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Page 1
Invention of novel 3-aminopiperidin-2-ones as calcitonin gene-related peptide receptor antagonists.
Staas DD, Bell IM, Burgey CS, Deng JZ, Gallicchio SN, Lim JJ, Paone DV, Potteiger CM, Shaw AW, Stevenson H, Stump CA, Blair Zartman C, Moore EL, Bruno JG, Mosser SD, White RB, Kane SA, Salvatore CA, Graham SL, Williams TM, Selnick HG, Fraley ME. Staas DD, et al. Among authors: fraley me. Bioorg Med Chem Lett. 2024 Nov 1;112:129944. doi: 10.1016/j.bmcl.2024.129944. Epub 2024 Sep 2. Bioorg Med Chem Lett. 2024. PMID: 39233187
Fluorinated Isoindolinone-Based Glucosylceramide Synthase Inhibitors with Low Human Dose Projections.
Loughran HM, Schirripa KM, Roecker AJ, Breslin MJ, Tong L, Fillgrove KL, Kuo Y, Bleasby K, Collier H, Altman MD, Ford MC, Newman JA, Drolet RE, Cosden M, Jinn S, Flick RB, Liu X, Minnick C, Watt ML, Lemaire W, Burlein C, Adam GC, Austin LA, Marcus JN, Smith SM, Fraley ME. Loughran HM, et al. Among authors: fraley me. ACS Med Chem Lett. 2023 Dec 21;15(1):123-131. doi: 10.1021/acsmedchemlett.3c00436. eCollection 2024 Jan 11. ACS Med Chem Lett. 2023. PMID: 38229758 Free PMC article.
Pyrazole Ureas as Low Dose, CNS Penetrant Glucosylceramide Synthase Inhibitors for the Treatment of Parkinson's Disease.
Roecker AJ, Schirripa KM, Loughran HM, Tong L, Liang T, Fillgrove KL, Kuo Y, Bleasby K, Collier H, Altman MD, Ford MC, Drolet RE, Cosden M, Jinn S, Hatcher NG, Yao L, Kandebo M, Vardigan JD, Flick RB, Liu X, Minnick C, Price LA, Watt ML, Lemaire W, Burlein C, Adam GC, Austin LA, Marcus JN, Smith SM, Fraley ME. Roecker AJ, et al. Among authors: fraley me. ACS Med Chem Lett. 2023 Jan 12;14(2):146-155. doi: 10.1021/acsmedchemlett.2c00441. eCollection 2023 Feb 9. ACS Med Chem Lett. 2023. PMID: 36793422 Free PMC article.
Characterization of Ubrogepant: A Potent and Selective Antagonist of the Human Calcitonin Gene‒Related Peptide Receptor.
Moore E, Fraley ME, Bell IM, Burgey CS, White RB, Li CC, Regan CP, Danziger A, Stranieri Michener M, Hostetler E, Banerjee P, Salvatore C. Moore E, et al. Among authors: fraley me. J Pharmacol Exp Ther. 2020 Jan 28:jpet.119.261065. doi: 10.1124/jpet.119.261065. Online ahead of print. J Pharmacol Exp Ther. 2020. PMID: 31992609 Free 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: fraley me. 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
Adenosine analogue inhibitors of S-adenosylhomocysteine hydrolase.
Converso A, Hartingh T, Fraley ME, Garbaccio RM, Hartman GD, Huang SY, Majercak JM, McCampbell A, Na SJ, Ray WJ, Savage MJ, Wolffe C, Yeh S, Yu Y, White R, Zhang R. Converso A, et al. Among authors: fraley me. Bioorg Med Chem Lett. 2014 Jun 15;24(12):2737-40. doi: 10.1016/j.bmcl.2014.04.034. Epub 2014 Apr 18. Bioorg Med Chem Lett. 2014. PMID: 24813734
Discovery of 5''-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide (MK-1064): a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.
Roecker AJ, Mercer SP, Schreier JD, Cox CD, Fraley ME, Steen JT, 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: fraley me. ChemMedChem. 2014 Feb;9(2):311-22. doi: 10.1002/cmdc.201300447. Epub 2013 Dec 27. ChemMedChem. 2014. PMID: 24376006
Pyridyl aminothiazoles as potent inhibitors of Chk1 with slow dissociation rates.
Dudkin VY, Rickert K, Kreatsoulas C, Wang C, Arrington KL, Fraley ME, Hartman GD, Yan Y, Ikuta M, Stirdivant SM, Drakas RA, Walsh ES, Hamilton K, Buser CA, Lobell RB, Sepp-Lorenzino L. Dudkin VY, et al. Among authors: fraley me. Bioorg Med Chem Lett. 2012 Apr 1;22(7):2609-12. doi: 10.1016/j.bmcl.2012.01.110. Epub 2012 Feb 9. Bioorg Med Chem Lett. 2012. PMID: 22374217
36 results