UCLA Bristol-Myers Squibb Lectureship: "Heterocycles as Bioisosteres in the Discovery of Orally Active CGRP Receptor Antagonists for the Treatment of Migraine"

Seminar series
Organic Colloquium
When
Thu, May 1 4:00pm
Where
Cram Conference Room – 3440 Molecular Sciences Bldg
Speaker Dr. John E. Macor
Executive Director of Immunoscience Discovery Chemistry
Bristol-Myers Squibb Co.
Description

UCLA Bristol-Myers Squibb Lectureship

"Heterocycles as Bioisosteres in the Discovery of Orally Active CGRP Receptor Antagonists for the Treatment of Migraine"

Abstract.  The use of heterocycles as replacements for amides, esters and other groups in biologically active molecules to make drug-like molecules will be reviewed. Concepts of this will be demonstrated for the discovery of antagonists of the CGRP (calcitonin gene-related peptide) receptor, which have been shown to be clinically effective in the acute treatment of migraine headaches.  In this seminar, the discovery of a series of CGRP receptor antagonists will be presented.  Specifically, the discovery of an intranasally bioavailable, picomolar potent CGRP receptor antagonist (BMS-742413) and an orally bioavailable picomolar CGRP receptor antagonist (BMS-927711) will be detailed.  Ph I and Ph II clinical results for BMS-927711 will also be presented.

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