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 …
…, M Gibson, PA Goldsmith, DN Hurst, A Naylor…
文献索引：Hall, Adrian; Billinton, Andy; Brown, Susan H.; Chowdhury, Anita; Clayton, Nicholas M.; Giblin, Gerard M.P.; Gibson, Mairi; Goldsmith, Paul A.; Hurst, David N.; Naylor, Alan; Peet, Caroline F.; Scoccitti, Tiziana; Wilson, Alexander W.; Winchester, Wendy Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 9 p. 2599 - 2603
We describe the medicinal chemistry programme that led to the identification of the EP1 receptor antagonist GSK269984A (8h). GSK269984A was designed to overcome development issues encountered with previous EP1 antagonists such as GW848687X and was found to display excellent activity in preclinical models of inflammatory pain. However, upon cross species pharmacokinetic profiling, GSK269984A was predicted to have ...
