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Page 1
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: burnett da. 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 and synthesis of tricyclic sulfones as gamma-secretase inhibitors with greatly reduced Notch toxicity.
Xu R, Cole D, Asberom T, Bara T, Bennett C, Burnett DA, Clader J, Domalski M, Greenlee W, Hyde L, Josien H, Li H, McBriar M, McKittrick B, McPhail AT, Pissarnitski D, Qiang L, Rajagopalan M, Sasikumar T, Su J, Tang H, Wu WL, Zhang L, Zhao Z. Xu R, et al. Among authors: burnett da. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2591-6. doi: 10.1016/j.bmcl.2010.02.080. Epub 2010 Feb 23. Bioorg Med Chem Lett. 2010. PMID: 20236824
Iminoheterocycles as gamma-secretase modulators.
Caldwell JP, Bennett CE, McCracken TM, Mazzola RD, Bara T, Buevich A, Burnett DA, Chu I, Cohen-Williams M, Josein H, Hyde L, Lee J, McKittrick B, Song L, Terracina G, Voigt J, Zhang L, Zhu Z. Caldwell JP, et al. Among authors: burnett da. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5380-4. doi: 10.1016/j.bmcl.2010.07.121. Epub 2010 Aug 1. Bioorg Med Chem Lett. 2010. PMID: 20724152
Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious γ-secretase modulators in vivo.
Sun ZY, Asberom T, Bara T, Bennett C, Burnett D, Chu I, Clader J, Cohen-Williams M, Cole D, Czarniecki M, Durkin J, Gallo G, Greenlee W, Josien H, Huang X, Hyde L, Jones N, Kazakevich I, Li H, Liu X, Lee J, Maccoss M, Mandal MB, McCracken T, Nomeir A, Mazzola R, Palani A, Parker EM, Pissarnitski DA, Qin J, Song L, Terracina G, Vicarel M, Voigt J, Xu R, Zhang L, Zhang Q, Zhao Z, Zhu X, Zhu Z. Sun ZY, et al. Among authors: burnett d. J Med Chem. 2012 Jan 12;55(1):489-502. doi: 10.1021/jm201407j. Epub 2011 Dec 8. J Med Chem. 2012. PMID: 22098494
Discovery of SCH 900229, a Potent Presenilin 1 Selective γ-Secretase Inhibitor for the Treatment of Alzheimer's Disease.
Wu WL, Domalski M, Burnett DA, Josien H, Bara T, Rajagopalan M, Xu R, Clader J, Greenlee WJ, Brunskill A, Hyde LA, Del Vecchio RA, Cohen-Williams ME, Song L, Lee J, Terracina G, Zhang Q, Nomeir A, Parker EM, Zhang L. Wu WL, et al. Among authors: burnett da. ACS Med Chem Lett. 2012 Apr 9;3(11):892-6. doi: 10.1021/ml300044f. eCollection 2012 Nov 8. ACS Med Chem Lett. 2012. PMID: 24900404 Free PMC article.
Synthesis and SAR Studies of Fused Oxadiazines as γ-Secretase Modulators for Treatment of Alzheimer's Disease.
Huang X, Zhou W, Liu X, Li H, Sun G, Mandal M, Vicarel M, Zhu X, Bennett C, McCraken T, Pissarnitski D, Zhao Z, Cole D, Gallo G, Zhu Z, Palani A, Aslanian R, Clader J, Czarniecki M, Greenlee W, Burnett D, Cohen-Williams M, Hyde L, Song L, Zhang L, Chu I, Buevich A. Huang X, et al. ACS Med Chem Lett. 2012 Sep 4;3(11):931-5. doi: 10.1021/ml300209g. eCollection 2012 Nov 8. ACS Med Chem Lett. 2012. PMID: 24900409 Free PMC article.
Discovery of a Novel, Potent Spirocyclic Series of γ-Secretase Inhibitors.
Zhao Z, Pissarnitski DA, Josien HB, Wu WL, Xu R, Li H, Clader JW, Burnett DA, Terracina G, Hyde L, Lee J, Song L, Zhang L, Parker EM. Zhao Z, et al. Among authors: burnett da. J Med Chem. 2015 Nov 25;58(22):8806-17. doi: 10.1021/acs.jmedchem.5b00774. Epub 2015 Nov 6. J Med Chem. 2015. PMID: 26496070
100 results