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Page 1
Discovery of Clinical Candidate PF-06648671: A Potent γ-Secretase Modulator for the Treatment of Alzheimer's Disease.
Pettersson M, Johnson DS, Humphrey JM, Am Ende CW, Butler TW, Dorff PH, Efremov IV, Evrard E, Green ME, Helal CJ, Kauffman GW, Mullins PB, Navaratnam T, O'Donnell CJ, O'Sullivan TJ, Patel NC, Stepan AF, Stiff CM, Subramanyam C, Trapa P, Tran TP, Vetelino BC, Yang E, Xie L, Pustilnik LR, Steyn SJ, Wood KM, Bales KR, Hajos-Korcsok E, Verhoest PR. Pettersson M, et al. Among authors: evrard e. J Med Chem. 2024 Jun 27;67(12):10248-10262. doi: 10.1021/acs.jmedchem.4c00580. Epub 2024 Jun 7. J Med Chem. 2024. PMID: 38848667
Discovery of indole-derived pyridopyrazine-1,6-dione γ-secretase modulators that target presenilin.
Pettersson M, Johnson DS, Humphrey JM, Am Ende CW, Evrard E, Efremov I, Kauffman GW, Stepan AF, Stiff CM, Xie L, Bales KR, Hajos-Korcsok E, Murrey HE, Pustilnik LR, Steyn SJ, Wood KM, Verhoest PR. Pettersson M, et al. Among authors: evrard e. Bioorg Med Chem Lett. 2015 Feb 15;25(4):908-13. doi: 10.1016/j.bmcl.2014.12.059. Epub 2014 Dec 25. Bioorg Med Chem Lett. 2015. PMID: 25582600
Discovery of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators with robust central efficacy.
Pettersson M, Johnson DS, Rankic DA, Kauffman GW, Am Ende CW, Butler TW, Boscoe B, Evrard E, Helal CJ, Humphrey JM, Stepan AF, Stiff CM, Yang E, Xie L, Bales KR, Hajos-Korcsok E, Jenkinson S, Pettersen B, Pustilnik LR, Ramirez DS, Steyn SJ, Wood KM, Verhoest PR. Pettersson M, et al. Among authors: evrard e. Medchemcomm. 2016 Nov 2;8(4):730-743. doi: 10.1039/c6md00406g. eCollection 2017 Apr 1. Medchemcomm. 2016. PMID: 30108792 Free PMC article.
PF-04859989 as a template for structure-based drug design: identification of new pyrazole series of irreversible KAT II inhibitors with improved lipophilic efficiency.
Dounay AB, Anderson M, Bechle BM, Evrard E, Gan X, Kim JY, McAllister LA, Pandit J, Rong S, Salafia MA, Tuttle JB, Zawadzke LE, Verhoest PR. Dounay AB, et al. Among authors: evrard e. Bioorg Med Chem Lett. 2013 Apr 1;23(7):1961-6. doi: 10.1016/j.bmcl.2013.02.039. Epub 2013 Feb 15. Bioorg Med Chem Lett. 2013. PMID: 23466229
Photoaffinity Labeling and Quantitative Chemical Proteomics Identify LXRβ as the Functional Target of Enhancers of Astrocytic apoE.
Seneviratne U, Huang Z, Am Ende CW, Butler TW, Cleary L, Dresselhaus E, Evrard E, Fisher EL, Green ME, Helal CJ, Humphrey JM, Lanyon LF, Marconi M, Mukherjee P, Sciabola S, Steppan CM, Sylvain EK, Tuttle JB, Verhoest PR, Wager TT, Xie L, Ramaswamy G, Johnson DS, Pettersson M. Seneviratne U, et al. Among authors: evrard e. Cell Chem Biol. 2021 Feb 18;28(2):148-157.e7. doi: 10.1016/j.chembiol.2020.09.002. Epub 2020 Sep 29. Cell Chem Biol. 2021. PMID: 32997975 Free article.
Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo efficacy in cognition models.
O'Donnell CJ, Rogers BN, Bronk BS, Bryce DK, Coe JW, Cook KK, Duplantier AJ, Evrard E, Hajós M, Hoffmann WE, Hurst RS, Maklad N, Mather RJ, McLean S, Nedza FM, O'Neill BT, Peng L, Qian W, Rottas MM, Sands SB, Schmidt AW, Shrikhande AV, Spracklin DK, Wong DF, Zhang A, Zhang L. O'Donnell CJ, et al. Among authors: evrard e. J Med Chem. 2010 Feb 11;53(3):1222-37. doi: 10.1021/jm9015075. J Med Chem. 2010. PMID: 20043678
Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia.
Dounay AB, Anderson M, Bechle BM, Campbell BM, Claffey MM, Evdokimov A, Evrard E, Fonseca KR, Gan X, Ghosh S, Hayward MM, Horner W, Kim JY, McAllister LA, Pandit J, Paradis V, Parikh VD, Reese MR, Rong S, Salafia MA, Schuyten K, Strick CA, Tuttle JB, Valentine J, Wang H, Zawadzke LE, Verhoest PR. Dounay AB, et al. Among authors: evrard e. ACS Med Chem Lett. 2012 Jan 25;3(3):187-92. doi: 10.1021/ml200204m. eCollection 2012 Mar 8. ACS Med Chem Lett. 2012. PMID: 24900455 Free PMC article.
Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions.
Tuttle JB, Anderson M, Bechle BM, Campbell BM, Chang C, Dounay AB, Evrard E, Fonseca KR, Gan X, Ghosh S, Horner W, James LC, Kim JY, McAllister LA, Pandit J, Parikh VD, Rago BJ, Salafia MA, Strick CA, Zawadzke LE, Verhoest PR. Tuttle JB, et al. Among authors: evrard e. ACS Med Chem Lett. 2012 Oct 24;4(1):37-40. doi: 10.1021/ml300237v. eCollection 2013 Jan 10. ACS Med Chem Lett. 2012. PMID: 24900560 Free PMC article.
128 results