Conjugates of a polypeptide and a pentasaccharide

Details Conjugates of a polypeptide and a pentasaccharide Conjugates of a polypeptide and a pentasaccharide

C - Chemistry, Metallurgy

07

K

C07K 17/10 (2006.01) A61K 47/48 (2006.01) C07K 14/47 (2006.01) C07K 14/55 (2006.01) C07K 14/575 (2006.01) C07K 14/585 (2006.01) C07K 14/605 (2006.01) C07K 14/62 (2006.01) C07K 14/655 (2006.01) C07K 9/00 (2006.01)

Patent

CA 2594970

The present invention relates to conjugates of a polypeptide and an oligosaccharide, wherein the polypeptide is conjugated to at least one oligosaccharide-spacer residue, the oligosaccharide being a synthetic sulfated oligosaccharide comprising 4-18 monosaccharide units and per se having affinity to antithrombin III and the spacer being a bond or an essentially pharmacologically inactive flexible linking residue, or a pharmaceutically acceptable salt thereof. The conjugates of the invention have improved pharmacokinetic properties when compared to the original polypeptides (i.e. the corresponding non-conjugated polypeptides per se).

L'invention porte sur des conjugués d'un polypeptide et d'un oligosaccharide, ce polypeptide étant conjugué à au moins un résidu d'un oligosaccharide-espaceur, cet oligosaccharide étant un oligosaccharide sulfaté synthétique contenant 4-18 unités de monosaccharide et présentant per se une affinité avec antithrombine III et l'espaceur étant une liaison ou un résidu de liaison flexible essentiellement inactif d'un point de vue pharmacologique, ou un sel de celui-ci pharmaceutiquement acceptable. Les conjugués de l'invention présentent des propriétés pharmacocinétiques améliorées en comparaison avec les polypeptides originaux (i.e. les polypeptides per non conjugués correspondants).

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