Ire-celltarg S.a.

Philippe Pirson

Jean-Bernard Falmagne

Philippe Teyssie

Robert Jerome

Andre B Trouet

Jose Bontemps

Luc Delattre

The invention relates to new quinoline derivatives containing a free amine group and having antimalarial properties, in particular new primaquine derivatives or their addition salts with acids, and to a method for preparing them. According to the invention, these new derivatives are represented schematically by the formula:

New compounds which are active against the tissue forms of malaria and

The present invention relates to microparticles containing an active principle against malaria, such as primaquine, one of its amino acid derivatives, or their conjugates with a hepatotropic vector or their pharmaceutically acceptable salts, and a biocompatible and biodegradable polymer controlling the kinetics of release of the active principle, like (DL)polylactide. The invention also relates to pharmaceutical compositions comprising microcapsules according to the invention. Lastly, the invention relates to processes for the preparation of microparticles as mentioned above, the processes comprising: dissolving the polymer in a volatile solvent, adding to this solution the active principle and possibly a substance regulating the size of the microparticles, and at the end of evaporation, recovering the microparticles by centrifugation and filtration.

Microparticles comprising a biodegradable polymer controlling the

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Wezembeek-Oppem, Belgium

Philippe Pirson