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104 results

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Page 1
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: shaffer cl. 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
Discovery and characterization of a novel dihydroisoxazole class of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor potentiators.
Patel NC, Schwarz J, Hou XJ, Hoover DJ, Xie L, Fliri AJ, Gallaschun RJ, Lazzaro JT, Bryce DK, Hoffmann WE, Hanks AN, McGinnis D, Marr ES, Gazard JL, Hajós M, Scialis RJ, Hurst RS, Shaffer CL, Pandit J, O'Donnell CJ. Patel NC, et al. Among authors: shaffer cl. J Med Chem. 2013 Nov 27;56(22):9180-91. doi: 10.1021/jm401274b. Epub 2013 Nov 11. J Med Chem. 2013. PMID: 24215237
Discovery and preclinical characterization of 1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): a highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator.
Zhang L, Balan G, Barreiro G, Boscoe BP, Chenard LK, Cianfrogna J, Claffey MM, Chen L, Coffman KJ, Drozda SE, Dunetz JR, Fonseca KR, Galatsis P, Grimwood S, Lazzaro JT, Mancuso JY, Miller EL, Reese MR, Rogers BN, Sakurada I, Skaddan M, Smith DL, Stepan AF, Trapa P, Tuttle JB, Verhoest PR, Walker DP, Wright AS, Zaleska MM, Zasadny K, Shaffer CL. Zhang L, et al. Among authors: shaffer cl. J Med Chem. 2014 Feb 13;57(3):861-77. doi: 10.1021/jm401622k. Epub 2014 Jan 22. J Med Chem. 2014. PMID: 24392688
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. Among authors: shaffer cl. 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
A novel series of [3.2.1] azabicyclic biaryl ethers as alpha3beta4 and alpha6/4beta4 nicotinic receptor agonists.
Lowe JA 3rd, DeNinno SL, Coe JW, Zhang L, Mente S, Hurst RS, Mather RJ, Ward KM, Shrikhande A, Rollema H, Johnson DE, Horner W, Gorczyca R, Tingley FD 3rd, Kozak R, Majchrzak MJ, Tritto T, Sadlier J, Shaffer CL, Ellerbrock B, Osgood SM, MacDougall MC, McDowell LL. Lowe JA 3rd, et al. Among authors: shaffer cl. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4749-52. doi: 10.1016/j.bmcl.2010.06.142. Bioorg Med Chem Lett. 2010. PMID: 20663668
The discovery and characterization of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor potentiator N-{(3S,4S)-4-[4-(5-cyano-2-thienyl)phenoxy]tetrahydrofuran-3-yl}propane-2-sulfonamide (PF-04958242).
Shaffer CL, Patel NC, Schwarz J, Scialis RJ, Wei Y, Hou XJ, Xie L, Karki K, Bryce DK, Osgood SM, Hoffmann WE, Lazzaro JT, Chang C, McGinnis DF, Lotarski SM, Liu J, Obach RS, Weber ML, Chen L, Zasadny KR, Seymour PA, Schmidt CJ, Hajós M, Hurst RS, Pandit J, O'Donnell CJ. Shaffer CL, et al. J Med Chem. 2015 May 28;58(10):4291-308. doi: 10.1021/acs.jmedchem.5b00300. Epub 2015 May 14. J Med Chem. 2015. PMID: 25905800
Unbound Brain-to-Plasma Partition Coefficient, Kp,uu,brain-a Game Changing Parameter for CNS Drug Discovery and Development.
Loryan I, Reichel A, Feng B, Bundgaard C, Shaffer C, Kalvass C, Bednarczyk D, Morrison D, Lesuisse D, Hoppe E, Terstappen GC, Fischer H, Di L, Colclough N, Summerfield S, Buckley ST, Maurer TS, Fridén M. Loryan I, et al. Pharm Res. 2022 Jul;39(7):1321-1341. doi: 10.1007/s11095-022-03246-6. Epub 2022 Apr 11. Pharm Res. 2022. PMID: 35411506 Free PMC article.
104 results