Procedure for the synthesis of glycosaminoglycan (GAG) conjugates with biologically active molecules, polymer conjugates and their relative uses
2010
A method for the synthesis of glycosaminoglycan (GAG) conjugates with biologically active molecules, comprising the following phases: a) the formation of GAG derivatives with at least one aldehyde group (CHO), by the reaction of GAG with a spacer molecule (SP), wherein said spacer molecule comprises, as the first functional group, one or more aldehyde groups (SP-CHO), said aldehyde groups (SP- (CHO)) being optionally protected and, as the second functional group, a nucleophilic group suitable for conjugation with the GAG; a1) hydrolysis of the activated intermediate with aqueous acids when said one or more aldehyde groups are protected; b) reaction of the adduct obtained in phase a) or a1) with at least one biologically active molecule (TA), characterized in that said biologically active molecule (TA) comprises a functional group capable of reacting with the aldehyde group and is selected from the group consisting of polypeptides and proteins, nucleic acids and therapeutic agents that contain at least one amine group not essential for biological functioning, said therapeutic agent being selected from the group consisting of antitumor drugs; antiviral agents and antibiotics; protease and polymerase inhibitors; anti-inflammatory drugs, analgesics, anesthetics, against pain; narcotics; steroids; minoxidil
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