Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives of the formula and the phamaceutically-accepted salts thereof 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-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.

Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives of the formula ##STR1## and the pharmaceutically-acceptable salts thereof 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.

Abstract: 4-Chloro-2-thiophenecarboxylic acid is made by forming a compound of formula (Ia), disclosed herein, wherein R.sup.3 is (C.sub.1 -C.sub.6) alkyl, phenyl, or benzyl; converting the compound to a compound of formula (IVa), disclosed herein, and removing the silyl group R.sub.3 Si--. The product is useful as an intermediate in making pharmaceutical products.

Abstract: Macrolides of formula (I) and methods of treatment of resistance to transplantation, fungal infections and autoimmune diseases such as rheumatoid arthritis and psoriasis using said macrolides of formula (I), wherein n is 1 or 2; A and B are taken together and form .dbd.O or A and B are taken separately and are each H or A is OH and B is H; R.sup.1 is a 2-aminoglycosyl group; R.sup.2 is OH or a glycosyloxy group; and R.sup.3 is an alkyl or allyl group.

Abstract: Certain 4-aminopyrazolo[3,4-d]pyrimidine compounds, and their pharmaceutically-acceptable salts and prodrugs, are inhibitors of tyrosine kinase enzymes and are useful for immunoregulation and for the treatment of cancer, angiogenesis and atherosclerosis.

Abstract: Macrolides of formula (I) and methods of treatment of resistance to transplantation, fungal infections and auto-immune diseases such as rheumatoid arthritis and psoriasis using said macrolides of formula (I), ##STR1## wherein n is 1 or 2; A and B are taken together and form .dbd.O or A and B are taken separately and are each H or A is OH and B is H; R.sup.1 is a desosamino group; R.sup.2 is OH or a desosaminyloxy group; and R.sup.3 is an alkyl or allyl group.

Abstract: Macrolides of the FK-506 type and methods of treatment of resistance to transplantation, fungal infections, and autoimmune diseases such as rheumatoid arthritis and psoriasis using said macrolides.

Abstract: The use of rapamycin prodrugs of formula I as immunosuppressant agents, intermediates formed in the preparation of its prodrugs as well as the prodrugs themselves.

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.

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.

Abstract: This invention relates to the use of certain 3-substituted-2-oxindole derivatives to inhibit interleukin-1 biosynthesis in a mammal. This invention also relates to the use of such compounds for treating interleukin-1 mediated disorders and dysfunctions such as bone and connective tissue metabolism disorders and immune dysfunction in a mammal. The methods of this invention comprise administering an interleukin-1 biosynthesis inhibiting amount of the compounds and salts of this invention to such a mammal.

Abstract: This invention relates to novel 3-(1-substituted-pyrazoyl)-2-oxindole derivatives which are inhibitors of prostaglandin H.sub.2 synthease, 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-(1-substituted-pyrazoyl-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 compounds useful as intermediates in the preparation of the 3-(1-substituted-pyrazoyl-2-oxindole derivatives of this invention and to a process for the preparation of the 3-(1-substituted-pyrazoyl)-2-oxindole derivatives.

Abstract: Process for making antiinflammatory 3-aroyl-2-oxindole-1-carboxamides by reductive debromination or deiodination of 3-(bromo- or iodoaroyl)-2-oxindole-1-carboxamides.

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.