Mixture of heparin-derived oligosaccharides, useful for treatment or prevention of e.g. thrombosis or cancer, comprises high anti-activated factor X activity but almost no anti-activated factor II activity

摘要

Mixture (A) of oligosaccharides (OS) that have the general structure of polysaccharides that make up heparin, with mean molecular weight 1.8-2.4 kD; anti-Xa activity of 190-450 international units (IU)/mg and (practically) no anti-IIa activity, are new. Mixture (A) of oligosaccharides (OS) that have the general structure of polysaccharides that make up heparin,with mean molecular weight 1.8-2.4 kD; anti-Xa activity 190-450 international units (IU)/mg and (practically) no anti-IIa activity. The OS contain 2-16 sugar residues; have a 4,5-unsaturated uronic acid-2-O-sulfate residue at one end and contain the hexasaccharides (X), as alkali or alkaline earth metal salt. [Image] An independent claim is also included for a method for preparing (A). ACTIVITY : Anticoagulant; Thrombolytic; Antianginal; Cardiant; Vasotropic; Antiarteriosclerotic; Cytostatic; Antidiabetic; Ophthalomological; Nephrotropic. MECHANISM OF ACTION : Inhibition of activated factor X. The hexasaccharide (X) has strong affinity for antithrombin III and anti-Xa activity over 740 IU/mg.