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AssigneeFresenius Kabi Deutschland GmbH
InventorsMichele Orlando, Jurgen Hemberger
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The invention relates to a method for coupling low-molecular weight substances to a starch-derived modified polysaccharide. The binding interaction between the modified polysaccharide and the low-molecular weight substance is based on a covalent bond which is the result of a coupling reaction between the terminal aldehyde group or a functional group of the modified polysaccharide molecule resulting from the chemical reaction of this aldehyde group and a functional group of the low-molecular weight substance which reacts with this aldehyde group or with the resulting functional group of the polysaccharide molecule. The bond directly resulting from the coupling reaction can be optionally modified by a further reaction to the aforementioned covalent bond. The invention further relates to pharmaceutical compositions that comprise conjugates formed in this coupling process and to the use of said conjugates and compositions for the prophylaxis or therapy of the human or animal body.
1-36. (canceled)
A conjugate of hydroxyalkylstarch and a low molecular weight substance, characterized in that the binding interaction between the hydroxyalkylstarch molecule and the low molecular weight substance is based on a covalent bonding which is the result of a coupling reaction between (i) the terminal aldehyde group, or a functional group derived from this aldehyde group by chemical reaction, of the hydroxyalkylstarch molecule and (ii) a functional group, which is able to react with this aldehyde group or functional group derived therefrom of the hydroxyalkylstarch molecule, of the low molecular weight substance, where the bonding resulting directly in the coupling reaction can be modified where appropriate by a further reaction to give the abovementioned covalent bonding.
A method for preparing hydroxyalkylstarch which is selectively oxidized at the terminal aldehyde group, characterized in that the hydroxyalkylstarch is reacted in a molar ratio of iodine to HAS of 2:1 to 20:1 in basic aqueous solution.
A method for preparing hydroxyalkylstarch which is selectively oxidized at the terminal aldehyde group, characterized in that the HAS is oxidized in aqueous alkaline solution with a molar excess of stabilized metal ions selected from Cu2+ ions and Ag+ ions.
A conjugate of hydroxyalkylstarch and a low molecular weight substance, wherein the binding interaction between the hydroxyalkylstarch molecule and the low molecular weight substance comprises at least one covalent bond between:
Dependencies are inferred from the claim text.