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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: billinton a. J Med Chem. 2009 Oct 8;52(19):5785-8. doi: 10.1021/jm9009857. J Med Chem. 2009. PMID: 19743867
Discovery of a novel indole series of EP1 receptor antagonists by scaffold hopping.
Hall A, Billinton A, Brown SH, Chowdhury A, Giblin GM, Goldsmith P, Hurst DN, Naylor A, Patel S, Scoccitti T, Theobald PJ. Hall A, et al. Among authors: billinton a. Bioorg Med Chem Lett. 2008 Apr 15;18(8):2684-90. doi: 10.1016/j.bmcl.2008.03.018. Epub 2008 Mar 10. Bioorg Med Chem Lett. 2008. PMID: 18378447
Discovery of brain penetrant, soluble, pyrazole amide EP1 receptor antagonists.
Hall A, Billinton A, Bristow AK, Brown SH, Chowdhury A, Cutler L, Giblin GM, Goldsmith P, Hayhow TG, Kilford IR, Naylor A, Passingham B, Rawlings DA. Hall A, et al. Among authors: billinton a. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4027-32. doi: 10.1016/j.bmcl.2008.05.118. Epub 2008 Jun 5. Bioorg Med Chem Lett. 2008. PMID: 18571922
Discovery of a novel series of nonacidic benzofuran EP1 receptor antagonists.
Allan AC, Billinton A, Brown SH, Chowdhury A, Eatherton AJ, Fieldhouse C, Giblin GM, Goldsmith P, Hall A, Hurst DN, Naylor A, Rawlings DA, Sime M, Scoccitti T, Theobald PJ. Allan AC, et al. Among authors: billinton a. Bioorg Med Chem Lett. 2011 Jul 15;21(14):4343-8. doi: 10.1016/j.bmcl.2011.05.047. Epub 2011 May 23. Bioorg Med Chem Lett. 2011. PMID: 21676612
Discovery of {4-[4,9-bis(ethyloxy)-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl]-2-fluorophenyl}acetic acid (GSK726701A), a novel EP4 receptor partial agonist for the treatment of pain.
Healy MP, Allan AC, Bailey K, Billinton A, Chessell IP, Clayton NM, Giblin GMP, Kay MA, Khaznadar T, Michel AD, Naylor A, Price H, Spalding DJ, Stevens DA, Swarbrick ME, Wilson AW. Healy MP, et al. Among authors: billinton a. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1892-1896. doi: 10.1016/j.bmcl.2018.03.091. Epub 2018 Mar 31. Bioorg Med Chem Lett. 2018. PMID: 29636218
EP1 antagonists for the treatment of inflammatory pain.
Hall A, Billinton A, Giblin GM. Hall A, et al. Among authors: billinton a. Curr Opin Drug Discov Devel. 2007 Sep;10(5):597-612. Curr Opin Drug Discov Devel. 2007. PMID: 17786859 Review.
Non-acidic pyrazole EP1 receptor antagonists with in vivo analgesic efficacy.
Hall A, Billinton A, Brown SH, Clayton NM, Chowdhury A, Giblin GM, Goldsmith P, Hayhow TG, Hurst DN, Kilford IR, Naylor A, Passingham B, Winyard L. Hall A, et al. Among authors: billinton a. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3392-9. doi: 10.1016/j.bmcl.2008.04.018. Epub 2008 Apr 11. Bioorg Med Chem Lett. 2008. PMID: 18462938
Discovery of sodium 6-[(5-chloro-2-{[(4-chloro-2-fluorophenyl)methyl]oxy}phenyl)methyl]-2-pyridinecarboxylate (GSK269984A) an EP(1) receptor antagonist for the treatment of inflammatory pain.
Hall A, Billinton A, Brown SH, Chowdhury A, Clayton NM, Giblin GM, Gibson M, Goldsmith PA, Hurst DN, Naylor A, Peet CF, Scoccitti T, Wilson AW, Winchester W. Hall A, et al. Among authors: billinton a. Bioorg Med Chem Lett. 2009 May 1;19(9):2599-603. doi: 10.1016/j.bmcl.2009.02.112. Epub 2009 Mar 3. Bioorg Med Chem Lett. 2009. PMID: 19332369
Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor.
Abdi MH, Beswick PJ, Billinton A, Chambers LJ, Charlton A, Collins SD, Collis KL, Dean DK, Fonfria E, Gleave RJ, Lejeune CL, Livermore DG, Medhurst SJ, Michel AD, Moses AP, Page L, Patel S, Roman SA, Senger S, Slingsby B, Steadman JG, Stevens AJ, Walter DS. Abdi MH, et al. Among authors: billinton a. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5080-4. doi: 10.1016/j.bmcl.2010.07.033. Epub 2010 Jul 14. Bioorg Med Chem Lett. 2010. PMID: 20673717
48 results