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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: wright as. 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 of a novel Kv7 channel opener as a treatment for epilepsy.
Davoren JE, Claffey MM, Snow SL, Reese MR, Arora G, Butler CR, Boscoe BP, Chenard L, DeNinno SL, Drozda SE, Duplantier AJ, Moine L, Rogers BN, Rong S, Schuyten K, Wright AS, Zhang L, Serpa KA, Weber ML, Stolyar P, Whisman TL, Baker K, Tse K, Clark AJ, Rong H, Mather RJ, Lowe JA 3rd. Davoren JE, et al. Among authors: wright as. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4941-4944. doi: 10.1016/j.bmcl.2015.04.074. Epub 2015 May 1. Bioorg Med Chem Lett. 2015. PMID: 25987375
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: wright as. 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
Late-Stage Microsomal Oxidation Reduces Drug-Drug Interaction and Identifies Phosphodiesterase 2A Inhibitor PF-06815189.
Stepan AF, Tran TP, Helal CJ, Brown MS, Chang C, O'Connor RE, De Vivo M, Doran SD, Fisher EL, Jenkinson S, Karanian D, Kormos BL, Sharma R, Walker GS, Wright AS, Yang EX, Brodney MA, Wager TT, Verhoest PR, Obach RS. Stepan AF, et al. Among authors: wright as. ACS Med Chem Lett. 2018 Jan 4;9(2):68-72. doi: 10.1021/acsmedchemlett.7b00343. eCollection 2018 Feb 8. ACS Med Chem Lett. 2018. PMID: 29456790 Free PMC article.
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. 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.
Discovery and biological characterization of capromorelin analogues with extended half-lives.
Carpino PA, Lefker BA, Toler SM, Pan LC, Hadcock JR, Murray MC, Cook ER, DiBrino JN, DeNinno SL, Chidsey-Frink KL, Hada WA, Inthavongsay J, Lewis SK, Mangano FM, Mullins MA, Nickerson DF, Ng O, Pirie CM, Ragan JA, Rose CR, Tess DA, Wright AS, Yu L, Zawistoski MP, Pettersen JC, DaSilva-Jardine PA, Wilson TC, Thompson DD. Carpino PA, et al. Among authors: wright as. Bioorg Med Chem Lett. 2002 Nov 18;12(22):3279-82. doi: 10.1016/s0960-894x(02)00734-5. Bioorg Med Chem Lett. 2002. PMID: 12392732
Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin.
Carpino PA, Lefker BA, Toler SM, Pan LC, Hadcock JR, Cook ER, DiBrino JN, Campeta AM, DeNinno SL, Chidsey-Frink KL, Hada WA, Inthavongsay J, Mangano FM, Mullins MA, Nickerson DF, Ng O, Pirie CM, Ragan JA, Rose CR, Tess DA, Wright AS, Yu L, Zawistoski MP, DaSilva-Jardine PA, Wilson TC, Thompson DD. Carpino PA, et al. Among authors: wright as. Bioorg Med Chem. 2003 Feb 20;11(4):581-90. doi: 10.1016/s0968-0896(02)00433-9. Bioorg Med Chem. 2003. PMID: 12538023
Design and application of synthetic 17B-HSD13 substrates reveals preserved catalytic activity of protective human variants.
Garnsey MR, Wang Y, Edmonds DJ, Sammons MF, Reidich B, Ahn Y, Ashkenazi Y, Carlo A, Cerny MA, Coffman KJ, Culver JA, Dechert Schmitt AM, Eng H, Fisher EL, Gutierrez JA, James L, Jordan S, Kohrt JT, Kramer M, LaChapelle EA, Lee JC, Lee J, Li D, Li Z, Liu S, Liu J, Magee TV, Miller MR, Moran M, Nason DM, Nedoma NL, O'Neil SV, Piotrowski MA, Racich J, Sommese RF, Stevens LM, Wright AS, Xiao J, Zhang L, Zhou D, Barrandon O, Clasquin MF. Garnsey MR, et al. Among authors: wright as. Nat Commun. 2025 Jan 2;16(1):297. doi: 10.1038/s41467-024-54487-5. Nat Commun. 2025. PMID: 39746932 Free PMC article.
136 results