Heparin derivatives and process for the preparation thereof

C - Chemistry – Metallurgy – 08 – B

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C08B 37/10 (2006.01) A61K 31/725 (1990.01)

Patent

CA 2084301

The invention relates to new heparin derivatives from bovine or porcine heparin which have a molecular weight equal to or larger than the standard heparin, show a sulfur content which is equal to or higher than that of the starting heparin or at least 13 % w/w, have an anticoagulant activity in the anti-PXa assay of less than 10 % of the standard heparin it was made from, show a ratio of APTT activity over anti-FXa activity of 3-35; show a reduced prolongation of bleeding time compared to the standard heparin it was made from as measured in the rat tail after i.v. administration and show enhancement of the rate of development of coronary collaterals in dogs equal to or better than clinically used heparin. The invention also relates to processes for preparation of the new bovine and porcine heparin derivatives. The use of this product for the manufacturing of a medicament for treatment of ischemic heart disease and related vascular disorders and for the enhancement of the rate of development of coronary collateral perfusion is disclosed.

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