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The identification of potent,orally bioavailable tricyclic CGRP receptor antagonists |
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| Authors: | Ian M. Bell Rodney A. Bednar Halea A. Corcoran John F. Fay Steven N. Gallicchio Victor K. Johnston James C. Hershey Cynthia M. Miller-Stein Eric L. Moore Scott D. Mosser Shane A. Roller Christopher A. Salvatore Cory R. Theberge Bradley K. Wong C. Blair Zartman Stefanie A. Kane Theresa M. Williams Samuel L. Graham Joseph P. Vacca |
| Affiliation: | 1. Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA;2. Department of Pain Research, Merck Research Laboratories, West Point, PA 19486, USA;3. Department of Bone Respiratory Immunology & Endocrine, Merck Research Laboratories, West Point, PA 19486, USA;4. Department of Drug Metabolism, Merck Research Laboratories, West Point, PA 19486, USA |
| Abstract: | A series of tricyclic CGRP receptor antagonists was optimized in order to improve oral bioavailability. Attenuation of polar surface area and incorporation of a weakly basic indoline nitrogen led to compound 5, a potent antagonist with good oral bioavailability in three species. |
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