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Page 1
Identification of novel, orally bioavailable spirohydantoin CGRP receptor antagonists.
Bell IM, Bednar RA, Fay JF, Gallicchio SN, Hochman JH, McMasters DR, Miller-Stein C, Moore EL, Mosser SD, Pudvah NT, Quigley AG, Salvatore CA, Stump CA, Theberge CR, Wong BK, Zartman CB, Zhang XF, Kane SA, Graham SL, Vacca JP, Williams TM. Bell IM, et al. Bioorg Med Chem Lett. 2006 Dec 15;16(24):6165-9. doi: 10.1016/j.bmcl.2006.09.045. Epub 2006 Oct 5. Bioorg Med Chem Lett. 2006. PMID: 17027263
Pharmacological characterization of MK-0974 [N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide], a potent and orally active calcitonin gene-related peptide receptor antagonist for the treatment of migraine.
Salvatore CA, Hershey JC, Corcoran HA, Fay JF, Johnston VK, Moore EL, Mosser SD, Burgey CS, Paone DV, Shaw AW, Graham SL, Vacca JP, Williams TM, Koblan KS, Kane SA. Salvatore CA, et al. J Pharmacol Exp Ther. 2008 Feb;324(2):416-21. doi: 10.1124/jpet.107.130344. Epub 2007 Nov 26. J Pharmacol Exp Ther. 2008. PMID: 18039958
The discovery of highly potent CGRP receptor antagonists.
Stump CA, Bell IM, Bednar RA, Bruno JG, Fay JF, Gallicchio SN, Johnston VK, Moore EL, Mosser SD, Quigley AG, Salvatore CA, Theberge CR, Blair Zartman C, Zhang XF, Kane SA, Graham SL, Vacca JP, Williams TM. Stump CA, et al. Bioorg Med Chem Lett. 2009 Jan 1;19(1):214-7. doi: 10.1016/j.bmcl.2008.10.106. Epub 2008 Oct 31. Bioorg Med Chem Lett. 2009. PMID: 19010673
The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists.
Bell IM, Bednar RA, Corcoran HA, Fay JF, Gallicchio SN, Johnston VK, Hershey JC, Miller-Stein CM, Moore EL, Mosser SD, Roller SA, Salvatore CA, Theberge CR, Wong BK, Blair Zartman C, Kane SA, Williams TM, Graham SL, Vacca JP. Bell IM, et al. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4740-2. doi: 10.1016/j.bmcl.2009.06.057. Epub 2009 Jun 17. Bioorg Med Chem Lett. 2009. PMID: 19577468
Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist.
Salvatore CA, Moore EL, Calamari A, Cook JJ, Michener MS, O'Malley S, Miller PJ, Sur C, Williams DL Jr, Zeng Z, Danziger A, Lynch JJ, Regan CP, Fay JF, Tang YS, Li CC, Pudvah NT, White RB, Bell IM, Gallicchio SN, Graham SL, Selnick HG, Vacca JP, Kane SA. Salvatore CA, et al. J Pharmacol Exp Ther. 2010 Apr;333(1):152-60. doi: 10.1124/jpet.109.163816. Epub 2010 Jan 11. J Pharmacol Exp Ther. 2010. PMID: 20065019
Identification of potent, highly constrained CGRP receptor antagonists.
Stump CA, Bell IM, Bednar RA, Fay JF, Gallicchio SN, Hershey JC, Jelley R, Kreatsoulas C, Moore EL, Mosser SD, Quigley AG, Roller SA, Salvatore CA, Sharik SS, Theberge CR, Zartman CB, Kane SA, Graham SL, Selnick HG, Vacca JP, Williams TM. Stump CA, et al. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2572-6. doi: 10.1016/j.bmcl.2010.02.086. Epub 2010 Feb 25. Bioorg Med Chem Lett. 2010. PMID: 20299218
4,284 results