Merck + Co., Inc.

Morris Zimmerman

James B Doherty

Bonnie M Ashe

Paul E Finke

Howard Jones

Shrenik K Shah

Conrad P Dorn

Robert L Clark

Raymond A Firestone

Dennis M Mulvey

Kevan R Thompson

Bunnie M Ashe

Derivatives of cephalosporin esters are found to be potent elastase inhibitors and therefore are useful antiinflammatory agents.

Cephalosporin derivatives as anti-inflammatory agents

.beta.-Lactam derivatives and analogs are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.

.beta.-Lactam derivatives as anti-inflammatory and antidegenerative

.beta.-lactam derivatives as anti-inflammatory and antidegenerative

Substituted cephalosporin sulfoxides are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.

Substituted cephalosporin sulfoxides as anti-inflammatory and

Substituted cephalosporin sulfones are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.

Substituted cephalosporin sulfones as anti-inflammatory and

Derivatives of N-carboxyl-thienamycin esters and analogs thereof are found to be potent elastase inhibitors and thereby useful anti-inflammatory agents.

N-Carboxyl-thienamycin esters and analogs thereof as anti-inflammatory

Derivatives of 1-carbapenem-3-carboxylic esters are found to be potent elastase inhibitors and therefore are useful anti-inflammatory agents.

1-Carbapenem-3-carboxylic esters as anti-inflammatory agents

N-acyl-derivatives of thienamycin esters are found to be potent elastase inhibitors and therefore are useful anti-inflammatory agents.

Thienamycin derivatives as anti-inflammatory agents

The invention concerns novel 2-aryl-1,2-benzisothiazolinone-1,1-dioxide compounds; methods for their preparation; pharmaceutical compositions containing them as an active ingredient; and methods of selectively inhibiting proteases, especially elastase, and of treating emphysema, rheumatoid arthritis, and various inflammatory diseases, for example, bronchial inflammation.

2-Pyridyl-1,2-benzisothiazolinone-1,1-dioxides and their use as

The invention concerns novel 2-aryl-1,2-benzisothiazolinone-1,1-dioxide compounds; methods for their preparation; pharmaceutical compositions containing them as an active ingredient; and methods of inhibiting proteases, especially elastase, and of treating emphysema, rheumatoid arthritis, and various inflammatory diseases, for example, bronchial inflammation.

2-Aryl-1,2-benzisothiazolinone-1,1-dioxides and their use as selective

Certain novel acyl saccharins and acyl 3-oxo-1,2-benzisothiazolines, their preparation, pharmaceutical compositions and novel methods of inhibiting elatase and treating emphysema are disclosed.

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Watchung, NJ, United States of America

Morris Zimmerman