1289023-94-4Relevant articles and documents
Discovery of (5S,6S,9R)-5-aqmino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro- 5H-cyclohepta[b]pyridin-9-yl4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl) piperidine-1-carboxylate (BMS-927711): An oral Calcitonin Gene-Related Peptide (CGRP) antagonist in cinical trials for treating migraine
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.
, p. 10644 - 10651 (2013/02/23)
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.
CGRP RECEPTOR ANTAGONISTS
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, (2011/05/05)
The disclosure generally relates to the novel compounds of formula (I), including pharmaceutically acceptable salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD).
