3-substituted-2-oxindole derivatives

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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544233, 544246, 544343, 546 61, 546 79, 548129, 548130, 548136, 548151, 548207, 548217, 548243, 548247, 548251, 548259, 5482632, 548372, 548420, 548501, 549 16, 549 31, 549 25, 549 27, 549 44, 549358, 549383, 549432, 549456, 568732, 574183, C07D20934

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050475541

ABSTRACT:
This invention relates to novel 3-substituted-2-oxindole derivatives which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 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 H.sub.2 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.

REFERENCES:
patent: 4721712 (1988-01-01), Kadin
patent: 4752609 (1988-06-01), Kadin
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Black, T. H., Organic Preparation and Procedures Int. 21: 179-217 (1989).
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Bergmann, M. et al., Hoppe-Seyler's Zeitschrift Fur Physiol. Chem. 125: 145-155 (1928).
Staab, H. A. et al., Chemische Berichte 95: 1275-1283 (1962) (Staab II).
Staab, H. A. et al., Chemische Berichte 95: 1284-1297 (1962), (Staab III).
Kobuke, Y. et al., Tetrahedron Letters No. 4, 367-370 (1978).
Brooks, D. W. et al., Angew Chem. Int. Ed. Engl. 18: 72-74 (1979).
Staab, H., Angewandte Chemie, International Edition in English, vol. 1, #7, 1962.

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