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Page 1
Identification and Preclinical Evaluation of the Bicyclic Pyrimidine γ-Secretase Modulator BMS-932481.
Boy KM, Guernon JM, Zuev DS, Xu L, Zhang Y, Shi J, Marcin LR, Higgins MA, Wu YJ, Krishnananthan S, Li J, Trehan A, Smith D, Toyn JH, Meredith JE, Burton CR, Kimura SR, Zvyaga T, Zhuo X, Lentz KA, Grace JE, Denton R, Morrison JS, Mathur A, Albright CF, Ahlijanian MK, Olson RE, Thompson LA, Macor JE. Boy KM, et al. Among authors: meredith je. ACS Med Chem Lett. 2019 Feb 17;10(3):312-317. doi: 10.1021/acsmedchemlett.8b00541. eCollection 2019 Mar 14. ACS Med Chem Lett. 2019. PMID: 30891132 Free PMC article.
Monosubstituted γ-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of β-secretase (BACE).
Boy KM, Guernon JM, Shi J, Toyn JH, Meredith JE, Barten DM, Burton CR, Albright CF, Marcinkeviciene J, Good AC, Tebben AJ, Muckelbauer JK, Camac DM, Lentz KA, Bronson JJ, Olson RE, Macor JE, Thompson LA 3rd. Boy KM, et al. Among authors: meredith je. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6916-24. doi: 10.1016/j.bmcl.2011.06.109. Epub 2011 Jun 30. Bioorg Med Chem Lett. 2011. PMID: 21782431
Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors.
Thompson LA, Shi J, Decicco CP, Tebben AJ, Olson RE, Boy KM, Guernon JM, Good AC, Liauw A, Zheng C, Copeland RA, Combs AP, Trainor GL, Camac DM, Muckelbauer JK, Lentz KA, Grace JE, Burton CR, Toyn JH, Barten DM, Marcinkeviciene J, Meredith JE, Albright CF, Macor JE. Thompson LA, et al. Among authors: meredith je. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6909-15. doi: 10.1016/j.bmcl.2011.06.116. Epub 2011 Jul 2. Bioorg Med Chem Lett. 2011. PMID: 21974952
Acyl guanidine inhibitors of β-secretase (BACE-1): optimization of a micromolar hit to a nanomolar lead via iterative solid- and solution-phase library synthesis.
Gerritz SW, Zhai W, Shi S, Zhu S, Toyn JH, Meredith JE Jr, Iben LG, Burton CR, Albright CF, Good AC, Tebben AJ, Muckelbauer JK, Camac DM, Metzler W, Cook LS, Padmanabha R, Lentz KA, Sofia MJ, Poss MA, Macor JE, Thompson LA 3rd. Gerritz SW, et al. Among authors: meredith je jr. J Med Chem. 2012 Nov 8;55(21):9208-23. doi: 10.1021/jm300931y. Epub 2012 Oct 2. J Med Chem. 2012. PMID: 23030502
Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor.
Gillman KW, Starrett JE Jr, Parker MF, Xie K, Bronson JJ, Marcin LR, McElhone KE, Bergstrom CP, Mate RA, Williams R, Meredith JE Jr, Burton CR, Barten DM, Toyn JH, Roberts SB, Lentz KA, Houston JG, Zaczek R, Albright CF, Decicco CP, Macor JE, Olson RE. Gillman KW, et al. Among authors: meredith je jr. ACS Med Chem Lett. 2010 Mar 22;1(3):120-4. doi: 10.1021/ml1000239. eCollection 2010 Jun 10. ACS Med Chem Lett. 2010. PMID: 24900185 Free PMC article.
Identification and Preclinical Pharmacology of the γ-Secretase Modulator BMS-869780.
Toyn JH, Thompson LA, Lentz KA, Meredith JE Jr, Burton CR, Sankaranararyanan S, Guss V, Hall T, Iben LG, Krause CM, Krause R, Lin XA, Pierdomenico M, Polson C, Robertson AS, Denton RR, Grace JE, Morrison J, Raybon J, Zhuo X, Snow K, Padmanabha R, Agler M, Esposito K, Harden D, Prack M, Varma S, Wong V, Zhu Y, Zvyaga T, Gerritz S, Marcin LR, Higgins MA, Shi J, Wei C, Cantone JL, Drexler DM, Macor JE, Olson RE, Ahlijanian MK, Albright CF. Toyn JH, et al. Among authors: meredith je jr. Int J Alzheimers Dis. 2014;2014:431858. doi: 10.1155/2014/431858. Epub 2014 Jul 8. Int J Alzheimers Dis. 2014. PMID: 25097793 Free PMC article.
Macrocyclic prolinyl acyl guanidines as inhibitors of β-secretase (BACE).
Boy KM, Guernon JM, Wu YJ, Zhang Y, Shi J, Zhai W, Zhu S, Gerritz SW, Toyn JH, Meredith JE, Barten DM, Burton CR, Albright CF, Good AC, Grace JE, Lentz KA, Olson RE, Macor JE, Thompson LA 3rd. Boy KM, et al. Among authors: meredith je. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5040-7. doi: 10.1016/j.bmcl.2015.10.031. Epub 2015 Oct 20. Bioorg Med Chem Lett. 2015. PMID: 26497283
Robust Translation of γ-Secretase Modulator Pharmacology across Preclinical Species and Human Subjects.
Toyn JH, Boy KM, Raybon J, Meredith JE Jr, Robertson AS, Guss V, Hoque N, Sweeney F, Zhuo X, Clarke W, Snow K, Denton RR, Zuev D, Thompson LA, Morrison J, Grace J, Berisha F, Furlong M, Wang JS, Lentz KA, Padmanabha R, Cook L, Wei C, Drexler DM, Macor JE, Albright CF, Gasior M, Olson RE, Hong Q, Soares HD, AbuTarif M, Ahlijanian MK. Toyn JH, et al. Among authors: meredith je jr. J Pharmacol Exp Ther. 2016 Jul;358(1):125-37. doi: 10.1124/jpet.116.232249. Epub 2016 Apr 20. J Pharmacol Exp Ther. 2016. PMID: 27189974 Free PMC article.
Discovery of Clinical Candidate BMS-906024: A Potent Pan-Notch Inhibitor for the Treatment of Leukemia and Solid Tumors.
Gavai AV, Quesnelle C, Norris D, Han WC, Gill P, Shan W, Balog A, Chen K, Tebben A, Rampulla R, Wu DR, Zhang Y, Mathur A, White R, Rose A, Wang H, Yang Z, Ranasinghe A, D'Arienzo C, Guarino V, Xiao L, Su C, Everlof G, Arora V, Shen DR, Cvijic ME, Menard K, Wen ML, Meredith J, Trainor G, Lombardo LJ, Olson R, Baran PS, Hunt JT, Vite GD, Fischer BS, Westhouse RA, Lee FY. Gavai AV, et al. ACS Med Chem Lett. 2015 Mar 11;6(5):523-7. doi: 10.1021/acsmedchemlett.5b00001. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005526 Free PMC article.
Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors.
Thompson LA, Liauw AY, Ramanjulu MM, Kasireddy-Polam P, Mercer SE, Maduskuie TP, Glicksman M, Roach AH, Meredith JE, Liu RQ, Combs AP, Higaki JN, Cordell B, Seiffert D, Zaczek RC, Robertson DW, Olson RE. Thompson LA, et al. Among authors: meredith je. Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63. doi: 10.1016/j.bmcl.2006.01.055. Epub 2006 Feb 10. Bioorg Med Chem Lett. 2006. PMID: 16473009
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