Sanofi

Elf Sanofi

Alain Pellet

Gerard Valette

Loic Foulon

Bernard Christophe

Claudine Serradeil-Le Gal

Simon F Campbell

Gilles V Courtemanche

Claudine Serradeil-Le-Gal

Cécile Pascal

Gilles Courtemanche

The present disclosure relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof wherein Rmeans a fluorine atom or a perhalogeno linear alkyl radical containing 1, 2 or 3 carbon atoms; Rmeans a chlorine atom, a linear alkyl radical containing 1, 2 or 3 carbon atoms or a perhalogeno linear alkyl radical containing 1, 2 or 3 carbon atoms, and R means a hydrogen atom or a radical of formula (Ia). The present disclosure also relates to processes for their preparation as well their therapeutic uses, in particular such as for use in the treatment of malaria.

Ethynyl compounds, their preparation and their therapeutic use for the treatment of malaria

The invention relates to the nitrobenzothiazole derivatives of general formula (I): and to the use thereof for treating tuberculosis. 

Nitrobenzothiazole derivatives, preparation thereof and therapeutic applications thereof

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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Ramonville, France

Alain Pellet