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Page 1
Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation.
Harmange JC, Weiss MM, Germain J, Polverino AJ, Borg G, Bready J, Chen D, Choquette D, Coxon A, DeMelfi T, DiPietro L, Doerr N, Estrada J, Flynn J, Graceffa RF, Harriman SP, Kaufman S, La DS, Long A, Martin MW, Neervannan S, Patel VF, Potashman M, Regal K, Roveto PM, Schrag ML, Starnes C, Tasker A, Teffera Y, Wang L, White RD, Whittington DA, Zanon R. Harmange JC, et al. Among authors: regal k. J Med Chem. 2008 Mar 27;51(6):1649-67. doi: 10.1021/jm701097z. Epub 2008 Mar 7. J Med Chem. 2008. PMID: 18324761
Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors.
Weiss MM, Harmange JC, Polverino AJ, Bauer D, Berry L, Berry V, Borg G, Bready J, Chen D, Choquette D, Coxon A, DeMelfi T, Doerr N, Estrada J, Flynn J, Graceffa RF, Harriman SP, Kaufman S, La DS, Long A, Neervannan S, Patel VF, Potashman M, Regal K, Roveto PM, Schrag ML, Starnes C, Tasker A, Teffera Y, Whittington DA, Zanon R. Weiss MM, et al. Among authors: regal k. J Med Chem. 2008 Mar 27;51(6):1668-80. doi: 10.1021/jm701098w. Epub 2008 Mar 7. J Med Chem. 2008. PMID: 18324759
The discovery of an orally efficacious positive allosteric modulator of the calcium sensing receptor containing a dibenzylamine core.
Harrington PE, St Jean DJ Jr, Clarine J, Coulter TS, Croghan M, Davenport A, Davis J, Ghiron C, Hutchinson J, Kelly MG, Lott F, Lu JY, Martin D, Morony S, Poon SF, Portero-Larragueta E, Reagan JD, Regal KA, Tasker A, Wang M, Yang Y, Yao G, Zeng Q, Henley C 3rd, Fotsch C. Harrington PE, et al. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5544-7. doi: 10.1016/j.bmcl.2010.07.060. Epub 2010 Aug 12. Bioorg Med Chem Lett. 2010. PMID: 20708930
Potent hFPRL1 (ALXR) agonists as potential anti-inflammatory agents.
Bürli RW, Xu H, Zou X, Muller K, Golden J, Frohn M, Adlam M, Plant MH, Wong M, McElvain M, Regal K, Viswanadhan VN, Tagari P, Hungate R. Bürli RW, et al. Among authors: regal k. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3713-8. doi: 10.1016/j.bmcl.2006.04.068. Epub 2006 May 11. Bioorg Med Chem Lett. 2006. PMID: 16697190
Discovery of 7-tetrahydropyran-2-yl chromans: β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloid β-protein (Aβ) in the central nervous system.
Thomas AA, Hunt KW, Volgraf M, Watts RJ, Liu X, Vigers G, Smith D, Sammond D, Tang TP, Rhodes SP, Metcalf AT, Brown KD, Otten JN, Burkard M, Cox AA, Do MK, Dutcher D, Rana S, DeLisle RK, Regal K, Wright AD, Groneberg R, Scearce-Levie K, Siu M, Purkey HE, Lyssikatos JP, Gunawardana IW. Thomas AA, et al. Among authors: regal k. J Med Chem. 2014 Feb 13;57(3):878-902. doi: 10.1021/jm401635n. Epub 2014 Jan 22. J Med Chem. 2014. PMID: 24397738
Spirocyclic β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloid β in a higher species.
Hunt KW, Cook AW, Watts RJ, Clark CT, Vigers G, Smith D, Metcalf AT, Gunawardana IW, Burkard M, Cox AA, Geck Do MK, Dutcher D, Thomas AA, Rana S, Kallan NC, DeLisle RK, Rizzi JP, Regal K, Sammond D, Groneberg R, Siu M, Purkey H, Lyssikatos JP, Marlow A, Liu X, Tang TP. Hunt KW, et al. Among authors: regal k. J Med Chem. 2013 Apr 25;56(8):3379-403. doi: 10.1021/jm4002154. Epub 2013 Apr 16. J Med Chem. 2013. PMID: 23537249
8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors.
Thomas AA, Hunt KW, Newhouse B, Watts RJ, Liu X, Vigers G, Smith D, Rhodes SP, Brown KD, Otten JN, Burkard M, Cox AA, Geck Do MK, Dutcher D, Rana S, DeLisle RK, Regal K, Wright AD, Groneberg R, Liao J, Scearce-Levie K, Siu M, Purkey HE, Lyssikatos JP. Thomas AA, et al. Among authors: regal k. J Med Chem. 2014 Dec 11;57(23):10112-29. doi: 10.1021/jm5015132. Epub 2014 Nov 26. J Med Chem. 2014. PMID: 25411915
Mechanistic pharmacokinetic-pharmacodynamic modeling of BACE1 inhibition in monkeys: development of a predictive model for amyloid precursor protein processing.
Liu X, Wong H, Scearce-Levie K, Watts RJ, Coraggio M, Shin YG, Peng K, Wildsmith KR, Atwal JK, Mango J, Schauer SP, Regal K, Hunt KW, Thomas AA, Siu M, Lyssikatos J, Deshmukh G, Hop CE. Liu X, et al. Among authors: regal k. Drug Metab Dispos. 2013 Jul;41(7):1319-28. doi: 10.1124/dmd.112.050864. Epub 2013 Apr 12. Drug Metab Dispos. 2013. PMID: 23584887
24 results