Water-soluble esters of camptothecin compounds

C - Chemistry – Metallurgy – 07 – D

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C07D 491/22 (2006.01) A61K 31/4738 (2006.01)

Patent

CA 2195428

Non-toxic camptothecin prodrugs are prepared by esterifying the 20-position hydroxyl group of camptothecin derivatives to form a camptothecin compound in which the E-ring has the formula: (see formula I and II) wherein m = 1-6, R9 is the side chain of one of the naturally occurring a- amino acids, R10 and R11 are, independently, hydrogen or C1-8 alkyl, with the proviso that the camptothecin compound is different from camptothecin or camptothecin substituted on the A-ring thereof with an alkyl group or with a substituted alkyl group, said alkyl group or substituted alkyl group corresponding to the side chain in natural amino acids.

Des promédicaments non toxiques à la camptothécine sont préparés par estérification du groupe hydroxyle en position 20 de dérivés de camptothécine.

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