343629-25-4Relevant articles and documents
In vitro and in vivo profile of 2-(3-di-fluoromethyl-5-phenylpyrazol-1-yl)- 5-methanesulfonylpyridine, a potent, selective, and orally active canine COX-2 inhibitor
Li, Jin,Lynch, Michael P.,DeMello, Kristin Lundy,Sakya, Subas M.,Cheng, Hengmiao,Rafka, Robert J.,Bronk, Brian S.,Jaynes, Burton H.,Kilroy, Carolyn,Mann, Donald W.,Haven, Michelle L.,Kolosko, Nicole L.,Petras, Carol,Seibel, Scott B.,Lund, Lisa A.
, p. 1805 - 1809 (2008/02/02)
The synthesis of a novel canine COX-2 selective inhibitor, 2-(3-difluoromethyl-5-phenylpyrazol-1-yl)-5-methanesulfonylpyridine, and its in vitro and in vivo profile are described. Pyrazole 8 demonstrated excellent potency and selectivity for canine COX-2
Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine
Li, Jin,Lundy DeMello, Kristin M.,Cheng, Henry,Sakya, Subas M.,Bronk, Brian S.,Rafka, Robert J.,Jaynes, Burton H.,Ziegler, Carl B.,Kilroy, Carolyn,Mann, Donald W.,Nimz, Eric L.,Lynch, Michael P.,Haven, Michelle L.,Kolosko, Nicole L.,Minich, Martha L.,Li, Chao,Dutra, Jason K.,Rast, Bryson,Crosson, Rhonda M.,Morton, Barry J.,Kirk, Glen W.,Callaghan, Kathleen M.,Koss, David A.,Shavnya, Andrei,Lund, Lisa A.,Seibel, Scott B.,Petras, Carol F.,Silvia, Annette
, p. 95 - 98 (2007/10/03)
Structure-activity relationship (SAR) studies of 2-[3-di(and tri)fluoromethyl-5-arylpyrazol-1-yl]-5-methanesulfonylpyridine derivatives for canine COX enzymes are described. This led to the identification of 12a as a lead candidate for further progression. The in vitro and in vivo activity of 12a for the canine COX-2 enzyme as well as its in vivo efficacy and pharmacokinetic properties in dog are highlighted.
Process for preparing heterocyclo-alkysulfonyl pyrazole derivatives
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, (2008/06/13)
The invention relates to processes for preparing compounds of formula 1: as well as intermediates useful in such processes, wherein R1-R4 are as defined herein. The compounds of formula 1 are useful in the treatment or alleviation of
