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Claims for Patent: 4,303,651

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Claims for Patent: 4,303,651

Title: Heparin fragments having selective anticoagulation activity
Abstract:Heparin fragments having selective anticoagulation activity having 14-18 sugar units, the disaccharide unit L-iduronosyl-2-O-sulphate-N-sulpho-U-glucosamine-6-O-sulphate being the main component, and where unsulphated L-iduronic acid is in a position situated 3-5 sugar units from the unreducing terminal. Pharmaceutical compositions containing such heparin fragments. Processes for the preparation of the heparin fragments.
Inventor(s): Lindahl; Ulf P. F. (Uppsala, SE), Backstrom; Gudrun E. (Alunda, SE), Thunberg; John Y. L. (Uppsala, SE), Fransson; Lars-Ake (Lund, SE), Andersson; Lars-Olov (Knivsta, SE), Holmer; Erik Y. (Bromma, SE), Sandberg; Inga H. (Sollentuna, SE), Soderstrom; Ewa G. (Saltsjobaden, SE)
Assignee: Kabi AB (Stockholm, SE)
Application Number:06/109,936
Patent Claims: 1. Heparin fragments having 14-18 sugar units, wherein the main component is the disaccharide unit L-iduronosyl-2-O-sulphate-N-sulpho-D-glucosamine-6-O-sulphate, and where unsulphated L-iduronic acid is in a position situated 3-5 sugar units from the unreducing terminal and is followed by a unit selected from the group consisting of N-sulpho-D-glucosamine sulphate and N-acetyl-glucosamine in sulphated and unsulphated form.

2. Heparin fragments having the structure (U-G).sub.n -I-G-(U-G).sub.m where n is 1 or 2 and m is 5 or 6, I is unsulphated L-iduronic acid, U is L-iduronic acid-2-O-sulphate, and G is N-sulpho-D-glucosamine-6-O-sulphate.

3. Pharmaceutical compositions for preventative treatment or treatment of arterial thrombosis containing heparin fragments having selective anticoagulation activity and containing 14-18 sugar units, wherein the main component is the disaccharide unit L-iduronosyl-2-O-sulphate-N-sulpho-D-glucosamine-6-O-sulphate, and where unsulphated L-iduronic acid is in a position situated 3-5 sugar units from the unreducing terminal and is followed by a unit selected from the group consisting of N-sulpho-D-glucosamine sulphate and N-acetyl-glucosamine in sulphated and unsulphated form in an amount sufficient for anticoagulation activity; and a pharmaceutical carrier.

4. Pharmaceutical composition for preventative treatment or treatment of arterial thrombosis containing heparin fragments of the structure (U-G).sub.n -I-G-(U-G).sub.m where n is 1 or 2 and m is 5 or 6, I is unsulphated L-iduronic acid, U is L-iduronic acid-2-O-sulphate and G is N-sulpho-D-glucosamine-6-O-sulphate in an amount sufficient for anticoagulation activity; and a pharmaceutical carrier.

5. The composition of claim 3 or 4 wherein said carrier is water.

6. The composition of claim 3 or 4 which is in the form of an ointment.
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