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Page 1
Identification of potent, soluble, and orally active TRPV1 antagonists.
Ratcliffe P, Maclean J, Abernethy L, Clarkson T, Dempster M, Easson AM, Edwards D, Everett K, Feilden H, Littlewood P, McArthur D, McGregor D, McLuskey H, Nimz O, Nisbet LA, Palin R, Tracey H, Walker G. Ratcliffe P, et al. Among authors: littlewood p. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2559-63. doi: 10.1016/j.bmcl.2011.01.112. Epub 2011 Jan 31. Bioorg Med Chem Lett. 2011. PMID: 21435873
Structure-activity studies of a novel series of isoxazole-3-carboxamide derivatives as TRPV1 antagonists.
Palin R, Abernethy L, Ansari N, Cameron K, Clarkson T, Dempster M, Dunn D, Easson AM, Edwards D, Maclean J, Everett K, Feilden H, Ho KK, Kultgen S, Littlewood P, McArthur D, McGregor D, McLuskey H, Neagu I, Neale S, Nisbet LA, Ohlmeyer M, Pham Q, Ratcliffe P, Rong Y, Roughton A, Sammons M, Swanson R, Tracey H, Walker G. Palin R, et al. Among authors: littlewood p. Bioorg Med Chem Lett. 2011 Feb 1;21(3):892-8. doi: 10.1016/j.bmcl.2010.12.092. Epub 2010 Dec 23. Bioorg Med Chem Lett. 2011. PMID: 21236666
Discovery of potent, soluble and orally active TRPV1 antagonists. Structure-activity relationships of a series of isoxazoles.
Ratcliffe P, Abernethy L, Ansari N, Cameron K, Clarkson T, Dempster M, Dunn D, Easson AM, Edwards D, Everett K, Feilden H, Ho KK, Kultgen S, Littlewood P, Maclean J, McArthur D, McGregor D, McLuskey H, Neagu I, Nimz O, Nisbet LA, Ohlmeyer M, Palin R, Pham Q, Rong Y, Roughton A, Sammons M, Swanson R, Tracey H, Walker G. Ratcliffe P, et al. Among authors: littlewood p. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4652-7. doi: 10.1016/j.bmcl.2011.01.051. Epub 2011 Jan 26. Bioorg Med Chem Lett. 2011. PMID: 21723725
Discovery and optimisation of a selective non-steroidal glucocorticoid receptor antagonist.
Brown AR, Bosies M, Cameron H, Clark J, Cowley A, Craighead M, Elmore MA, Firth A, Goodwin R, Goutcher S, Grant E, Grassie M, Grove SJ, Hamilton NM, Hampson H, Hillier A, Ho KK, Kiczun M, Kingsbury C, Kultgen SG, Littlewood PT, Lusher SJ, Macdonald S, McIntosh L, McIntyre T, Mistry A, Morphy JR, Nimz O, Ohlmeyer M, Pick J, Rankovic Z, Sherborne B, Smith A, Speake M, Spinks G, Thomson F, Watson L, Weston M. Brown AR, et al. Bioorg Med Chem Lett. 2011 Jan 1;21(1):137-40. doi: 10.1016/j.bmcl.2010.11.054. Epub 2010 Nov 16. Bioorg Med Chem Lett. 2011. PMID: 21129964
Rational Design of 5-(4-(Isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amine (VX-970, M6620): Optimization of Intra- and Intermolecular Polar Interactions of a New Ataxia Telangiectasia Mutated and Rad3-Related (ATR) Kinase Inhibitor.
Knegtel R, Charrier JD, Durrant S, Davis C, O'Donnell M, Storck P, MacCormick S, Kay D, Pinder J, Virani A, Twin H, Griffiths M, Reaper P, Littlewood P, Young S, Golec J, Pollard J. Knegtel R, et al. Among authors: littlewood p. J Med Chem. 2019 Jun 13;62(11):5547-5561. doi: 10.1021/acs.jmedchem.9b00426. Epub 2019 May 16. J Med Chem. 2019. PMID: 31074988
150 results