Anthracycline-conjugates

C - Chemistry – Metallurgy – 07 – H

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C07H 15/252 (2006.01) A61K 47/48 (2006.01)

Patent

CA 2075288

A conjugate of formula (1); wherein the moiety A-O- is the residue of any anthracycline of formula A-O-H bearing at least one primary or secondary hydroxyl group; a is an integer of from 1 to 30; W is a residue of formula (2), wherein B represents a C1-C6 alkylene group optionally hetero interrupted and m is 0 or 1; Z is a spacer group and T is a carrier moiety. The conjugates of formula (1) of the present invention are useful antitumor agents since they contain an acetalic bond which releases the parent drug A-O-H upon hydronium-ion-catalyzed hydrolysis or "in vivo" enzymatic cleavage.

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