- 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
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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
- 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.
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p. 1805 - 1809
(2008/02/02)
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- Crystal forms of 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl pyridine
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The invention concerns crystalline forms of 2-(3-difluromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine, their preparation and use in pharmaceuticals.
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- Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine
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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.
- 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
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- Heterocyclo-alkylsulfonyl pyrazole derivatives as anti-inflammatory/analgesic agents
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The present invention relates to compounds of the formula wherein R2, R3, R6and A are defined as in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as osteoarthritis, rheumatoid arthritis, colon cancer and Alzheimer's disease, in mammals (preferably humans, dogs, cats and livestock).
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- Process for preparing heterocyclo-alkysulfonyl pyrazole derivatives
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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
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