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Discovery of 6-Amino-2-{[(1S)-1-methylbutyl]oxy}-9-[5-(1-piperidinyl)pentyl]-7,9-dihydro-8H-purin-8-one (GSK2245035), a Highly Potent and Selective Intranasal Toll-Like Receptor 7 Agonist for the Treatment of Asthma.
Biggadike K, Ahmed M, Ball DI, Coe DM, Dalmas Wilk DA, Edwards CD, Gibbon BH, Hardy CJ, Hermitage SA, Hessey JO, Hillegas AE, Hughes SC, Lazarides L, Lewell XQ, Lucas A, Mallett DN, Price MA, Priest FM, Quint DJ, Shah P, Sitaram A, Smith SA, Stocker R, Trivedi NA, Tsitoura DC, Weller V. Biggadike K, et al. Among authors: coe dm. J Med Chem. 2016 Mar 10;59(5):1711-26. doi: 10.1021/acs.jmedchem.5b01647. Epub 2016 Feb 10. J Med Chem. 2016. PMID: 26861551
Investigation of Janus Kinase (JAK) Inhibitors for Lung Delivery and the Importance of Aldehyde Oxidase Metabolism.
Wellaway CR, Baldwin IR, Bamborough P, Barker D, Bartholomew MA, Chung CW, Dümpelfeld B, Evans JP, Fazakerley NJ, Homes P, Keeling SP, Lewell XQ, McNab FW, Morley J, Needham D, Neu M, van Oosterhout AJM, Pal A, Reinhard FBM, Rianjongdee F, Robertson CM, Rowland P, Shah RR, Sherriff EB, Sloan LA, Teague S, Thomas DA, Wellaway N, Wojno-Picon J, Woolven JM, Coe DM. Wellaway CR, et al. Among authors: coe dm. J Med Chem. 2022 Jan 13;65(1):633-664. doi: 10.1021/acs.jmedchem.1c01765. Epub 2021 Dec 20. J Med Chem. 2022. PMID: 34928601
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
Procopiou PA, Barrett VJ, Bevan NJ, Biggadike K, Butchers PR, Coe DM, Conroy R, Edney DD, Field RN, Ford AJ, Guntrip SB, Looker BE, McLay IM, Monteith MJ, Morrison VS, Mutch PJ, Richards SA, Sasse R, Smith CE. Procopiou PA, et al. Among authors: coe dm. J Med Chem. 2009 Apr 23;52(8):2280-8. doi: 10.1021/jm801016j. J Med Chem. 2009. PMID: 19317397
Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists.
Biggadike K, Caivano M, Clackers M, Coe DM, Hardy GW, Humphreys D, Jones HT, House D, Miles-Williams A, Skone PA, Uings I, Weller V, McLay IM, Macdonald SJ. Biggadike K, et al. Among authors: coe dm. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4846-50. doi: 10.1016/j.bmcl.2009.06.020. Epub 2009 Jun 13. Bioorg Med Chem Lett. 2009. PMID: 19592247
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.
Procopiou PA, Barrett VJ, Bevan NJ, Biggadike K, Box PC, Butchers PR, Coe DM, Conroy R, Emmons A, Ford AJ, Holmes DS, Horsley H, Kerr F, Li-Kwai-Cheung AM, Looker BE, Mann IS, McLay IM, Morrison VS, Mutch PJ, Smith CE, Tomlin P. Procopiou PA, et al. Among authors: coe dm. J Med Chem. 2010 Jun 10;53(11):4522-30. doi: 10.1021/jm100326d. J Med Chem. 2010. PMID: 20462258
Discovery of a potent series of non-steroidal non α-trifluoromethyl carbinol glucocorticoid receptor agonists with reduced lipophilicity.
Diallo H, Angell DC, Barnett HA, Biggadike K, Coe DM, Cooper TW, Craven A, Gray JR, House D, Jack TI, Keeling SP, Macdonald SJ, McLay IM, Oliver S, Taylor SJ, Uings IJ, Wellaway N. Diallo H, et al. Among authors: coe dm. Bioorg Med Chem Lett. 2011 Feb 15;21(4):1126-33. doi: 10.1016/j.bmcl.2010.12.121. Epub 2010 Dec 31. Bioorg Med Chem Lett. 2011. PMID: 21257309
Pyrazolopyridines as potent PDE4B inhibitors: 5-heterocycle SAR.
Mitchell CJ, Ballantine SP, Coe DM, Cook CM, Delves CJ, Dowle MD, Edlin CD, Hamblin JN, Holman S, Johnson MR, Jones PS, Keeling SE, Kranz M, Lindvall M, Lucas FS, Neu M, Solanke YE, Somers DO, Trivedi NA, Wiseman JO. Mitchell CJ, et al. Among authors: coe dm. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5803-6. doi: 10.1016/j.bmcl.2010.07.136. Epub 2010 Aug 5. Bioorg Med Chem Lett. 2010. PMID: 20732811
Nonsteroidal glucocorticoid agonists: tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (transrepression/transactivation) efficacy selectivity.
Biggadike K, Boudjelal M, Clackers M, Coe DM, Demaine DA, Hardy GW, Humphreys D, Inglis GG, Johnston MJ, Jones HT, House D, Loiseau R, Needham D, Skone PA, Uings I, Veitch G, Weingarten GG, McLay IM, Macdonald SJ. Biggadike K, et al. Among authors: coe dm. J Med Chem. 2007 Dec 27;50(26):6519-34. doi: 10.1021/jm070778w. Epub 2007 Nov 27. J Med Chem. 2007. PMID: 18038970
Design and x-ray crystal structures of high-potency nonsteroidal glucocorticoid agonists exploiting a novel binding site on the receptor.
Biggadike K, Bledsoe RK, Coe DM, Cooper TW, House D, Iannone MA, Macdonald SJ, Madauss KP, McLay IM, Shipley TJ, Taylor SJ, Tran TB, Uings IJ, Weller V, Williams SP. Biggadike K, et al. Among authors: coe dm. Proc Natl Acad Sci U S A. 2009 Oct 27;106(43):18114-9. doi: 10.1073/pnas.0909125106. Epub 2009 Oct 12. Proc Natl Acad Sci U S A. 2009. PMID: 19822747 Free PMC article.
36 results