Pyrazole derivatives and COX inhibitors containing them
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United States of America Patent
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Oct 24, 2000
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N/A
app pub date -
Oct 7, 1999
filing date -
Apr 11, 1997
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Abstract
The purpose is to provide anti-inflammatory agents which have potent pharmacological actions and exert a selective inhibitory activity on COX-2, thereby being expected to reduce adverse effects such as disorders in gastric mucosa. The present invention encompasses a compound of the formula (1): wherein R.sup.1 is hydrogen or halogen, R.sup.2 and R.sup.3 are each independently hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy or lower alkanoyloxy, R.sup.4 is lower haloalkyl or lower alkyl, X is sulfur, oxygen or NH, and Y is lower alkylthio, lower alkylsulfonyl or sulfamoyl, which exerts superior anti-inflammatory activity, and highly inhibits COX-2 induced in inflamed sites, with less inhibitory action on COX-1 present in stomach, kidney, etc. Pharmaceutical agents comprising the compound of the present invention are provided as selective COX-2 inhibitors, and anti-inflammatory agents rarely accompanying adverse actions including attacks on gastric mucosa.
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