Conjugates of hydroxyalkyl starch and an active substance,...

A - Human Necessities – 61 – K

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A61K 47/48 (2006.01) C08B 31/00 (2006.01)

Patent

CA 2619036

The present invention relates to a method for preparing conjugates of an active substance and hydroxy alkyl starch and to conjugates of an active substance and hydroxyalkyl starch, preferably hydroxy ethyl starch, wherein the conjugates are prepared by covalently linking the hydroxyalkyl starch and the active substance by a chemical residue having a structure according to formula (I) (I~) (I~~) wherein R1, R2, R2~, R3, R3~and R4 are independently selected from the group consisting of hydrogen, an optionally suitably substituted, linear, cyclic and/or branched alkyl, aryl, heteroaryl, aralkyl, and heteroaralkyl group, preferably hydrogen.

Cette invention concerne un procédé permettant de préparer des conjugués d'une substance active et d'amidon hydroxyalkyle. Cette invention concerne également des conjugués d'une substance active et d'amidon hydroxyalkyle, de préférence, de l'amidon hydroxyéthyle. De préférence, ces conjugués sont préparés par liaison par covalences de l'amidon hydroxyalkyle et de la substance active par l'intermédiaire d'un reste chimique présentant une structure représentée par la formule (I) (I') (I''), dans cette formule R1, R2, R2', R3, R3' et R4 sont indépendamment les uns des autres choisis dans le groupe comprenant l'hydrogène, un groupe hétéroaralkyle, alkyle, aryle, hétéroaryle, aralkyle ramifié et/ou cyclique, linéaire éventuellement substitué de manière adéquate, de préférence, l'hydrogène.

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