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Page 1
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. Among authors: johnston vk. 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
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: johnston vk. 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: johnston vk. 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: johnston vk. 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
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. Among authors: johnston vk. 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
Substituted benzothiadizine inhibitors of Hepatitis C virus polymerase.
Shaw AN, Tedesco R, Bambal R, Chai D, Concha NO, Darcy MG, Dhanak D, Duffy KJ, Fitch DM, Gates A, Johnston VK, Keenan RM, Lin-Goerke J, Liu N, Sarisky RT, Wiggall KJ, Zimmerman MN. Shaw AN, et al. Among authors: johnston vk. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4350-3. doi: 10.1016/j.bmcl.2009.05.091. Epub 2009 May 28. Bioorg Med Chem Lett. 2009. PMID: 19515564
Synthesis and biological activity of heteroaryl 3-(1,1-dioxo-2H-(1,2,4)-benzothiadizin-3-yl)-4-hydroxy-2(1H)-quinolinone derivatives as hepatitis C virus NS5B polymerase inhibitors.
Tedesco R, Chai D, Darcy MG, Dhanak D, Fitch DM, Gates A, Johnston VK, Keenan RM, Lin-Goerke J, Sarisky RT, Shaw AN, Valko KL, Wiggall KJ, Zimmerman MN, Duffy KJ. Tedesco R, et al. Among authors: johnston vk. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4354-8. doi: 10.1016/j.bmcl.2009.05.080. Epub 2009 May 27. Bioorg Med Chem Lett. 2009. PMID: 19505821
3-(1,1-dioxo-2H-(1,2,4)-benzothiadiazin-3-yl)-4-hydroxy-2(1H)-quinolinones, potent inhibitors of hepatitis C virus RNA-dependent RNA polymerase.
Tedesco R, Shaw AN, Bambal R, Chai D, Concha NO, Darcy MG, Dhanak D, Fitch DM, Gates A, Gerhardt WG, Halegoua DL, Han C, Hofmann GA, Johnston VK, Kaura AC, Liu N, Keenan RM, Lin-Goerke J, Sarisky RT, Wiggall KJ, Zimmerman MN, Duffy KJ. Tedesco R, et al. Among authors: johnston vk. J Med Chem. 2006 Feb 9;49(3):971-83. doi: 10.1021/jm050855s. J Med Chem. 2006. PMID: 16451063
18 results