BIARYL-ACETIC ACID DERIVATIVES AND THEIR USE AS COX-2 INHIBITORS
The present invention relates to inhibitors of COX-2, compositions which contain such compounds and methods of use. The compounds are represented by formula I: and include pharmaceutically acceptable salts and esters thereof.
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Page/Page column 19-20
(2010/02/03)
Bisaryl COX-2 inhibiting compounds, compositions and methods of use
The present invention relates to inhibitors of COX-2, compositions which contain such compounds and methods of use. The compounds are represented by formula I: STR1 and include pharmaceutically acceptable salts and esters thereof.
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(2008/06/13)
Structure-based design of COX-2 selectivity into flurbiprofen
Comparative computer modeling of the X-ray crystal structures of cyclooxygenase isoforms COX-1 and COX-2 has led to the design of COX-2 selectivity into the nonselective inhibitor flurbiprofen. The COX-2 modeling was based on a postulated binding mode for flurbiprofen and took advantage of a small alcove in the COX-2 active site created by different positions of the Leu384 sidechain between COX-1 and COX-2. The design hypothesis was tested by synthesis and biological assay of a series of flurbiprofen analogs, culminating in the discovery of several inhibitors having up to 78-fold selectivity for COX-2 over COX-1.
Bayly, Christopher I.,Black, W. Cameron,Leger, Serge,Ouimet, Nathalie,Ouellet, Marc,Percival, M. David
p. 307 - 312
(2007/10/03)
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