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Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.
Lee KL, Ambler CM, Anderson DR, Boscoe BP, Bree AG, Brodfuehrer JI, Chang JS, Choi C, Chung S, Curran KJ, Day JE, Dehnhardt CM, Dower K, Drozda SE, Frisbie RK, Gavrin LK, Goldberg JA, Han S, Hegen M, Hepworth D, Hope HR, Kamtekar S, Kilty IC, Lee A, Lin LL, Lovering FE, Lowe MD, Mathias JP, Morgan HM, Murphy EA, Papaioannou N, Patny A, Pierce BS, Rao VR, Saiah E, Samardjiev IJ, Samas BM, Shen MWH, Shin JH, Soutter HH, Strohbach JW, Symanowicz PT, Thomason JR, Trzupek JD, Vargas R, Vincent F, Yan J, Zapf CW, Wright SW. Lee KL, et al. Among authors: drozda se. J Med Chem. 2017 Jul 13;60(13):5521-5542. doi: 10.1021/acs.jmedchem.7b00231. Epub 2017 Jun 14. J Med Chem. 2017. PMID: 28498658
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: drozda se. 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: drozda se. 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: drozda se. 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
Aminocarbonylation of aryl tosylates to carboxamides.
Chung S, Sach N, Choi C, Yang X, Drozda SE, Singer RA, Wright SW. Chung S, et al. Among authors: drozda se. Org Lett. 2015 Jun 5;17(11):2848-51. doi: 10.1021/acs.orglett.5b01283. Epub 2015 May 21. Org Lett. 2015. PMID: 25994500
Aza-tricyclic substance P antagonists.
Lowe JA 3rd, Drozda SE, McLean S, Bryce DK, Crawford RT, Snider RM, Longo KP, Nagahisa A, Tsuchiya M. Lowe JA 3rd, et al. Among authors: drozda se. J Med Chem. 1994 Sep 2;37(18):2831-40. doi: 10.1021/jm00044a002. J Med Chem. 1994. PMID: 7520943
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