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Page 1
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. Among authors: kane sa. 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
Non-peptide calcitonin gene-related peptide receptor antagonists from a benzodiazepinone lead.
Williams TM, Stump CA, Nguyen DN, Quigley AG, Bell IM, Gallicchio SN, Zartman CB, Wan BL, Penna KD, Kunapuli P, Kane SA, Koblan KS, Mosser SD, Rutledge RZ, Salvatore C, Fay JF, Vacca JP, Graham SL. Williams TM, et al. Among authors: kane sa. Bioorg Med Chem Lett. 2006 May 15;16(10):2595-8. doi: 10.1016/j.bmcl.2006.02.051. Epub 2006 Mar 9. Bioorg Med Chem Lett. 2006. PMID: 16527483
Benzodiazepine calcitonin gene-related peptide (CGRP) receptor antagonists: optimization of the 4-substituted piperidine.
Burgey CS, Stump CA, Nguyen DN, Deng JZ, Quigley AG, Norton BR, Bell IM, Mosser SD, Salvatore CA, Rutledge RZ, Kane SA, Koblan KS, Vacca JP, Graham SL, Williams TM. Burgey CS, et al. Among authors: kane sa. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5052-6. doi: 10.1016/j.bmcl.2006.07.044. Epub 2006 Aug 2. Bioorg Med Chem Lett. 2006. PMID: 16889959
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. Among authors: kane sa. 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
Potent, orally bioavailable calcitonin gene-related peptide receptor antagonists for the treatment of migraine: discovery of 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 (MK-0974).
Paone DV, Shaw AW, Nguyen DN, Burgey CS, Deng JZ, Kane SA, Koblan KS, Salvatore CA, Mosser SD, Johnston VK, Wong BK, Miller-Stein CM, Hershey JC, Graham SL, Vacca JP, Williams TM. Paone DV, et al. Among authors: kane sa. J Med Chem. 2007 Nov 15;50(23):5564-7. doi: 10.1021/jm070668p. Epub 2007 Oct 11. J Med Chem. 2007. PMID: 17929795
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. Among authors: kane sa. 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
Potent benzimidazolone-based CGRP receptor antagonists.
Theberge CR, Bednar RA, Bell IM, Corcoran HA, Fay JF, Hershey JC, Johnston VK, Kane SA, Mosser S, Salvatore CA, Williams TM, Zartman CB, Zhang XF, Graham SL, Vacca JP. Theberge CR, et al. Among authors: kane sa. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6122-5. doi: 10.1016/j.bmcl.2008.10.019. Epub 2008 Oct 7. Bioorg Med Chem Lett. 2008. PMID: 18947992
136 results