Bis-anthracyclines with high activity against doxorubicin...

C - Chemistry – Metallurgy – 07 – H

Patent

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C07H 15/252 (2006.01) A61K 31/70 (2006.01) C07H 15/24 (2006.01)

Patent

CA 2249593

The present invention discloses new and novel bis-anthracyclines linked through the C-3' or C-4' saccharide portions. These compounds show high activity against two clinically relevant mechanisms of resistance. A novel approach of the invention produces compounds that are as active or more so than the parent compounds. Furthermore, the inventor's discovery is also for the design of effective DNA-binding bis-anthracyclines as well as anthracyclines mixed with other intercalators and groove binders.

L'invention a pour objet de nouvelles bisanthracyclines liées par les parties saccharides C-3' ou C-4'. Ces composés présentent une forte activité contre deux mécanismes de résistance cliniquement importants. Un nouveau procédé permet de produire des composés qui sont au moins aussi actifs que les composés parents. En outre, l'invention concerne la conception de bisanthracyclines efficaces liant l'ADN et d'anthracyclines mélangées à d'autres intercalants et liants de sillon.

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