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Development of CXCR3 antagonists. Part 4: discovery of 2-amino-(4-tropinyl)quinolines.
Knight RL, Allen DR, Birch HL, Chapman GA, Galvin FC, Jopling LA, Lock CJ, Meissner JW, Owen DA, Raphy G, Watson RJ, Williams SC. Knight RL, et al. Among authors: watson rj. Bioorg Med Chem Lett. 2008 Jan 15;18(2):629-33. doi: 10.1016/j.bmcl.2007.11.075. Epub 2007 Nov 28. Bioorg Med Chem Lett. 2008. PMID: 18068363
Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.
Demont EH, Arpino S, Bit RA, Campbell CA, Deeks N, Desai S, Dowell SJ, Gaskin P, Gray JR, Harrison LA, Haynes A, Heightman TD, Holmes DS, Humphreys PG, Kumar U, Morse MA, Osborne GJ, Panchal T, Philpott KL, Taylor S, Watson R, Willis R, Witherington J. Demont EH, et al. J Med Chem. 2011 Oct 13;54(19):6724-33. doi: 10.1021/jm200609t. Epub 2011 Sep 9. J Med Chem. 2011. PMID: 21838322
Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.
Liddle J, Atkinson FL, Barker MD, Carter PS, Curtis NR, Davis RP, Douault C, Dickson MC, Elwes D, Garton NS, Gray M, Hayhow TG, Hobbs CI, Jones E, Leach S, Leavens K, Lewis HD, McCleary S, Neu M, Patel VK, Preston AG, Ramirez-Molina C, Shipley TJ, Skone PA, Smithers N, Somers DO, Walker AL, Watson RJ, Weingarten GG. Liddle J, et al. Among authors: watson rj. Bioorg Med Chem Lett. 2011 Oct 15;21(20):6188-94. doi: 10.1016/j.bmcl.2011.07.082. Epub 2011 Aug 12. Bioorg Med Chem Lett. 2011. PMID: 21903390
Discovery of a Selective S1P1 Receptor Agonist Efficacious at Low Oral Dose and Devoid of Effects on Heart Rate.
Demont EH, Andrews BI, Bit RA, Campbell CA, Cooke JW, Deeks N, Desai S, Dowell SJ, Gaskin P, Gray JR, Haynes A, Holmes DS, Kumar U, Morse MA, Osborne GJ, Panchal T, Patel B, Perboni A, Taylor S, Watson R, Witherington J, Willis R. Demont EH, et al. ACS Med Chem Lett. 2011 Mar 24;2(6):444-9. doi: 10.1021/ml2000214. eCollection 2011 Jun 9. ACS Med Chem Lett. 2011. PMID: 24900328 Free PMC article.
Optimization of sphingosine-1-phosphate-1 receptor agonists: effects of acidic, basic, and zwitterionic chemotypes on pharmacokinetic and pharmacodynamic profiles.
Skidmore J, Heer J, Johnson CN, Norton D, Redshaw S, Sweeting J, Hurst D, Cridland A, Vesey D, Wall I, Ahmed M, Rivers D, Myatt J, Giblin G, Philpott K, Kumar U, Stevens A, Bit RA, Haynes A, Taylor S, Watson R, Witherington J, Demont E, Heightman TD. Skidmore J, et al. J Med Chem. 2014 Dec 26;57(24):10424-42. doi: 10.1021/jm5010336. Epub 2014 Dec 15. J Med Chem. 2014. PMID: 25431977
333 results