Camptothecin derivatives and polymeric conjugates thereof

Details Camptothecin derivatives and polymeric conjugates thereof Camptothecin derivatives and polymeric conjugates thereof

C - Chemistry, Metallurgy

07

D

C07D 491/22 (2006.01) A61K 31/4745 (2006.01) A61K 47/48 (2006.01) B32B 27/32 (2006.01) C07D 471/04 (2006.01) C07D 471/14 (2006.01) C07D 519/00 (2006.01) C07K 4/00 (2006.01)

Patent

CA 2485006

Polymeric conjugates of camptothecin derivatives having increased circulating half-lives are disclosed. In preferred aspects, the E ring lactone of the camptothecin derivatives is opened and funtionalzed to allow attachment of a polymer such as PEG in the 17-or 20-position thereof. A representative example of such compound is (I) methods of preparing and using the same are also disclosed.

La présente invention concerne des conjugués polymères de dérivés de camptothécine présentant des demi-vies de circulation accrues. Selon des modes de réalisation préférés, la lactone à anneau E des dérivés de camptothécine est ouverte et fonctionnalisée pour permettre la fixation d'un polymère tel que de PEG au niveau de sa position 17 ou 20. La formule (I) constitue un exemple représentatif de tels composés. L'invention concerne également des méthodes de préparation et d'utilisation desdits conjugués.

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