Non anti-coagulative glycosaminoglycans comprising repeating disaccharide unit and their medical use

摘要

The present invention relates to a chemically modified glycosaminoglycan with an antifactor II activity of less than 10 IU/mg, an antifactor Xa activity of less than 10 IU/mg and an average molecular weight (Mw, weight average) from about 4.6 to 6.9 kDa. Also disclosed is a method of preparing the modified glycosaminoglycan and its medical uses.

主权项

1. A chemically modified glycosaminoglycan, which glycosaminoglycan is selected from the group consisting of heparin and heparan sulfate, which chemically modified glycosaminoglycan has an antifactor IIa activity and an antifactor Xa activity, with the antifactor IIa activity being less than 10 IU/mg and the antifactor Xa activity being less than 10 IU/mg, the chemically modified glycosaminoglycan having a weight average molecular weight (Mw) from about 4.6 to about 6.9 kDa, and wherein, in the chemically modified glycosaminoglycan:
the polysaccharide chains have from 2 to 20 disaccharide units corresponding to molecular weights between 1.2 and 12 kDa; the polysaccharide chains are essentially free of chemically intact non-sulfated iduronic and/or glucuronic acids from pentasaccharide sequences mediating the anticoagulant effect of heparin and heparin sulfate; the predominantly occurring disaccharide is (Formula I) n is an integer from 2 to 20; and the distribution of molecular weights of the polysaccharides in the chemically modified glycosaminoglycan are expressed as cumulative % of weight according to the following table:Molecular Cumulativemass, kDaweight, %>10 4-15>8 10-25>6 22-45>3 >70.