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

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 activat...

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Main Authors ATSUO KUKI, LARRY KENNETH TRUESDALE, MIN TENG, RICHARD A. BYCHOWSKI, TSO-SHENG CHOU, VLAD EDWARD GREGOR, RANJAN JAGATH RAJAPAKSE, MICHAEL DAVID JOHNSON, ANTHONY L. LING, JAVIER GONZALEZ, DAN KIEL, DALJIT S. DHANOA, YUFENG HONG
Format Patent
LanguageEnglish
Published 26.06.2000
Edition7
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary: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.
Bibliography:Application Number: AU20000000175