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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: trapa p. 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 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: trapa p. 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: trapa p. 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 a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging.
Liang SH, Chen JM, Normandin MD, Chang JS, Chang GC, Taylor CK, Trapa P, Plummer MS, Para KS, Conn EL, Lopresti-Morrow L, Lanyon LF, Cook JM, Richter KE, Nolan CE, Schachter JB, Janat F, Che Y, Shanmugasundaram V, Lefker BA, Enerson BE, Livni E, Wang L, Guehl NJ, Patnaik D, Wagner FF, Perlis R, Holson EB, Haggarty SJ, El Fakhri G, Kurumbail RG, Vasdev N. Liang SH, et al. Among authors: trapa p. Angew Chem Int Ed Engl. 2016 Aug 8;55(33):9601-5. doi: 10.1002/anie.201603797. Epub 2016 Jun 29. Angew Chem Int Ed Engl. 2016. PMID: 27355874 Free PMC article.
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. Among authors: trapa p. 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
Target occupancy study and whole-body dosimetry with a MAGL PET ligand [11C]PF-06809247 in non-human primates.
Arakawa R, Takano A, Nag S, Jia Z, Amini N, Maresca KP, Zhang L, Keliher EJ, Butler CR, Piro JR, Samad TA, Smith D, Nason D, O'Neil S, Trapa P, Fonseca KR, Litchfield J, McCarthy T, Carson RE, Halldin C. Arakawa R, et al. Among authors: trapa p. EJNMMI Res. 2022 Mar 4;12(1):13. doi: 10.1186/s13550-022-00882-2. EJNMMI Res. 2022. PMID: 35244788 Free PMC article.
27 results