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Discovery of 1-[4-(3-chlorophenylamino)-1-methyl-1H-pyrrolo[3,2-c]pyridin-7-yl]-1-morpholin-4-ylmethanone (GSK554418A), a brain penetrant 5-azaindole CB2 agonist for the treatment of chronic pain.
Giblin GM, Billinton A, Briggs M, Brown AJ, Chessell IP, Clayton NM, Eatherton AJ, Goldsmith P, Haslam C, Johnson MR, Mitchell WL, Naylor A, Perboni A, Slingsby BP, Wilson AW. Giblin GM, et al. Among authors: haslam c. J Med Chem. 2009 Oct 8;52(19):5785-8. doi: 10.1021/jm9009857. J Med Chem. 2009. PMID: 19743867
Discovery of 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro- 2H-pyran-4-yl)methyl]-4-(trifluoromethyl)- 5-pyrimidinecarboxamide, a selective CB2 receptor agonist for the treatment of inflammatory pain.
Giblin GM, O'Shaughnessy CT, Naylor A, Mitchell WL, Eatherton AJ, Slingsby BP, Rawlings DA, Goldsmith P, Brown AJ, Haslam CP, Clayton NM, Wilson AW, Chessell IP, Wittington AR, Green R. Giblin GM, et al. J Med Chem. 2007 May 31;50(11):2597-600. doi: 10.1021/jm061195+. Epub 2007 May 4. J Med Chem. 2007. PMID: 17477516
Pyridine-3-carboxamides as novel CB(2) agonists for analgesia.
Mitchell WL, Giblin GM, Naylor A, Eatherton AJ, Slingsby BP, Rawlings AD, Jandu KS, Haslam CP, Brown AJ, Goldsmith P, Clayton NM, Wilson AW, Chessell IP, Green RH, Whittington AR, Wall ID. Mitchell WL, et al. Bioorg Med Chem Lett. 2009 Jan 1;19(1):259-63. doi: 10.1016/j.bmcl.2008.10.118. Epub 2008 Nov 5. Bioorg Med Chem Lett. 2009. PMID: 19010671
The discovery of potent and selective kynurenine 3-monooxygenase inhibitors for the treatment of acute pancreatitis.
Liddle J, Beaufils B, Binnie M, Bouillot A, Denis AA, Hann MM, Haslam CP, Holmes DS, Hutchinson JP, Kranz M, McBride A, Mirguet O, Mole DJ, Mowat CG, Pal S, Rowland P, Trottet L, Uings IJ, Walker AL, Webster SP. Liddle J, et al. Bioorg Med Chem Lett. 2017 May 1;27(9):2023-2028. doi: 10.1016/j.bmcl.2017.02.078. Epub 2017 Mar 9. Bioorg Med Chem Lett. 2017. PMID: 28336141 Free article.
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives.
Westaway SM, Preston AG, Barker MD, Brown F, Brown JA, Campbell M, Chung CW, Drewes G, Eagle R, Garton N, Gordon L, Haslam C, Hayhow TG, Humphreys PG, Joberty G, Katso R, Kruidenier L, Leveridge M, Pemberton M, Rioja I, Seal GA, Shipley T, Singh O, Suckling CJ, Taylor J, Thomas P, Wilson DM, Lee K, Prinjha RK. Westaway SM, et al. Among authors: haslam c. J Med Chem. 2016 Feb 25;59(4):1370-87. doi: 10.1021/acs.jmedchem.5b01538. Epub 2016 Jan 15. J Med Chem. 2016. PMID: 26771203
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives.
Westaway SM, Preston AG, Barker MD, Brown F, Brown JA, Campbell M, Chung CW, Diallo H, Douault C, Drewes G, Eagle R, Gordon L, Haslam C, Hayhow TG, Humphreys PG, Joberty G, Katso R, Kruidenier L, Leveridge M, Liddle J, Mosley J, Muelbaier M, Randle R, Rioja I, Rueger A, Seal GA, Sheppard RJ, Singh O, Taylor J, Thomas P, Thomson D, Wilson DM, Lee K, Prinjha RK. Westaway SM, et al. Among authors: haslam c. J Med Chem. 2016 Feb 25;59(4):1357-69. doi: 10.1021/acs.jmedchem.5b01537. Epub 2016 Jan 15. J Med Chem. 2016. PMID: 26771107
223 results