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Page 1
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
Bell IM, Stump CA, Gallicchio SN, Staas DD, Zartman CB, Moore EL, Sain N, Urban M, Bruno JG, Calamari A, Kemmerer AL, Mosser SD, Fandozzi C, White RB, Zrada MM, Selnick HG, Graham SL, Vacca JP, Kane SA, Salvatore CA. Bell IM, et al. Among authors: stump ca. Bioorg Med Chem Lett. 2012 Jun 15;22(12):3941-5. doi: 10.1016/j.bmcl.2012.04.105. Epub 2012 Apr 30. Bioorg Med Chem Lett. 2012. PMID: 22607672
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: stump ca. 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: stump ca. 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: stump ca. 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
Caprolactams as potent CGRP receptor antagonists for the treatment of migraine.
Shaw AW, Paone DV, Nguyen DN, Stump CA, Burgey CS, Mosser SD, Salvatore CA, Rutledge RZ, Kane SA, Koblan KS, Graham SL, Vacca JP, Williams TM. Shaw AW, et al. Among authors: stump ca. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4795-8. doi: 10.1016/j.bmcl.2007.06.062. Epub 2007 Jun 26. Bioorg Med Chem Lett. 2007. PMID: 17616394
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
Novel CGRP receptor antagonists through a design strategy of target simplification with addition of molecular flexibility.
Wood MR, Schirripa KM, Kim JJ, Quigley AG, Stump CA, Bell IM, Bednar RA, Fay JF, Bruno JG, Moore EL, Mosser SD, Roller S, Salvatore CA, Kane SA, Vacca JP, Selnick HG. Wood MR, et al. Among authors: stump ca. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5787-90. doi: 10.1016/j.bmcl.2009.07.134. Epub 2009 Aug 6. Bioorg Med Chem Lett. 2009. PMID: 19703767
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
Discovery of MK-3207: A Highly Potent, Orally Bioavailable CGRP Receptor Antagonist.
Bell IM, Gallicchio SN, Wood MR, Quigley AG, Stump CA, Zartman CB, Fay JF, Li CC, Lynch JJ, Moore EL, Mosser SD, Prueksaritanont T, Regan CP, Roller S, Salvatore CA, Kane SA, Vacca JP, Selnick HG. Bell IM, et al. Among authors: stump ca. ACS Med Chem Lett. 2010 Jan 12;1(1):24-9. doi: 10.1021/ml900016y. eCollection 2010 Apr 8. ACS Med Chem Lett. 2010. PMID: 24900170 Free PMC article.
20 results