Pradimicin derivatives

C - Chemistry – Metallurgy – 07 – H

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C07H 15/252 (2006.01) C07C 235/84 (2006.01) C07H 15/244 (2006.01)

Patent

CA 2030166

Disclosed are neutral sugar derivatives of pradimicins (BU-3608 antibiotics), their use as antifungal agents, methods for their preparation and intermediates for their synthesis. Said derivatives include a compound having the formula (see fig.I) wherein R1 is selected from the group consisting of H and hydroxymethyl, and when R1 is hydroxymethyl, the resulting amino acid residue has the D-configuration; and R2 is H or .beta.-D-xylosyl or a pharmaceutically acceptable salt thereof.

L'invention porte sur des dérivés de sucre neutre des pradimicines (antibiotiques BU-3608), leur utilisation comme agents antifongiques, les méthodes de préparation et les intermédiaires de synthèse. Lesdits dérivés comprennent un composé de formule (voir fig.I) où R1 est choisi dans un groupe constitué de H et d'un groupe hydroxyméthyle, et lorsque R1 est un hydroxyméthyle, le résidu d'acide aminé produit possède la configuration D; et R2 est H ou un groupe bêta-D-xylosyle ou un sel pharmaceutiquement acceptable de ce dernier.

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