Dual molecules containing peroxy derivative, the synthesis...

Details Dual molecules containing peroxy derivative, the synthesis... Dual molecules containing peroxy derivative, the synthesis...

C - Chemistry, Metallurgy

07

D

C07D 491/10 (2006.01) A61K 31/47 (2006.01) A61P 33/06 (2006.01)

Patent

CA 2545491

The invention relates to dual molecules of formula (I), wherein A is an antimalarial molecule residue and/or a bioavailability facilitating residue, p, p', p'' are 0 or 1 independent from each other, at least one of p or p'' being equal to 1, identical or different Y¿1? and Y¿2? are an alkylene chain possibly containing one or several amine, amide, thioamide, sulfonyl, sulfonate, sulphonamide, carbonyl, thiocarbonyl, carboxyl, thiocarboxyl, ether or thioether radicals, U is an amine, amide, thioamide, sulfonyl, sulfonate, sulphonamide, carbonyl, thiocarbonyl, carboxyl, thiocarboxyl, ether or thioether radical,¿ ?Z¿1? and¿ ?Z¿2? represent a alkylene radical or Z¿1?+Z¿2 ?represent a polycyclic structure,¿?R ¿x? and R¿y? form together a cyclic peroxide comprising from 4 to 8 chain links and contain 1 or 2 additional oxygen atoms in the cyclic structure. A method for producing and using the inventive dual molecules in the form of antimalarial drugs is also disclosed.

L'invention concerne des molécules duales répondant à la formule (I) : dans laquelle - A représente un résidu de molécule à activité antipaludique et/ou un résidu facilitant la biodisponibilité, - p, p', p" représentent indépendamment les uns des autres 0 ou 1, l'un au moins de p ou de p" étant égal à 1, - Y1 et Y2, identiques ou différents, représentent une chaîne alkylène comportant éventuellement un ou plusieurs radicaux amine, amide, thioamide, sulfonyle, sulfonate, sulfonamide, carbonyle, thiocarbonyle, carboxyle, thiocarboxyle, éther ou thioéther, - U représente un radical amine, amide, thioamide, sulfonyle, sulfonate, sulfonamide, carbonyle, thiocarbonyle, carboxyle, thiocarboxyle, éther ou thioéther, - Z1, et Z2 représentent un radical alkylène, ou l'ensemble Z1 + Z2 représente une structure polycyclique, - RX et Ry forment ensemble un peroxyde cyclique comprenant de 4 à 8 chaînons et comportant 1 ou 2 atomes d'oxygène supplémentaires dans la structure cyclique. Procédé de préparation et application en tant que médicaments à activité antipaludique.

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