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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: chung s. 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
Aminocarbonylation of aryl tosylates to carboxamides.
Chung S, Sach N, Choi C, Yang X, Drozda SE, Singer RA, Wright SW. Chung S, et al. Org Lett. 2015 Jun 5;17(11):2848-51. doi: 10.1021/acs.orglett.5b01283. Epub 2015 May 21. Org Lett. 2015. PMID: 25994500
Potent inhibitors of LpxC for the treatment of Gram-negative infections.
Brown MF, Reilly U, Abramite JA, Arcari JT, Oliver R, Barham RA, Che Y, Chen JM, Collantes EM, Chung SW, Desbonnet C, Doty J, Doroski M, Engtrakul JJ, Harris TM, Huband M, Knafels JD, Leach KL, Liu S, Marfat A, Marra A, McElroy E, Melnick M, Menard CA, Montgomery JI, Mullins L, Noe MC, O'Donnell J, Penzien J, Plummer MS, Price LM, Shanmugasundaram V, Thoma C, Uccello DP, Warmus JS, Wishka DG. Brown MF, et al. Among authors: chung sw. J Med Chem. 2012 Jan 26;55(2):914-23. doi: 10.1021/jm2014748. Epub 2012 Jan 11. J Med Chem. 2012. PMID: 22175825
Pyridone methylsulfone hydroxamate LpxC inhibitors for the treatment of serious gram-negative infections.
Montgomery JI, Brown MF, Reilly U, Price LM, Abramite JA, Arcari J, Barham R, Che Y, Chen JM, Chung SW, Collantes EM, Desbonnet C, Doroski M, Doty J, Engtrakul JJ, Harris TM, Huband M, Knafels JD, Leach KL, Liu S, Marfat A, McAllister L, McElroy E, Menard CA, Mitton-Fry M, Mullins L, Noe MC, O'Donnell J, Oliver R, Penzien J, Plummer M, Shanmugasundaram V, Thoma C, Tomaras AP, Uccello DP, Vaz A, Wishka DG. Montgomery JI, et al. Among authors: chung sw. J Med Chem. 2012 Feb 23;55(4):1662-70. doi: 10.1021/jm2014875. Epub 2012 Feb 8. J Med Chem. 2012. PMID: 22257165
Heterocyclic methylsulfone hydroxamic acid LpxC inhibitors as Gram-negative antibacterial agents.
McAllister LA, Montgomery JI, Abramite JA, Reilly U, Brown MF, Chen JM, Barham RA, Che Y, Chung SW, Menard CA, Mitton-Fry M, Mullins LM, Noe MC, O'Donnell JP, Oliver RM 3rd, Penzien JB, Plummer M, Price LM, Shanmugasundaram V, Tomaras AP, Uccello DP. McAllister LA, et al. Bioorg Med Chem Lett. 2012 Nov 15;22(22):6832-8. doi: 10.1016/j.bmcl.2012.09.058. Epub 2012 Sep 24. Bioorg Med Chem Lett. 2012. PMID: 23046961
9,909 results