892663-03-5Relevant academic research and scientific papers
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
Selection and development of the manufacturing route for EP1 antagonist GSK269984B
Whiting, Matthew,Harwood, Kathy,Hossner, Frank,Turner, Peter G.,Wilkinson, Mark C.
scheme or table, p. 820 - 831 (2011/03/19)
A potential manufacturing route for the EP1 antagonist GSK269984B was developed. Four synthetic approaches were examined, and a successful realisation of each is presented. The rationale supporting selection of the preferred route is discussed.
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
Development and scope of the phenolic aldol reaction of 2-formylpyridines
Whiting, Matthew,Wilkinson, Mark C.,Harwood, Kathy
experimental part, p. 1609 - 1613 (2009/12/03)
2-Formylpyridines have been shown to be suitable electrophiles for the magnesium-promoted phenolic aldol reaction. Exceptionally mild reaction conditions have been developed and a brief survey of the reaction scope has been conducted. This process gives straightforward access to a range of functionalised 2-hydroxyphenyl-2-pyridylmethanols and 2-hydroxyphenyl-2- pyridylmethanes via their subsequent reduction. Georg Thieme Verlag Stuttgart.
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
BENZOFURAN COMPOUNDS
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Page/Page column 35, (2008/12/08)
A compound of formula (I), wherein R1, R2, and R3 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in
BENZOFURAN COMPOUNDS AS EP1 RECEPTOR ANTAGONISTS
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Page/Page column 34, (2008/06/13)
Compounds of formula (I) or a pharmaceutically acceptable derivative thereof, wherein R1,R2a, R2b, R2c, and R3 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
PYRIDINE COMPOUNDS FOR THE TREATMENT OF PROSTAGLANDIN MEDIATED DISEASES
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Page/Page column 29-30, (2008/06/13)
Compounds of formula (I) or a pharmaceutiically acceptable derivative thereof: wherein X, Y, Z, R2a, R2b, R3a, R3b, R8, R9, and Rx are as defined in the specification, a process
