New n-acylated 4-hydroxyphenylamine derivatives with...

C - Chemistry – Metallurgy – 07 – D

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C07D 275/06 (2006.01) A61K 31/425 (2006.01)

Patent

CA 2218664

The present invention relates to a series of new N-acylated 4-hydroxyphenylamine derivatives, linked via an alkylene bridge to the nitrogen atom of a l,2-benzisothiazol-3(2H)-one 1,1-dioxide group, of formula (I), in which n is a number from I to 5, and to processes for preparing these derivatives and to pharmaceutical compositions containing said derivatives; these compounds possess high analgesic activity free from antipyretic activity, and they display little hepatotoxic effect.

La présente invention concerne une série de nouveaux dérivés de 4-hydroxyphénylamine N-acylés, lesquels sont liés par l'intermédiaire d'un pont alkylène à l'atome d'azote d'un groupe 1,2-benzisothiazol-3(2H)-one 1,1-dioxyde, et correspondent à la formule (I) où n est un nombre choisi entre 1 et 5. Cette invention concerne également des processus de préparation de ces dérivés ainsi que des compositions pharmaceutiques contenant ces derniers. Ces composés possèdent une activité analgésique importante, aucune activité antipyrétique, et n'ont que des effets hépatotoxiques limités.

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