Sterling Drug Inc.

Sterling Winthrop Inc.

James H Ackerman

Albert J Mura, Jr

Ranjit C Desai

Dennis J Hlasta

Malcolm R Bell

Franklin J Rosenberg

Ardie R Nickel

Compounds having the structural formula ##STR1## which inhibit the enzymatic activity of proteolytic enzymes, and processes for preparation thereof, method of use thereof in treatment of degenerative diseases and pharmaceutical compositions thereof are disclosed.

Saccharin derivative proteolytic enzyme inhibitors

Pyrazolo[3,4-b]quinolines having the formula ##STR1## where R is hydrogen, hydroxy or alkoxy; R.sub.2 is halogen, cyano, carbamyl, carboxy, lower-alkylcarbonyl, amino or aminomethyl; and R.sub.1 is hydrogen or selected substituents as defined herein, are useful as antiviral agents and/or as vasodilators.

Pyrazolo[3,4-b]quinolines and their use as antiviral agents

3-Amino-2,4,6-triiodobenzoic acids optionally substituted in the 5-position by amino or carboxy or a derivative thereof react with dibasic acid anhydrides to give the corresponding cyclic imides (A), which can be hydrolyzed to the corresponding anilic acids (B). The latter can be further alkylated on the anilide nitrogen atom. Compounds A and B are useful as cholecystographic and urographic agents.

Iodinated anilic acids

Trichloroamino(and acylamino)phenylalkanoic acids or esters, useful as uricosuric agents, are prepared by chlorination of the corresponding aminophenylalkanoic acids or esters, followed, if desired, by N-acylation and N-alkylation.

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Albany, NY, United States of America

James H Ackerman