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Carbamates as potent calcitonin gene-related peptide antagonists with improved solution stability. | LitMetric

Carbamates as potent calcitonin gene-related peptide antagonists with improved solution stability.

Bioorg Med Chem Lett

Neuroscience Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492-7660, USA.

Published: July 2009

AI Article Synopsis

Article Abstract

The calcitonin gene-related peptide (CGRP) receptor has been implicated in the pathogenesis of migraine. A class of urethanamide derivatives has been identified as potent inhibitors of the CGRP receptor. Compound 20 was found to be among the most potent (IC(50)=17pM). It was shown to retain excellent aqueous solubility (>50mg/mL, pH 7) while dramatically improving solution stability as compared to our previously disclosed development candidate, BMS-694153 (1).

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http://dx.doi.org/10.1016/j.bmcl.2009.04.150DOI Listing

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