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Page 1
Discovery of the Potent and Selective M1 PAM-Agonist N-[(3R,4S)-3-Hydroxytetrahydro-2H-pyran-4-yl]-5-methyl-4-[4-(1,3-thiazol-4-yl)benzyl]pyridine-2-carboxamide (PF-06767832): Evaluation of Efficacy and Cholinergic Side Effects.
Davoren JE, Lee CW, Garnsey M, Brodney MA, Cordes J, Dlugolenski K, Edgerton JR, Harris AR, Helal CJ, Jenkinson S, Kauffman GW, Kenakin TP, Lazzaro JT, Lotarski SM, Mao Y, Nason DM, Northcott C, Nottebaum L, O'Neil SV, Pettersen B, Popiolek M, Reinhart V, Salomon-Ferrer R, Steyn SJ, Webb D, Zhang L, Grimwood S. Davoren JE, et al. Among authors: o neil sv. J Med Chem. 2016 Jul 14;59(13):6313-28. doi: 10.1021/acs.jmedchem.6b00544. Epub 2016 Jul 1. J Med Chem. 2016. PMID: 27275946
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: o neil sv. 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
Design and Synthesis of γ- and δ-Lactam M1 Positive Allosteric Modulators (PAMs): Convulsion and Cholinergic Toxicity of an M1-Selective PAM with Weak Agonist Activity.
Davoren JE, Garnsey M, Pettersen B, Brodney MA, Edgerton JR, Fortin JP, Grimwood S, Harris AR, Jenkinson S, Kenakin T, Lazzaro JT, Lee CW, Lotarski SM, Nottebaum L, O'Neil SV, Popiolek M, Ramsey S, Steyn SJ, Thorn CA, Zhang L, Webb D. Davoren JE, et al. Among authors: o neil sv. J Med Chem. 2017 Aug 10;60(15):6649-6663. doi: 10.1021/acs.jmedchem.7b00597. Epub 2017 Jul 26. J Med Chem. 2017. PMID: 28598634
Discovery and Characterization of (R)-6-Neopentyl-2-(pyridin-2-ylmethoxy)-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-one (PF-06462894), an Alkyne-Lacking Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Profiled in both Rat and Nonhuman Primates.
Stepan AF, Claffey MM, Reese MR, Balan G, Barreiro G, Barricklow J, Bohanon MJ, Boscoe BP, Cappon GD, Chenard LK, Cianfrogna J, Chen L, Coffman KJ, Drozda SE, Dunetz JR, Ghosh S, Hou X, Houle C, Karki K, Lazzaro JT, Mancuso JY, Marcek JM, Miller EL, Moen MA, O'Neil S, Sakurada I, Skaddan M, Parikh V, Smith DL, Trapa P, Tuttle JB, Verhoest PR, Walker DP, Won A, Wright AS, Whritenour J, Zasadny K, Zaleska MM, Zhang L, Shaffer CL. Stepan AF, et al. J Med Chem. 2017 Sep 28;60(18):7764-7780. doi: 10.1021/acs.jmedchem.7b00604. Epub 2017 Sep 13. J Med Chem. 2017. PMID: 28817277
Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation.
McAllister LA, Butler CR, Mente S, O'Neil SV, Fonseca KR, Piro JR, Cianfrogna JA, Foley TL, Gilbert AM, Harris AR, Helal CJ, Johnson DS, Montgomery JI, Nason DM, Noell S, Pandit J, Rogers BN, Samad TA, Shaffer CL, da Silva RG, Uccello DP, Webb D, Brodney MA. McAllister LA, et al. Among authors: o neil sv. J Med Chem. 2018 Apr 12;61(7):3008-3026. doi: 10.1021/acs.jmedchem.8b00070. Epub 2018 Mar 15. J Med Chem. 2018. PMID: 29498843
Identification and Development of an Irreversible Monoacylglycerol Lipase (MAGL) Positron Emission Tomography (PET) Radioligand with High Specificity.
Zhang L, Butler CR, Maresca KP, Takano A, Nag S, Jia Z, Arakawa R, Piro JR, Samad T, Smith DL, Nason DM, O'Neil S, McAllister L, Schildknegt K, Trapa P, McCarthy TJ, Villalobos A, Halldin C. Zhang L, et al. J Med Chem. 2019 Sep 26;62(18):8532-8543. doi: 10.1021/acs.jmedchem.9b00847. Epub 2019 Sep 16. J Med Chem. 2019. PMID: 31483137
Design of Next-Generation DGAT2 Inhibitor PF-07202954 with Longer Predicted Half-Life.
Filipski KJ, Edmonds DJ, Garnsey MR, Smaltz DJ, Coffman K, Futatsugi K, Lee J, O'Neil SV, Wright A, Nason D, Gosset JR, Orozco CC, Blackler D, Fakhoury G, Gutierrez JA, Perez S, Ross T, Stock I, Tesz G, Dullea R. Filipski KJ, et al. Among authors: o neil sv. ACS Med Chem Lett. 2023 Oct 2;14(10):1427-1433. doi: 10.1021/acsmedchemlett.3c00330. eCollection 2023 Oct 12. ACS Med Chem Lett. 2023. PMID: 37849537 Free PMC article.
24 results