Sanofi

Elf Sanofi

Bernard Christophe

Gerard Valette

Loic Foulon

Alain Pellet

Claudine Serradeil-Le Gal

Claudine Serradeil-Le-Gal

The subject of the invention is the compounds of formula I ##STR1## in which Ar.sub.1 represents naphtyl, phenyl, quinolyl or isoquinolyl optionally substituted;

Compounds bearing sulphamoyl and amidino radicals, their preparation

A compound of formula I ##STR1## in which Ar.sub.1 is naphthyl and phenyl, quinolyl or isoquinolyl optionally substituted; Ar.sub.2 is phenyl or thienyl optionally substituted; R.sub.1, R.sub.2 and R'.sub.2 are independently of each other H or (C.sub.1 -C.sub.4)alkyl or R.sub.1 represents a bond and N is covalently bonded to Ar.sub.2, and optionally R.sub.2 and R'.sub.2 form a double bond, or R.sub.1 or R.sub.2 is covalently bonded to Ar.sub.2 and represents a (C.sub.1 -C.sub.3 )alkylene; R.sub.3 and R.sub.4 are independently of each other H or (C.sub.1 -C.sub.4)alkyl or form, with the nitrogen atom to which they are attached pyrrolidine, ppiperidine, or hexahydroazepine; Z.sub.1 represents (C.sub.1 -C.sub.12)alkylene, optionally interrupted by a radical selected from the group consisting of (C.sub.5 -C.sub.7)cycloalkyl and phenyl or substituted with a radical selected from the group consisting of (C.sub.5 -C.sub.7)cycloalkyl and phenyl; Q.sub.1 is selected from the group consisting of methyl, amino, (C.sub.1 -C.sub.4)alkoxycarbonylamino, (C.sub.1 -C.sub.4)alkylamino, di(C.sub.1 -C.sub.4)-alkylamino, pyrrolidinyl, piperidino, morpholino, piperazinyl, 4-(C.sub.1 -C.sub.4)alkylpiperazinyl, amidino, (C.sub.1 -C.sub.4)-alkylamidino, guanidino, (C.sub.1 -C.sub.4)alkylguanidino, pyridyl, imidazolyl, pyrimidinyl, indolyl, hydroxy,(C.sub.1 -C.sub.4)alkoxy,(C.sub.2 -C.sub.8)alkoxycarbonyl,N-�amino(C.sub.1 -C.sub.4)alkyl!-N-�(C.sub.1 -C.sub.4)alkyl!amino, carbamoyl, phenyl and phenyl substituted by a radical selected from the group consisting of Cl, F, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy and hydroxyle; Q.sub.2 is selected from the group consisting of H and (C.sub.1 -C.sub.4)alkyl; Q.sub.3 is selected from the group consisting of H and (C.sub.1 -C.sub.4)alkyl or Q.sub.1 and Q.sub.3 are attached to form a heterocycle and together represent (C.sub.2 -C.sub.3)alkylene, whereas Z.sub.1 represents a bond, in the form of pure enantiomer or mixture thereof in any proportions as well as its salt with acid.

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Grand Rosiere, Belgium

Bernard Christophe