Polymeric derivatives of camptothecins

Details Polymeric derivatives of camptothecins Polymeric derivatives of camptothecins

A - Human Necessities

61

K

A61K 47/48 (2006.01)

Patent

CA 2303097

Water soluble polymeric conjugates of camptothecin comprise N-(2- hydroxypropyl)methacryloylamide units linked via a spacer of the formula -Gly- (CH2)n-CO-Gly wherein n = 2-8 to the C-20 position of a camptothecin residue. The conjugates possess enhanced antitumor activity and decreased toxicity with respect to the free drug. A process for their preparation and pharmaceutical compositions containing them are also described.

Des conjugués polymères hydrosolubles de camptothécine comprennent des unités N-(2-hydroxypropyl)méthacryloylamide liées par un élément d'espacement de la formule -Gly-(CH¿2?)¿n?-CO-Gly dans laquelle n = 2-8 à la position C-20 d'un reste de camptothécine. Les conjugués possèdent une activité antitumorale accrue et une toxicité réduite par rapport au médicament libre. Un procédé de préparation desdits conjugués ainsi que des compositions pharmaceutiques les contenant sont également décrits.

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