892663-03-5Relevant articles and documents
Development of an in vivo active, dual EP1 and EP3 selective antagonist based on a novel acyl sulfonamide bioisostere
Downey, Jason D.,Saleh, Sam A.,Bridges, Thomas M.,Morrison, Ryan D.,Scott Daniels,Lindsley, Craig W.,Breyer, Richard M.
, p. 37 - 41 (2013/02/23)
Recent preclinical studies demonstrate a role for the prostaglandin E 2 (PGE2) subtype 1 (EP1) receptor in mediating, at least in part, the pathophysiology of hypertension and diabetes mellitus. A series of amide and N-acylsulfonamid
Discovery of sodium 6-[(5-chloro-2-{[(4-chloro-2-fluorophenyl)methyl]oxy}phenyl)methyl]-2-pyridinecarboxylate (GSK269984A) an EP1 receptor antagonist for the treatment of inflammatory pain
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
scheme or table, p. 2599 - 2603 (2010/05/19)
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 GW8
Novel methylene-linked heterocyclic EP1 receptor antagonists
Hall, Adrian,Bit, Rino A.,Brown, Susan H.,Chowdhury, Anita,Giblin, Gerard M.P.,Hurst, David N.,Kilford, Ian R.,Lewell, Xiao,Naylor, Alan,Scoccitti, Tiziana
, p. 1592 - 1597 (2008/12/22)
We describe the SAR, in terms of heterocyclic replacements, for a series of pyrazole EP1 receptor antagonists. This study led to the identification of several aromatic heterocyclic replacements for the pyrazole in the original compound. Investi
