Synphar Laboratories, Inc.

Taiho Pharmaceutical Company Limited

Paul Spevak

Ronald G Micetich

Samarendra N Maiti

David P Czajkowski

Charles Y Fiakpui

Kazuo Adachi

Inder Pal Singh

Ronald J Micetich

Bhupinder Palak

A V Reddy

Harninder Atwal

Narender A Reddy

Samuel Amedjo

A high purity triazole is obtained by the reaction of a hydrazide of the general formula II and glyoxal followed by the treatment of the intermediate of general formula IV with ammonia. The total process is done in one pot and does not require the isolation of the intermediate IV. The triazole (I) is isolated by distillation. Synthesis of various N.sub.1 -substituted triazoles is also described following the same procedure.

Effective process for the production of 1,2,3-triazoles

This invention relates to 2-[(substituted)methylene]cephalosporin sulfones and in particular 2-[(heteroaryl substituted)methylene]cephalosporin sulfones which are effective elastase inhibitors as well as effective thrombin inhibitors and therefore are useful as anti-inflammatory, anti-degenerative and anti-thrombin agents.

2-[(substituted) methylene]cephalosporin sulfones as antiinflammatory,

Derivatives of 2-spirocyclopropyl cephalosporin sulfone of the structural formula I ##STR1## are provided which are useful as potent elastase inhibitors.

2-spirocyclopropyl cephalosporin sulfone derivatives

Derivatives of 2-spirocyclopropyl 4-acylcephem sulfones of the formula (I) ##STR1## are provided which are useful as potent elastase inhibitors and hence are useful in the prevention, control and treatment of inflammatory conditions, especially arthritis and emphysema.

2-spirocyclopropyl 4-acylcephems

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Edmonton, Canada

Paul Spevak