Rifamycin derivatives for treating microbial infections

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 498/08 (2006.01) A61K 31/4709 (2006.01) A61P 31/04 (2006.01)

Patent

CA 2574307

Novel rifamycin derivatives of formula (I) (both hydroquinone and corresponding quinone (C1-C4) forms), or their salts, hydrates or prodrugs thereof, wherein: a preferred R comprises hydrogen, acetyl; L is a linker, a preferred linker group elements selected from any combination of 1 to 5 groups shown, provided L is not formula (A), wherein R1 is H, methyl or alkyl. The inventive compounds exhibit valuable antibiotic properties. Formulations having these compounds can be used in the control or prevention of infectious diseases in mammals, both humans and non-humans. In particular, the compounds exhibit a pronounced antibacterial activity, even against multiresistant strains of microbes.

L'invention concerne de nouveaux dérivés de rifamycine de formule (I) (formes d'hydroquinone et de quinone (C1-C4) correspondante): (I), ou bien leurs sels, leurs hydrates ou leurs promédicaments, formule dans laquelle R comprend de préférence hydrogène et acétyle, L est un élément de liaison, un élément de groupe de liaison préféré sélectionné dans une combinaison quelconque de 1 à 5 groupes présentés en figure (1), dans la mesure où L n'est pas de formule (A), où R1 désigne H, méthyle ou alkyle. Les composés de l'invention ont des propriétés antibiotiques intéressantes. Des formulations contenant ces composés peuvent servir pour lutter contre des maladies infectieuses ou les prévenir chez les mammifères humains et animaux. Lesdits composés ont en particulier une activité antibactérienne prononcée, même contre des souches de microbes multirésistantes.

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