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Page 1
Design and optimization of selective azaindole amide M1 positive allosteric modulators.
Davoren JE, O'Neil SV, Anderson DP, Brodney MA, Chenard L, Dlugolenski K, Edgerton JR, Green M, Garnsey M, Grimwood S, Harris AR, Kauffman GW, LaChapelle E, Lazzaro JT, Lee CW, Lotarski SM, Nason DM, Obach RS, Reinhart V, Salomon-Ferrer R, Steyn SJ, Webb D, Yan J, Zhang L. Davoren JE, et al. Among authors: lachapelle e. Bioorg Med Chem Lett. 2016 Jan 15;26(2):650-655. doi: 10.1016/j.bmcl.2015.11.053. Epub 2015 Nov 17. Bioorg Med Chem Lett. 2016. PMID: 26631313
The Discovery of a Novel Phosphodiesterase (PDE) 4B-Preferring Radioligand for Positron Emission Tomography (PET) Imaging.
Zhang L, Chen L, Beck EM, Chappie TA, Coelho RV, Doran SD, Fan KH, Helal CJ, Humphrey JM, Hughes Z, Kuszpit K, Lachapelle EA, Lazzaro JT, Lee C, Mather RJ, Patel NC, Skaddan MB, Sciabola S, Verhoest PR, Young JM, Zasadny K, Villalobos A. Zhang L, et al. J Med Chem. 2017 Oct 26;60(20):8538-8551. doi: 10.1021/acs.jmedchem.7b01050. Epub 2017 Oct 9. J Med Chem. 2017. PMID: 28957634
Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation.
O'Neill BT, Beck EM, Butler CR, Nolan CE, Gonzales C, Zhang L, Doran SD, Lapham K, Buzon LM, Dutra JK, Barreiro G, Hou X, Martinez-Alsina LA, Rogers BN, Villalobos A, Murray JC, Ogilvie K, LaChapelle EA, Chang C, Lanyon LF, Steppan CM, Robshaw A, Hales K, Boucher GG, Pandher K, Houle C, Ambroise CW, Karanian D, Riddell D, Bales KR, Brodney MA. O'Neill BT, et al. Among authors: lachapelle ea. J Med Chem. 2018 May 24;61(10):4476-4504. doi: 10.1021/acs.jmedchem.8b00246. Epub 2018 Apr 17. J Med Chem. 2018. PMID: 29613789
Design and Synthesis of Clinical Candidate PF-06852231 (CVL-231): A Brain Penetrant, Selective, Positive Allosteric Modulator of the M4 Muscarinic Acetylcholine Receptor.
Butler CR, Popiolek M, McAllister LA, LaChapelle EA, Kramer M, Beck EM, Mente S, Brodney MA, Brown M, Gilbert A, Helal C, Ogilvie K, Starr J, Uccello D, Grimwood S, Edgerton J, Garst-Orozco J, Kozak R, Lotarski S, Rossi A, Smith D, O'Connor R, Lazzaro J, Steppan C, Steyn SJ. Butler CR, et al. Among authors: lachapelle ea. J Med Chem. 2024 Jul 11;67(13):10831-10847. doi: 10.1021/acs.jmedchem.4c00293. Epub 2024 Jun 18. J Med Chem. 2024. PMID: 38888621
Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization.
Davoren JE, Nason D, Coe J, Dlugolenski K, Helal C, Harris AR, LaChapelle E, Liang S, Liu Y, O'Connor R, Orozco CC, Rai BK, Salafia M, Samas B, Xu W, Kozak R, Gray D. Davoren JE, et al. Among authors: lachapelle e. J Med Chem. 2018 Dec 27;61(24):11384-11397. doi: 10.1021/acs.jmedchem.8b01622. Epub 2018 Dec 11. J Med Chem. 2018. PMID: 30431269
Intramolecular Ring-Opening Decomposition of Aryl Azetidines.
Bai G, O'Connell TN, Brodney MA, Butler CR, Czabaniuk LC, Gilbert AM, LaChapelle EA, Li C, McAllister LA, Ogilvie K, Philippe L, Salomon-Ferrer R, Shapiro MJ, Starr JT, Uccello DP, Withka JM, Yan J, Brown MF. Bai G, et al. Among authors: lachapelle ea. ACS Med Chem Lett. 2021 Sep 30;12(10):1585-1588. doi: 10.1021/acsmedchemlett.1c00402. eCollection 2021 Oct 14. ACS Med Chem Lett. 2021. PMID: 34676040 Free PMC article.
26 results