| 摘要 |
This invention relates to novel 3-substituted-2-oxindole derivatives which are inhibitors of prostaglandin H2 synthase, 5-lipoxpgenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H2 synthase and biosynthesis of interleukin-1 and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives, (wherein X and Y are H ar substituent, R1 is H, acyl, acylated alkyl, sulfonyl or phosphate, R2 is acyl, alkyl or phenyl, Q is heterocycle).
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