Merck + Co., Inc.

Robert L Clark

Tsung-Ying Shen

Arsenio A Pessolano

Howard Jones

Bruce E Witzel

Thomas J Lanza, Jr

Morris Zimmerman

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

1,3-Dihydroimidazo[4,5-b]pyridin-2-ones and corresponding thiones have utility as analgesic, antipyretic and antiinflammatory agents. They are generally prepared by treatment of a 2,3-diaminopyridine with phosgene or thiosphosgene followed by further substitution if desired.

Imidazo pyridine-2-ones and pharmaceutical compositions and methods of

The various isomers of oxazolo- and thiazolopyridines having utility as antiinflammatory, antipyretic and analgesic agents are prepared by condensation of an appropriate amino-hydroxypyridine or amino-mercaptopyridine with a carboxylic acid, halide or anhydride.

Anti-inflammatory oxazolo [5,4-b]pyridines

Anti-inflammatory oxazole[4,5-b]pyridines

3H-1,2,3-Triazolo[4,5-b]pyridines substituted in the 3-position have utility as analgesic, anti-inflammatory and anti-pyretic agents. They are prepared by diazotization of a 3-amino-2-(substitute) aminopyridine.

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Woodbridge, NJ, United States of America

Robert L Clark