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Page 1
Discovery of (R)-6-(1-(8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity.
Boezio AA, Copeland KW, Rex K, K Albrecht B, Bauer D, Bellon SF, Boezio C, Broome MA, Choquette D, Coxon A, Dussault I, Hirai S, Lewis R, Lin MH, Lohman J, Liu J, Peterson EA, Potashman M, Shimanovich R, Teffera Y, Whittington DA, Vaida KR, Harmange JC. Boezio AA, et al. Among authors: copeland kw. J Med Chem. 2016 Mar 24;59(6):2328-42. doi: 10.1021/acs.jmedchem.5b01716. Epub 2016 Feb 11. J Med Chem. 2016. PMID: 26812066
Discovery of triazine-benzimidazoles as selective inhibitors of mTOR.
Peterson EA, Andrews PS, Be X, Boezio AA, Bush TL, Cheng AC, Coats JR, Colletti AE, Copeland KW, DuPont M, Graceffa R, Grubinska B, Harmange JC, Kim JL, Mullady EL, Olivieri P, Schenkel LB, Stanton MK, Teffera Y, Whittington DA, Cai T, La DS. Peterson EA, et al. Among authors: copeland kw. Bioorg Med Chem Lett. 2011 Apr 1;21(7):2064-70. doi: 10.1016/j.bmcl.2011.02.007. Epub 2011 Feb 12. Bioorg Med Chem Lett. 2011. PMID: 21376583
Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors.
Peterson EA, Boezio AA, Andrews PS, Boezio CM, Bush TL, Cheng AC, Choquette D, Coats JR, Colletti AE, Copeland KW, DuPont M, Graceffa R, Grubinska B, Kim JL, Lewis RT, Liu J, Mullady EL, Potashman MH, Romero K, Shaffer PL, Stanton MK, Stellwagen JC, Teffera Y, Yi S, Cai T, La DS. Peterson EA, et al. Among authors: copeland kw. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4967-74. doi: 10.1016/j.bmcl.2012.06.033. Epub 2012 Jun 16. Bioorg Med Chem Lett. 2012. PMID: 22765895
Discovery of potent and selective 8-fluorotriazolopyridine c-Met inhibitors.
Peterson EA, Teffera Y, Albrecht BK, Bauer D, Bellon SF, Boezio A, Boezio C, Broome MA, Choquette D, Copeland KW, Dussault I, Lewis R, Lin MH, Lohman J, Liu J, Potashman M, Rex K, Shimanovich R, Whittington DA, Vaida KR, Harmange JC. Peterson EA, et al. Among authors: copeland kw. J Med Chem. 2015 Mar 12;58(5):2417-30. doi: 10.1021/jm501913a. Epub 2015 Mar 3. J Med Chem. 2015. PMID: 25699405
Development of novel azabenzofuran TRPA1 antagonists as in vivo tools.
Copeland KW, Boezio AA, Cheung E, Lee J, Olivieri P, Schenkel LB, Wan Q, Wang W, Wells MC, Youngblood B, Gavva NR, Lehto SG, Geuns-Meyer S. Copeland KW, et al. Bioorg Med Chem Lett. 2014 Aug 1;24(15):3464-8. doi: 10.1016/j.bmcl.2014.05.069. Epub 2014 Jun 6. Bioorg Med Chem Lett. 2014. PMID: 24953819
Correction to Discovery of Potent and Selective 8-Fluorotriazolopyridine c-Met Inhibitors.
Peterson EA, Teffera Y, Albrecht BK, Bauer D, Bellon SF, Boezio A, Boezio C, Broome MA, Choquette D, Copeland KW, Dussault I, Lewis R, Lin MH, Lohman J, Liu J, Potashman M, Rex K, Shimanovich R, Whittington DA, Vaida KR, Harmange JC. Peterson EA, et al. Among authors: copeland kw. J Med Chem. 2015 May 14;58(9):4087. doi: 10.1021/acs.jmedchem.5b00591. Epub 2015 Apr 22. J Med Chem. 2015. PMID: 25901648 No abstract available.
1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of NaV1.7 inhibition.
Boezio AA, Andrews K, Boezio C, Chu-Moyer M, Copeland KW, DiMauro EF, Foti RS, Fremeau RT Jr, Gao H, Geuns-Meyer S, Graceffa RF, Gunaydin H, Huang H, La DS, Ligutti J, Moyer BD, Peterson EA, Yu V, Weiss MM. Boezio AA, et al. Among authors: copeland kw. Bioorg Med Chem Lett. 2018 Jun 15;28(11):2103-2108. doi: 10.1016/j.bmcl.2018.04.035. Epub 2018 Apr 17. Bioorg Med Chem Lett. 2018. PMID: 29709252
Pharmacological effects of nonselective and subtype-selective nicotinic acetylcholine receptor agonists in animal models of persistent pain.
Gao B, Hierl M, Clarkin K, Juan T, Nguyen H, van der Valk M, Deng H, Guo W, Lehto SG, Matson D, McDermott JS, Knop J, Gaida K, Cao L, Waldon D, Albrecht BK, Boezio AA, Copeland KW, Harmange JC, Springer SK, Malmberg AB, McDonough SI. Gao B, et al. Among authors: copeland kw. Pain. 2010 Apr;149(1):33-49. doi: 10.1016/j.pain.2010.01.007. Epub 2010 Feb 18. Pain. 2010. PMID: 20167427