Small molecule ago-allosteric modulators of the human glucagon-like peptide-1 (hGLP-1) receptor
摘要:
Following our previous publication describing the biological profiles, we herein describe the structure-activity relationships of a core set of quinoxalines as the hGLP-1 receptor agonists. The most potent and efficacious compounds are 6,7-dichloroquinoxalines bearing an alkyl sulfonyl group at the C-2 position and a secondary alkyl amino group at the C-3 position. These findings serve as a valuable starting point for the discovery of more drug-like small molecule agonists for the hGLP-1 receptor. (C) Elsevier Ltd. All rights reserved.
[EN] NON-PEPTIDE GLP-1 AGONISTS<br/>[FR] AGONISTES NON PEPTIDIQUES DE GLP-1
申请人:NOVO NORDISK AS
公开号:WO2000042026A1
公开(公告)日:2000-07-20
Novel non-peptide GLP-1 agonists, pharmaceutical compositions comprising them, use of the non-peptide GLP-1 agonists for the preparation of pharmaceutical compositions and methods for the treatment and/or prevention of disorders and diseases wherein an activation of the human GLP-1 receptor is beneficial, especially metabolic disorders such as IGT, Type 1 diabetes, Type 2 diabetes and obesity.