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Page 1
Scaffold-hopping with zwitterionic CCR3 antagonists: identification and optimisation of a series with good potency and pharmacokinetics leading to the discovery of AZ12436092.
Bahl A, Barton P, Bowers K, Caffrey MV, Denton R, Gilmour P, Hawley S, Linannen T, Luckhurst CA, Mochel T, Perry MW, Riley RJ, Roe E, Springthorpe B, Stein L, Webborn P. Bahl A, et al. Among authors: riley rj. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6694-9. doi: 10.1016/j.bmcl.2012.08.103. Epub 2012 Sep 11. Bioorg Med Chem Lett. 2012. PMID: 23021991
Discovery of potent and selective adamantane-based small-molecule P2X(7) receptor antagonists/interleukin-1beta inhibitors.
Furber M, Alcaraz L, Bent JE, Beyerbach A, Bowers K, Braddock M, Caffrey MV, Cladingboel D, Collington J, Donald DK, Fagura M, Ince F, Kinchin EC, Laurent C, Lawson M, Luker TJ, Mortimore MM, Pimm AD, Riley RJ, Roberts N, Robertson M, Theaker J, Thorne PV, Weaver R, Webborn P, Willis P. Furber M, et al. Among authors: riley rj. J Med Chem. 2007 Nov 29;50(24):5882-5. doi: 10.1021/jm700949w. Epub 2007 Oct 27. J Med Chem. 2007. PMID: 17963373
From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis.
Springthorpe B, Bailey A, Barton P, Birkinshaw TN, Bonnert RV, Brown RC, Chapman D, Dixon J, Guile SD, Humphries RG, Hunt SF, Ince F, Ingall AH, Kirk IP, Leeson PD, Leff P, Lewis RJ, Martin BP, McGinnity DF, Mortimore MP, Paine SW, Pairaudeau G, Patel A, Rigby AJ, Riley RJ, Teobald BJ, Tomlinson W, Webborn PJ, Willis PA. Springthorpe B, et al. Bioorg Med Chem Lett. 2007 Nov 1;17(21):6013-8. doi: 10.1016/j.bmcl.2007.07.057. Epub 2007 Aug 19. Bioorg Med Chem Lett. 2007. PMID: 17827008
The discovery of CCR3/H1 dual antagonists with reduced hERG risk.
Bahl A, Barton P, Bowers K, Brough S, Evans R, Luckhurst CA, Mochel T, Perry MW, Rigby A, Riley RJ, Sanganee H, Sisson A, Springthorpe B. Bahl A, et al. Among authors: riley rj. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6688-93. doi: 10.1016/j.bmcl.2012.08.124. Epub 2012 Sep 15. Bioorg Med Chem Lett. 2012. PMID: 23031591
Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H₁ antagonists. Part II: optimising in vivo clearance.
Furber M, Alcaraz L, Luckhurst C, Bahl A, Beaton H, Bowers K, Collington J, Denton R, Donald D, Kinchin E, MacDonald C, Rigby A, Riley R, Soars M, Springthorpe B, Webborn P. Furber M, et al. Among authors: riley r. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7707-10. doi: 10.1016/j.bmcl.2012.09.112. Epub 2012 Oct 10. Bioorg Med Chem Lett. 2012. PMID: 23116889
Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H₁ antagonists. Part I.
Furber M, Alcaraz L, Luckhurst C, Bahl A, Beaton H, Bowers K, Collington J, Denton R, Donald D, Kinchin E, MacDonald C, Rigby A, Riley R, Soars M, Springthorpe B, Webborn P. Furber M, et al. Among authors: riley r. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7702-6. doi: 10.1016/j.bmcl.2012.09.113. Epub 2012 Oct 23. Bioorg Med Chem Lett. 2012. PMID: 23142617
Time-dependent CYP inhibition.
Riley RJ, Grime K, Weaver R. Riley RJ, et al. Expert Opin Drug Metab Toxicol. 2007 Feb;3(1):51-66. doi: 10.1517/17425255.3.1.51. Expert Opin Drug Metab Toxicol. 2007. PMID: 17269894 Review.
1,612 results