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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: bruno jg. 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
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: bruno jg. 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: bruno jg. 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
[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.
Bell IM, Gallicchio SN, Stump CA, Bruno JG, Fan H, Gantert LT, Hostetler ED, Kemmerer AL, McWherter M, Moore EL, Mosser SD, Purcell ML, Riffel K, Salvatore CA, Sanabria-Bohórquez S, Staas DD, White RB, Williams M, Zartman CB, Cook JJ, Hargreaves RJ, Kane SA, Graham SL, Selnick HG. Bell IM, et al. Among authors: bruno jg. ACS Med Chem Lett. 2013 Jul 18;4(9):863-8. doi: 10.1021/ml400199p. eCollection 2013 Sep 12. ACS Med Chem Lett. 2013. PMID: 24900761 Free PMC article.
Novel oxazolidinone calcitonin gene-related peptide (CGRP) receptor antagonists for the acute treatment of migraine.
Crowley BM, Stump CA, Nguyen DN, Potteiger CM, McWherter MA, Paone DV, Quigley AG, Bruno JG, Cui D, Culberson JC, Danziger A, Fandozzi C, Gauvreau D, Kemmerer AL, Menzel K, Moore EL, Mosser SD, Reddy V, White RB, Salvatore CA, Kane SA, Bell IM, Selnick HG, Fraley ME, Burgey CS. Crowley BM, et al. Among authors: bruno jg. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4777-4781. doi: 10.1016/j.bmcl.2015.07.021. Epub 2015 Jul 14. Bioorg Med Chem Lett. 2015. PMID: 26231160
Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant.
Raheem IT, Breslin MJ, Bruno J, Cabalu TD, Cooke A, Cox CD, Cui D, Garson S, Gotter AL, Fox SV, Harrell CM, Kuduk SD, Lemaire W, Prueksaritanont T, Renger JJ, Stump C, Tannenbaum PL, Williams PD, Winrow CJ, Coleman PJ. Raheem IT, et al. Bioorg Med Chem Lett. 2015 Feb 1;25(3):444-50. doi: 10.1016/j.bmcl.2014.12.056. Epub 2014 Dec 23. Bioorg Med Chem Lett. 2015. PMID: 25577040
Discovery of MK-3697: a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.
Roecker AJ, Reger TS, Mattern MC, Mercer SP, Bergman JM, Schreier JD, Cube RV, Cox CD, Li D, Lemaire W, Bruno JG, Harrell CM, Garson SL, Gotter AL, Fox SV, Stevens J, Tannenbaum PL, Prueksaritanont T, Cabalu TD, Cui D, Stellabott J, Hartman GD, Young SD, Winrow CJ, Renger JJ, Coleman PJ. Roecker AJ, et al. Among authors: bruno jg. Bioorg Med Chem Lett. 2014 Oct 15;24(20):4884-90. doi: 10.1016/j.bmcl.2014.08.041. Epub 2014 Aug 26. Bioorg Med Chem Lett. 2014. PMID: 25248679
102 results