Agouron Pharmaceuticals, Inc.

Tso-sheng Chou

Min Teng

Yufeng Hong

Daljit Singh Dhanoa

Vlad Edward Gregor

Anthony Lai Ling

Javier Gonzalez

Larry Kenneth Truesdale

Michael David Johnson

Atsuo Kuki

Dan Kiel

Ranjan Jagath Rajapakse

Richard A Bychowski

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.

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

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San Diego, CA, United States of America

Tso-sheng Chou