Certain 5-alkyl-2-arylaminophenylacetic acids and derivatives

The invention relates to 5-alkyl-2-arylaminophenylacetic acids and derivatives thereof as defined herein which are particularly potent and selective cyclooxygenase-2(COX-2) inhibitors, methods for preparation thereof, pharmaceutical compositions comprising said compounds, methods of selectively inhi...

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Bibliographic Details
Main Authors Fujimoto, Roger A, McQuire, Leslie W, Mugrage, Benjamin B, van Duzer, John H
Format Patent
LanguageEnglish
Published 27.04.2004
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Summary:The invention relates to 5-alkyl-2-arylaminophenylacetic acids and derivatives thereof as defined herein which are particularly potent and selective cyclooxygenase-2(COX-2) inhibitors, methods for preparation thereof, pharmaceutical compositions comprising said compounds, methods of selectively inhibiting COX-2 activity and of treating conditions in mammals which are responsive to COX-2 inhibition using said compounds or pharmaceutical compositions comprising said compounds of the invention. Disclosed are the compounds of formula I wherein R is methyl or ethyl; Ris chloro or fluoro; Ris hydrogen or fluoro; Ris hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; Ris hydrogen or fluoro; and Ris chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.