3-(1-substitutedpyrazoyl)-2-oxindole derivatives

Details 3-(1-substitutedpyrazoyl)-2-oxindole derivatives 3-(1-substitutedpyrazoyl)-2-oxindole derivatives

C - Chemistry, Metallurgy

07

D

C07D 403/06 (2006.01) A61K 31/40 (2006.01) A61K 31/415 (2006.01) C07D 209/34 (2006.01) C07D 231/04 (2006.01)

Patent

CA 2086432

This invention relates to novel 3-(1-substitutedpyrazoyl)-2-oxindole derivatives which are inhibitors of prostaglandin H2 synthase, 5-lipoxygenase 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-(1-substitutedpyrazoyl)-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 compounds useful as intermediates in the preparation of the 3-(1-substitutedpyrazoyl)-2-oxindole derivatives of this invention and to a process for the preparation of the 3-(1-substitutedpyrazoyl)-2-oxindole derivatives.

La présente invention concerne de nouveaux dérivés du 3-(pyrazoyl-1-substitué)-2-oxindole qui sont des inhibiteurs de la biosynthèse de la prostaglandine-H2-synthase, de la 5-lipoxygénase et de l'interleukine-1. Les composés de l'invention sont utiles comme inhibiteurs de la biosynthèse de la prostaglandine-H2-synthase et de l'interleukine-1, en soi, et comme agents analgésiques, anti-inflammatoires et anti-arthritiques dans le traitement des maladies inflammatoires chroniques. La présente invention concerne également des compositions pharmaceutiques comprenant lesdits dérivés du 3-(pyrazoyl-1-substitué)-2-oxindole; des méthodes pour inhiber la prostaglandine-H2-synthase et la biosynthèse de l'interleukine-1; et pour traiter les maladies inflammatoires chroniques chez un mammifère avec lesdits composés. De plus, la présente invention concerne certains nouveaux composés utiles comme intermédiaires dans la préparation des dérivés du 3-(pyrazoyl-1-substitué)-2-oxindole de la présente invention et un procédé pour la préparation des dérivés du 3-(pyrazoyl-1-substitué)-2-oxindole.

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