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Page 1
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: reese mr. J Med Chem. 2014 Feb 13;57(3):861-77. doi: 10.1021/jm401622k. Epub 2014 Jan 22. J Med Chem. 2014. PMID: 24392688
C-Aryl glycoside inhibitors of SGLT2: Exploration of sugar modifications including C-5 spirocyclization.
Robinson RP, Mascitti V, Boustany-Kari CM, Carr CL, Foley PM, Kimoto E, Leininger MT, Lowe A, Klenotic MK, Macdonald JI, Maguire RJ, Masterson VM, Maurer TS, Miao Z, Patel JD, Préville C, Reese MR, She L, Steppan CM, Thuma BA, Zhu T. Robinson RP, et al. Among authors: reese mr. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1569-72. doi: 10.1016/j.bmcl.2010.01.075. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20149653
Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia.
Dounay AB, Anderson M, Bechle BM, Campbell BM, Claffey MM, Evdokimov A, Evrard E, Fonseca KR, Gan X, Ghosh S, Hayward MM, Horner W, Kim JY, McAllister LA, Pandit J, Paradis V, Parikh VD, Reese MR, Rong S, Salafia MA, Schuyten K, Strick CA, Tuttle JB, Valentine J, Wang H, Zawadzke LE, Verhoest PR. Dounay AB, et al. Among authors: reese mr. ACS Med Chem Lett. 2012 Jan 25;3(3):187-92. doi: 10.1021/ml200204m. eCollection 2012 Mar 8. ACS Med Chem Lett. 2012. PMID: 24900455 Free PMC article.
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: reese mr. 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: reese mr. 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
5-Aryltetrazoles from Direct C-H Arylation with Aryl Bromides.
Zhang Y, Lee JCH, Reese MR, Boscoe BP, Humphrey JM, Helal CJ. Zhang Y, et al. Among authors: reese mr. J Org Chem. 2020 Apr 17;85(8):5718-5723. doi: 10.1021/acs.joc.0c00085. Epub 2020 Mar 31. J Org Chem. 2020. PMID: 32208719
An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19.
Owen DR, Allerton CMN, Anderson AS, Aschenbrenner L, Avery M, Berritt S, Boras B, Cardin RD, Carlo A, Coffman KJ, Dantonio A, Di L, Eng H, Ferre R, Gajiwala KS, Gibson SA, Greasley SE, Hurst BL, Kadar EP, Kalgutkar AS, Lee JC, Lee J, Liu W, Mason SW, Noell S, Novak JJ, Obach RS, Ogilvie K, Patel NC, Pettersson M, Rai DK, Reese MR, Sammons MF, Sathish JG, Singh RSP, Steppan CM, Stewart AE, Tuttle JB, Updyke L, Verhoest PR, Wei L, Yang Q, Zhu Y. Owen DR, et al. Among authors: reese mr. Science. 2021 Dec 24;374(6575):1586-1593. doi: 10.1126/science.abl4784. Epub 2021 Nov 2. Science. 2021. PMID: 34726479 Free article.
Discovery of the Potent and Selective MC4R Antagonist PF-07258669 for the Potential Treatment of Appetite Loss.
Garnsey MR, Smith AC, Polivkova J, Arons AL, Bai G, Blakemore C, Boehm M, Buzon LM, Campion SN, Cerny M, Chang SC, Coffman K, Farley KA, Fonseca KR, Ford KK, Garren J, Kong JX, Koos MRM, Kung DW, Lian Y, Li MM, Li Q, Martinez-Alsina LA, O'Connor R, Ogilvie K, Omoto K, Raymer B, Reese MR, Ryder T, Samp L, Stevens KA, Widlicka DW, Yang Q, Zhu K, Fortin JP, Sammons MF. Garnsey MR, et al. Among authors: reese mr. J Med Chem. 2023 Mar 9;66(5):3195-3211. doi: 10.1021/acs.jmedchem.2c02012. Epub 2023 Feb 19. J Med Chem. 2023. PMID: 36802610
A Second-Generation Oral SARS-CoV-2 Main Protease Inhibitor Clinical Candidate for the Treatment of COVID-19.
Allerton CMN, Arcari JT, Aschenbrenner LM, Avery M, Bechle BM, Behzadi MA, Boras B, Buzon LM, Cardin RD, Catlin NR, Carlo AA, Coffman KJ, Dantonio A, Di L, Eng H, Farley KA, Ferre RA, Gernhardt SS, Gibson SA, Greasley SE, Greenfield SR, Hurst BL, Kalgutkar AS, Kimoto E, Lanyon LF, Lovett GH, Lian Y, Liu W, Martínez Alsina LA, Noell S, Obach RS, Owen DR, Patel NC, Rai DK, Reese MR, Rothan HA, Sakata S, Sammons MF, Sathish JG, Sharma R, Steppan CM, Tuttle JB, Verhoest PR, Wei L, Yang Q, Yurgelonis I, Zhu Y. Allerton CMN, et al. Among authors: reese mr. J Med Chem. 2024 Aug 22;67(16):13550-13571. doi: 10.1021/acs.jmedchem.3c02469. Epub 2024 Apr 30. J Med Chem. 2024. PMID: 38687966 Free PMC article.
27 results