Journal of Medicinal Chemistry p. 10644 - 10651 (2012)
Update date:2022-08-03
Topics:
Luo, Guanglin
Chen, Ling
Conway, Charles M.
Denton, Rex
Keavy, Deborah
Signor, Laura
Kostich, Walter
Lentz, Kimberley A.
Santone, Kenneth S.
Schartman, Richard
Browning, Marc
Tong, Gary
Houston, John G.
Dubowchik, Gene M.
MacOr, John E.
Calcitonin gene-related peptide (CGRP) receptor antagonists have demonstrated clinical efficacy in the treatment of acute migraine. Herein, we describe the design, synthesis, and preclinical characterization of a highly potent, oral CGRP receptor antagonist BMS-927711 (8). Compound 8 has good oral bioavailability in rat and cynomolgus monkey, attractive overall preclinical properties, and shows dose-dependent activity in a primate model of CGRP-induced facial blood flow. Compound 8 is presently in phase II clinical trials.
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