157671-73-3Relevant academic research and scientific papers
Method of treating skin related conditions
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, (2008/06/13)
A class of 3,4-diaryl substituted thiophene, derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: wherein Y is S; wherein X is one or two substituents selected from hydrido, halo, lower alkoxycarbonyl and carboxyl; wherein R2 and R3 are independently aryl or heteroaryl; and wherein R2 and R3 are optionally substituted with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.
Chemistry and pharmacokinetics of diarylthiophenes and terphenyls as selective COX-2 inhibitors
Pinto, Donald J.P.,Copeland, Robert A.,Covington, Maryanne B.,Pitts, William J.,Batt, Douglas G.,Orwat, Michael J.,Lam, Gilbert N.,Joshi, Amita,Chan, Yuk-Charn,Wang, Shuaige,Trzaskos, James M.,Magolda, Ronald L.,Kornhauser, David M.
, p. 2907 - 2912 (2007/10/03)
DuP697, 2-bromo-4-(4'-sulfonylmethyl)phenyl-5-(4'-fluoro)phenylthiophene, is a selective type 2 cyclooxygenase (COX-2) inhibitor. Its relatively weak COX-2 selectivity coupled with a poor human pharmacokinetic profile led us to seek improvements on the in vitro selectivity while at the same time, addressing some of its pharmacokinetic liabilities. In this paper we discuss some strategies at solving the PK issue within a class of COX-2 inhibitors. The result of these efforts led to the discovery of a new class of COX-2 inhibitors the terphenyls, which prove to be superior alternatives to the diarylthiophenes.
