Calcitonin gene-related peptide (CGRP) receptor antagonists: novel aspartates and succinates.

Abstract Novel aspartate and succinateCGRP full antagonistswere identified through core modification of a potent lead CGRP antagonist, BMS-694153. While aspartates were much less active and had a flat SAR, some of the succinateswere very potent CGRP full antagonistsand matched the potencyof BMS-694153. The most potencyresides in the S enantiomer as demonstrated through an asymmetric synthesis.