Italfarmaco Spa

Great Lakes Chemical (europe) Gmbh

Flavio Somenzi

Carlo Neri

Paolo Mascagni

Giorgio Bertolini

Fabio Broussard

Flavio Leoni

Mauro Biffi

Jacques Mizrahi

Maria Letizia Marchetti

Process for the preparation of symmetrical diacylhydrazines having general formula (I): R &mdash;CO&mdash;NH&mdash;NH&mdash;CO&mdash;R wherein R represents a linear or branched C -C alkyl group; a linear or branched C -C alkoxyalkyl group; a C -C cyanoalkyl group; a C -C cycloalkyl group, said cycloalkyl group optionally containing a heteroatom selected from oxygen, nitrogen and sulfur; a C -C aryl group; a C C arylalkyl group or alkylaryl group, said arylalkyl or alkylaryl groups optionally substituted with one or more hydroxyl groups, or with one or more linear or branched C alkoxyl groups; comprising: (a) reacting an ester of a carboxylic acid having general formula (II): R &mdash;CO&mdash;OR wherein R has the same meanings defined above and R represents a linear or branched C -C alkyl group, with hydrazine, in its pure or hydrated state, obtaining a monoacylhydrazine having general formula (III): R &mdash;CO&mdash;NH&mdash;NH ; (b) reacting the monoacylhydrazine having general formula (III) obtained in step (a), with a &bgr;-ketoester having general formula (IV): R &mdash;CO&mdash;CH &mdash;COOR wherein R represents a linear or branched C -C alkyl group, or a C -C aryl group and R represents a linear or branched C -C alkyl group, obtaining the desired symmetrical diacylhydrazine having general formula (I).

Process for the preparation of symmetrical diacylhydrazines

Analogues of the active metabolite of leflunomide, and to the use thereof as immunosuppressive and/or antinflammatory agents.

Analogues of the active metabolite of leflunomide

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Cinisello Balsamo, Italy

Flavio Somenzi