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Discovery of the Oxadiazine FRM-024: A Potent CNS-Penetrant Gamma Secretase Modulator.
Bursavich MG, Harrison BA, Acharya R, Costa DE, Freeman EA, Hrdlicka LA, Jin H, Kapadnis S, Moffit JS, Murphy D, Nolan SJ, Patzke H, Tang C, Van Voorhies HE, Wen M, Koenig G, Blain JF, Burnett DA. Bursavich MG, et al. Among authors: nolan sj. J Med Chem. 2021 Oct 14;64(19):14426-14447. doi: 10.1021/acs.jmedchem.1c00904. Epub 2021 Sep 22. J Med Chem. 2021. PMID: 34550687
Design, Synthesis, and Evaluation of a Novel Series of Oxadiazine Gamma Secretase Modulators for Familial Alzheimer's Disease.
Bursavich MG, Harrison BA, Acharya R, Costa DE, Freeman EA, Hodgdon HE, Hrdlicka LA, Jin H, Kapadnis S, Moffit JS, Murphy DA, Nolan S, Patzke H, Tang C, Wen M, Koenig G, Blain JF, Burnett DA. Bursavich MG, et al. J Med Chem. 2017 Mar 23;60(6):2383-2400. doi: 10.1021/acs.jmedchem.6b01620. Epub 2017 Mar 10. J Med Chem. 2017. PMID: 28230986
Modulation of γ-secretase by EVP-0015962 reduces amyloid deposition and behavioral deficits in Tg2576 mice.
Rogers K, Felsenstein KM, Hrdlicka L, Tu Z, Albayya F, Lee W, Hopp S, Miller MJ, Spaulding D, Yang Z, Hodgdon H, Nolan S, Wen M, Costa D, Blain JF, Freeman E, De Strooper B, Vulsteke V, Scrocchi L, Zetterberg H, Portelius E, Hutter-Paier B, Havas D, Ahlijanian M, Flood D, Leventhal L, Shapiro G, Patzke H, Chesworth R, Koenig G. Rogers K, et al. Mol Neurodegener. 2012 Dec 18;7:61. doi: 10.1186/1750-1326-7-61. Mol Neurodegener. 2012. PMID: 23249765 Free PMC article.
DiPOA ([8-(3,3-diphenyl-propyl)-4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]dec-3-yl]-acetic acid), a novel, systemically available, and peripherally restricted mu opioid agonist with antihyperalgesic activity: I. In vitro pharmacological characterization and pharmacokinetic properties.
Valenzano KJ, Miller W, Chen Z, Shan S, Crumley G, Victory SF, Davies E, Huang JC, Allie N, Nolan SJ, Rotshteyn Y, Kyle DJ, Broglé K. Valenzano KJ, et al. Among authors: nolan sj. J Pharmacol Exp Ther. 2004 Aug;310(2):783-92. doi: 10.1124/jpet.103.063313. Epub 2004 Mar 30. J Pharmacol Exp Ther. 2004. PMID: 15054115
69 results