HIGH-MOLECULAR WEIGHT CAMPTOTECINE DERIVATIVES Russian patent published in 2008 - IPC C08G81/00 C08F8/14 C08F8/30 A61K31/4745 A61K31/4748 A61P35/00 A61P43/00 

Abstract RU 2315782 C2

FIELD: pharmaceutical chemistry.

SUBSTANCE: invention provides water-soluble camptotecine derivatives showing excellent therapeutical activity and retarded release suitable for cancer chemotherapy. High-molecular weight camptotecine derivative has structure wherein carboxylic acid group of block copolymer of polyethylene glycol and polymer containing carboxylic acid group in side chain and being acidic amino acid polymer is linked to phenol hydroxyl group of phenolic camptotecines through ester linkage. Also claimed is high-molecular weight camptotecine derivative of general formula (I): . Preparation method comprises combining carboxylic acid group of above-defined block copolymer with phenol hydroxyl group of phenolic camptotecines through ester linkage in presence of condensation agent. Anticancer drug includes above-defined camptotecine derivative and optionally pharmaceutically acceptable carrier.

EFFECT: augmented choice of anticancer drugs.

9 cl, 2 dwg, 2 tbl, 5 ex

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RU 2 315 782 C2

Authors

Kitagava Masajuki

Okamoto Kazuja

Dates

2008-01-27Published

2003-10-29Filed