1 peptide binding to the GLP-1 receptor and/or prevent activation of the receptor by bound GLP-1. The invention further relates to a method of inhibiting the binding of GLP-1 to the GLP-1 receptor and a method of inhibiting the activation of the GLP-1 receptor. Intermediate compounds useful for making non-peptide GLP-1 receptor antagonists are also described.