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filingDate 2014-10-22-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2019-06-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2019-06-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-105744940-B
titleOfInvention Carboxylated derivatives of glycosaminoglycans and their use as pharmaceuticals
abstract The present invention relates to glycosaminoglycan derivatives, which have heparanase inhibitory activity and antitumor activity, which have carboxyl groups at positions 2 and 3 of at least some of the glycosaminoglycan residues, and a method for preparing the same. The glycosaminoglycan derivatives of the present invention are produced by two oxidation steps starting from natural or synthetic glycosaminoglycans, preferably heparin or low molecular weight heparin, which are optionally 2-O- and 2N-desulfated. By the first oxidation, the adjacent diol and optionally the adjacent OH/NH of the glycosaminoglycan residue are converted to aldehydes, and by the second oxidation, the dialdehydes are converted to carboxyl groups . Said first oxidation preferably results in cleavage of the C2 - C3 bond of the loop of the oxidizable residue. The present invention also relates to a process for the preparation of said glycosaminoglycan derivatives, and also to their use as active ingredients of medicaments. Furthermore, the present invention relates to pharmaceutical compositions comprising di/tricarboxylated heparin derivatives as active substance.
priorityDate 2013-11-06-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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