190966-40-6Relevant academic research and scientific papers
2,3-diarylcyclopentenones as orally active, highly selective cyclooxygenase-2 inhibitors
Black, W. Cameron,Brideau, Christine,Chan, Chi-Chung,Charleson, Stella,Chauret, Nathalie,Claveau, David,Ethier, Diane,Gordon, Robert,Greig, Gillian,Guay, Jocelyne,Hughes, Gregory,Jolicoeur, Paule,Leblanc, Yves,Nicoll-Griffith, Deborah,Ouimet, Nathalie,Riendeau, Denis,Visco, Denise,Wang, Zhaoyin,Xu, Lijing,Prasit, Petpiboon
, p. 1274 - 1281 (2007/10/03)
Cyclopentenones containing a 4-(methylsulfonyl)phenyl group in the 3- position and a phenyl ring in the 2-position are selective inhibitors of cyclooxygenase-2 (COX-2). The selectivity for COX-2 over COX-1 is dramatically improved by substituting the 2-phenyl group with halogens in the meta position or by replacing the phenyl ring with a 2- or 3-pyridyl ring. Thus the 3,5-difluorophenyl derivative 7 (L-776,967) and the 3-pyridyl derivative 13 (L-784,506) are particularly interesting as potential antiinflammatory agents with reduced side-effect profiles. Both exhibit good oral bioavailability and are potent in standard models of pain, fever, and inflammation yet have a much reduced effect on the GI integrity of rats compared to standard nonsteroidal antiflammatory drugs.
Pyridinyl-2-cyclopenten-1-ones as selective cyclooxygenase-2 inhibitors
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, (2008/06/13)
The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I.
3,4-diaryl-2-hydroxy-2,5-dihydrofurans as prodrugs to COX-2 inhibitors
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, (2008/06/13)
The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. STR1 The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
