Sterling Winthrop Inc.

Sanofi

Eastman-kodak Company

Sterling Drug Inc.

Sanofi Sa

Lee H Latimer

Richard P Dunlap

Chakrapani Subramanyam

Ranjit C Desai

Dennis J Hlasta

William N Washburn

Carl R Illig

Malcolm R Bell

Virendra Kumar

John J Court

Barbara Boland Lussier

Albert J Mura, Jr

Neil Warren Boaz

Alexander L Weis

Eric P Lodge

Albert Joseph Mura

Elizabeth G Burns

Paul R Buckland

Lynda W McGarry

Gary S Proehl

Carl B Illig

Ranjit Chimanlal Desai

Barbara B Lussier

Albert A Mura

Dennis John Hlasta

Eric Piatt Lodge

Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytic enzymes, are useful in the treatment of degenerative diseases and have the formula ##STR1## wherein: L is --O--, --S--, --SO-- or --SO.sub.2 --;

Saccharin derivatives useful as proteolytic enzyme inhibitors and

4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl heterocyclic carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with either a heterocyclic carboxylic acid in the presence of an acid-acceptor or the alkali metal salt of a heterocyclic carboxylic acid.

2-Saccharinylmethyl heterocyclic carboxylates useful as proteolytic

4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl aryl and aryloxy acetates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with an aryl or aryloxyacetic acid in the presence of an acid-acceptor.

2-saccharinylmethyl aryl and arloxy acetates useful as proteolytic

Compounds having the structural formula ##STR1## wherein L is N, O or SO.sub.n wherein n is 0, 1 or 2;

Saccharin derivative proteolytic enzyme inhibitors

2-saccharinylmethyl heterocyclic carboxylates useful as proteolytic

Substituted hydroxylamines useful in photographic processing solution can be prepared by reacting a hydroxylamine with a vinylic compound having an electron withdrawing substituent in a suitable solvent, in the absence of a neutralizing base. The resulting products can be used without isolation from the reaction solution.

Method for preparing hydroxylamines using vinylic compounds without base

Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytic enzymes, are useful in the treatment of degenerative diseases and have the formula ##STR1## wherein: L is --O--, --S--, --SO--or --SO.sub.2 --;

Compounds having the structural formula ##STR1## wherein L is O;

2-saccharinylmethyl aryl and aryloxy acetates useful as proteolytic

Certain 3,4-disubstituted phenols and pharmaceutically acceptable salts thereof are provided which mimic IL-1 activity by inducing IL-2 synthesis and subsequent IL-2 receptor expression. Specifically, the invention provides compounds of Formula I and acid addition salts thereof: ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation; R is alkyl; R.sup.1 is --OH; R.sup.2 is H, alkyl, cycloalkyl, aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted nitrogen heterocyclic group having 4 to 5 nuclear carbon atoms; and R.sup.3 is a lipophilic moiety selected from the group consisting of substituted C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.16 cycloalkyl and 2,4-di-t-pentylphenyl.

3,4-disubstituted phenols-immunomodulating agents

A method for inducing the production of interleukin 2 in a warm blooded animal by administering an effective amount of a compound of the formula (I) ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation;

3,4-disubstituted anilines-immunomodulating agents

4-R.sup.4 --R.sup.5 -2-Saccharinylmethyl aryl and aryloxy acetates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 --R.sup.5 -2-halomethylsaccharin with an aryl or aryloxyacetic acid in the presence of an acid-acceptor.

Growing community of inventors

Brighton, NY, United States of America

Lee H Latimer