Derivatives of polyene macrolides and preparation and use...

A - Human Necessities – 61 – K

Patent

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A61K 31/70 (2006.01) C07H 17/08 (2006.01)

Patent

CA 2394833

The present invention provides a new class of polyene macrolide derivatives useful for treating or preventing fungal infections. The new polyene macrolide derivatives exhibit surprisingly superior antifungal activity and water solubility compared to amphotericin B methyl ester (AME). In addition, the new polyene macrolide derivatives have improved water solubility and lower toxicity than both amphotericin B (AmB) and AME.

La présente invention concerne une nouvelle classe de dérivés de macrolides de polyène s'utilisant dans le traitement ou la prévention d'infections fongiques. Ces nouveaux dérivés de macrolides de polyène présentent une activité antifongique et une solubilité dans l'eau nettement supérieures à celles de l'ester méthylique d'amphotéricine B (AME). En outre, ces nouveaux dérivés de macrolides de polyène présentent une meilleure solubilité dans l'eau et une moindre toxicité, aussi bien par rapport à l'amphotéricine B (AmB) que l'AME.

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