methods for conjugating a water soluble polymer to an oxidized carbohydrate fraction of a therapeutic protein, to form an oxime bond between an oxidized carbohydrate fraction in a therapeutic protein and an activated water soluble polymer, and to form a hydrazone bond between a oxidized carbohydrate fraction into a therapeutic protein and an activated water-soluble polymer, and modified therapeutic protein

摘要

methods for conjugating a water soluble polymer to an oxidized carbohydrate fraction of a therapeutic protein, to form an oxime bond between an oxidized carbohydrate fraction in a therapeutic protein and an activated water soluble polymer, and to form a hydrazone bond between a oxidized carbohydrate fraction into a therapeutic protein and an activated water-soluble polymer, and modified therapeutic protein. The invention relates to materials and methods of conjugating a water-soluble polymer to materials and methods of conjugating a water-soluble polymer to an oxidized carbohydrate fraction of a water-soluble therapeutic protein to an oxidized carbohydrate fraction of a therapeutic protein comprising contacting the oxidized carbohydrate fraction with a water-soluble polymer activated under conditions that allow conjugation. More specifically, the present invention relates to the aforementioned materials and methods wherein the water soluble polymer contains an active amino oxide group and wherein an oxime or hydrazone bond is formed between the oxidized carbohydrate moiety and the amino oxide group. active in the water-soluble polymer, and in which conjugation is conducted in the presence of a nucleophilic catalyst.