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Potent benzimidazolone-based CGRP receptor antagonists |
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| Authors: | Theberge Cory R Bednar Rodney A Bell Ian M Corcoran Halea A Fay John F Hershey James C Johnston Victor K Kane Stefanie A Mosser Scott Salvatore Christopher A Williams Theresa M Zartman C Blair Zhang Xu-Fang Graham Samuel L Vacca Joseph P |
| Affiliation: | Department of Medicinal Chemistry, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA. cory_theberge@merck.com |
| Abstract: | The previously disclosed spirohydantoin-based CGRP receptor antagonists were optimized for potency through modification of the benzimidazolone substituents. Compounds were identified which had minimal shift in the cAMP functional assay containing 50% human serum. Blockade of CGRP-mediated vasodilation was observed with these compounds in a rhesus pharmacodynamic assay and the in vivo potency correlated with the in vitro activity in the serum-shifted functional assay. |
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