3-substituted-2-oxindole derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514365, 514369, 514370, 514371, 514372, 514374, 514376, 514377, 514378, 514380, 514385, 514386, 514397, 514403, 514404, 514406, 514407, 548112, 548181, 548182, 548183, 548184, 548185, 548186, 548187, A61K 31405, A61K 31415, A61K 3142, A61K 31425

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active

052908020

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: 3634453 (1972-01-01), McManus et al.
patent: 3900563 (1975-08-01), Allen, Jr. et al.
patent: 4556672 (1985-12-01), Kadin
patent: 4569942 (1986-02-01), Kadin
patent: 4690943 (1987-09-01), Kadin
patent: 4695571 (1987-09-01), Melvin
patent: 4721712 (1988-01-01), Kadin
patent: 4752609 (1988-06-01), Kadin
patent: 4808601 (1989-02-01), Kadin
patent: 4861794 (1989-08-01), Otterness
Carpenter, A. J. et al., Regioselective alpha- and beta-Metallations of Thiophene Derivatives Bearing the 4,4-Dimethyloxazolin-2-yl Group. Application of the Method to Syntheses of 2,3- and 2,5-Disubstituted Thiophene Derivatives, J. Chem. Soc. Perkin Trans I:173-181 (1985) (Carpenter I).
Carpenter, A. J., et al., The Scope and Limitations of Carboxamide-Induced beta-Directed Metalation of 2-Substituted Furan, Thiophene, and 1-Methylpyrrole Derivatives. Application of the Method to Syntheses of 2,3-Disubstituted Thiophenes and Furans, J. Org. Chem. 50:4362-4368 (1985) (Carpenter II).
2-Mercaptothiazol-4-ylthiophenecarboxylic acids, Chem. Abstr. 103:22580m (1985).
2-Azolyl-5-oxadiazolylthiophenes, Chem. Abstr. 63, column 4432 (1965).
Benkeser, R. A., et al., Selective Reduction of Aromatic Carboxyl Groups to Methyl in the Presence of Ester Functionality. A New Procedure for the Preparation of Ester-Containing Organosilanes, J. Org. Chem. 38:3660-3661 (1973).
Chem. Abstr. 49 columns 2233-2236 (1955).
Brooks, D. W., et al., C-Acylation under Virtually Neutral Conditions, Angew. Chem. Int. Ed. Engl. 18:72-74 (1979).
Staab, H. A., Aregewande Chem. 17:415 part e (1962)(Angew. Chem. Internat. Edit. 1(7):351-367(1962)).
Baker, D. C., C-Acylation of Nitromethane. A Synthetic Route to alpha-Nitroketones, Synthesis (1978) pp. 478-479.
Otterness, I. G., et al., Effects of CP-66,248 on IL-1 Synthesis by Murine Peritoneal Macrophages, Arthritis & Rheumatism 31 No. 4 (Supplement):S90 Abstract C55 (1988).
Davis, J. S., et al., Clinical Efficacy of CP-66,248 [5-Chloro-2,3-dihydro-2-oxo-3-(2-thienylcarbonyl)-indole-1-carboxamide] in Osteoarthritis, Arthritis & Rheumatism 31 No. 4 (Supplement):S72 Abstract B78 (1988).
"Three Pfizer Drugs Promising; FDA Okay to Be Sought in '89", Chemical Marketing Reporter, Sep. 14, 1987, p. 7.
FDC Reports "The Pink Sheet".sup..RTM., Sep. 14, 1987, p.2.
FDC Reports "The Pink Sheet".sup..RTM., Sep. 28, 1987, p. 11.
Kobayashi, Goro et al., Chem. Abst. 69 (13): 4854 (No. 52001v), Sep. 23, 1968.
Oki, Sadao et al., Chem. Abst. 78 (21): 363 (No. 136057s), May 28, 1973.
Chem. Abst. 98 (21): 659 (No. 179366x), May 23, 1983.

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