- Discovery of GSK345931A: An EP1 receptor antagonist with efficacy in preclinical models of inflammatory pain
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Herein we describe the medicinal chemistry programme to identify a potential back-up compound to the EP1 receptor antagonist GW848687X. This work started with the lipophilic 1,2-biaryl benzene derivative 4 which displayed molecular weight of 41
- Hall, Adrian,Brown, Susan H.,Budd, Christopher,Clayton, Nicholas M.,Giblin, Gerard M.P.,Goldsmith, Paul,Hayhow, Thomas G.,Hurst, David N.,Naylor, Alan,Anthony Rawlings,Scoccitti, Tiziana,Wilson, Alexander W.,Winchester, Wendy J.
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p. 497 - 501
(2011/03/18)
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- PYRIDYL COMPOUNDS
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Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein R1, R2, and R3 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions compris
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Page/Page column 27
(2008/06/13)
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- BIPHENYLOXYACETIC ACID DERIVATIVES FOR THE TREATMENT OF RESPIRATORY DISEASE
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The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
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Page/Page column 32
(2008/06/13)
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- Discovery of novel biaryl heterocyclic EP1 receptor antagonists
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We describe the generation of novel EP1 receptor antagonists by investigation of thiophene isosteres. In addition, we disclose preliminary in vitro and in vivo DMPK for selected compounds.
- Hall, Adrian,Bit, Rino A.,Brown, Susan H.,Chaignot, Helene M.,Chessell, Iain P.,Coleman, Tanya,Giblin, Gerard M.P.,Hurst, David N.,Kilford, Ian R.,Lewell, Xiao Q.,Michel, Anton D.,Mohamed, Shiyam,Naylor, Alan,Novelli, Riccardo,Skinner, Lee,Spalding, David J.,Tang, Sac P.,Wilson, Richard J.
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p. 2666 - 2671
(2007/10/03)
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- 2,3-Diarylthiophenes as selective EP1 receptor antagonists
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The synthesis and the EP1 receptor binding affinity of 2,3-diarylthiophene derivatives are described. The evaluation of the structure-activity relationship (SAR) in this series led to the identification of compounds 4, 7, and 12a, which exhibit high affinity for the human EP 1 receptor and a selectivity greater than 100-fold against the EP2, EP3, EP4, DP, FP, and IP receptors and greater than 25-fold versus the TP receptor. These three antagonists present good pharmacokinetics in rats and significant differences in the way they are distributed in the brain.
- Ducharme, Yves,Blouin, Marc,Carriere, Marie-Claude,Chateauneuf, Anne,Cote, Bernard,Denis, Danielle,Frenette, Richard,Greig, Gillian,Kargman, Stacia,Lamontagne, Sonia,Martins, Evelyn,Nantel, Francois,O'Neill, Gary,Sawyer, Nicole,Metters, Kathleen M.,Friesen, Richard W.
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p. 1155 - 1160
(2007/10/03)
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- HETEROCYCLYL COMPOUNDS
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Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, B, D, Z, R1, R2a , R2b, and Rx are as defined in the specification, a process for the preparation of such compounds, pharm
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Page/Page column 41
(2010/02/11)
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- CYCLOHEXENE COMPOUNDS
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Formula (I) wherein A, B, Z, R1, R2a , R2b, R8, R9 and Rx 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.
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Page/Page column 26
(2010/02/11)
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- NOVEL COMPOUNDS
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The invention relates to substituted phenoxyacetic acids (I) as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation
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- PHENYL COMPOUNDS
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Compounds of formula (I) or derivatives thereof: wherein A, B, Z, R, R, R, R, R, and R 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.
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- (2-((2-ALKOXY) -PHENYL) -CYCLOPENT-1-ENYL) AROMATIC CARBO AND HETEROCYCLIC ACID AND DERIVATIVES
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Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: (I) wherein A, R1 , R2 , Rx , R8 , R9 and n 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.
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Page/Page column 25
(2010/02/07)
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