Seikagaku Corporation

Yutaka Kariya

Saburo Hara

Junichi Onaya

Seigou Usuki

Yusuke Hori

Kaeko Kamei

Ryo Takano

The invention provides novel glycosaminoglycan derivatives having a repeating unit structure of two saccharides of hexosamine and hexuronic acid as a backbone structure, in which the bonds between 2- and 3-positions carbon atoms of hexuronic acid as its constituting monosaccharide are partially cleaved and a part or all of the 2-position hydroxyl groups of uncleaved hexuronic acid are not substituted with a sulfate group, which has low anticoagulation activity and excellent neurite outgrowth promotion accelerating activity and sialidase inhibition activity; a process for producing the glycosaminoglycan derivatives, comprising a cleavage treatment of the bond between the 2- and 3-position carbon atoms of hexuronic acid having no sulfate group at the 2-position of glycosaminoglycan, and a selective desulfation treatment of the 2-position sulfate group of hexuronic acid; and a pharmaceutical composition comprising the glycosaminoglycan derivative as an active ingredient.

Glycosaminoglycan derivatives and processes for preparing same

There is provided a glycosaminoglycan having a backbone structure comprising a repetitive disaccharide bearing a uronic acid residue and a glucosamine residue, and having sulfate groups, wherein substantially no sulfate group bound to the hydroxyl group at the 6-position of the glucosamine residue in the backbone structure is detected as determined by a chemical disaccharide analysis method in which the glycosaminoglycan is decomposed with nitrous acid, reacted with para-nitrophenylhydrazine and analyzed by high performance liquid chromatography, and the molar % of a uronic acid residue having a sulfate group at the 2-position is not less than 45% relative to total uronic acid residues, which is calculated from a disaccharide composition obtained by an enzymatic disaccharide analysis method in which the glycosaminoglycan is digested with glycosaminoglycan-degrading enzymes and analyzed by high performance liquid chromatography. The glycosaminoglycan can be used as an active ingredient of pharmaceuticals.

Glycosaminoglycan and drug compositions containing the same

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Kanagawa, Japan

Yutaka Kariya