NOVEL GLP-1 RECEPTOR AGONISTS WITH CHOLESTEROL EFFLUX ACTIVITY

摘要

The present invention provides novel glucagon-like protein-1 (GLP-1) receptor agonist compounds that promote cholesterol efflux. The ABCA1-mediated cholesterol efflux present invention also provides compositions comprising the novel glucagon-like protein-1(GLP-1) receptor agonist compounds, and relates to the use of said compounds in therapy, to methods of treatment comprising administration of said compounds to patients, and to the use of said compounds in the manufacture of medicaments.

主权项

1. A GLP-1 receptor agonist peptide which in an alpha helical conformation comprise an amphipathic helix, wherein said peptide has cholesterol efflux activity with an Emax of at least 65% of that of L-4F, and a GLP-1 receptor potency measured as EC50, that is better than the potency of L-4F, when measured according to the methods described in Example 6.