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EP0014184A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Heparin fragments having a selective anticoagulation activity and process for their preparation

Assignee: Pfizer Health AB
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Filing: 1980-01-07
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Granted: —
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Expires: 2000-01-07
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Abstract

Abstract Heparin fragments having selective anticoagulation activity having 14-18 sugar units, the disaccharide unit L-induronosyl-2-O-sulphate-N-sulpho-U-glucosamine-6-O-sulphate being the main component, and where unsulphated L-induronic 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.

Inventors

  • 👤 Ulf Per Fredrik Lindahl
  • 👤 Gudrun Elisabet Bäckström
  • 👤 John Yngve Lennart Thunberg
  • 👤 Lars-Ake Fransson
  • 👤 Lars-Olov Andersson
  • 👤 Erik Yngve Holmer
  • 👤 Inga Helena Sandberg
  • 👤 Ewa Gunilla Söderström

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-23 19:52
CPC Classifications
C; C08; C08B; C08B37/00; C08B37/006; C08B37/0063; C08B37/0075; C08B37/0078; A; A61; A61P; A61P7/00; A61P7/02

Claims Analysis

Total Claims: 9
Claim 1
Independent Claim 45 words
Heparin fragments, characterised by 14-18 sugar units, the disaccharide unit L-iduronosyl-2-O-sulphate-N-sulpho-D-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 and is followed by N-sulpho-D-glucosamine sulphate or N-acetyl-glucosamine in sulphated or unsulphated form.
Claim 2
Dependent Claim 45 words
Heparin fragments, characterised by 14-18 sugar units, the disaccharide unit L-iduronosyl-2-O-sulphate-N-sulpho-D-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 and is followed by N-sulpho-D-glucosamine sulphate or N-acetyl-glucosamine in sulphated or unsulphated form.
Claim 3
Dependent Claim 35 words
Heparin fragments, characterised by the structure (U-G) n -I-G-(U-G) 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.
Claim 4
Dependent Claim 35 words
Heparin fragments, characterised by the structure (U-G) n -I-G-(U-G) 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.
Claim 5
Dependent Claim 56 words
Pharmaceutical compositions, characterised in that they comprise heparin fragments having selective anticoagulation activity and containing 14-18 sugar units, the disaccharide unit L-iduronosyl-2-0-sulphate-N-sulpho-D-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 and is followed by N-sulpho-D-glucosamine sulphate or N-acetyl-glucosamine in sulphated or unsulphated form.
Claim 6
Dependent Claim 56 words
Pharmaceutical compositions, characterised in that they comprise heparin fragments having selective anticoagulation activity and containing 14-18 sugar units, the disaccharide unit L-iduronosyl-2-0-sulphate-N-sulpho-D-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 and is followed by N-sulpho-D-glucosamine sulphate or N-acetyl-glucosamine in sulphated or unsulphated form.
Claim 7
Dependent Claim 41 words
Pharmaceutical compositions, characterised in that they contain heparin fragments of the structure (U-G) n -I-G-(U-G) 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.
Claim 8
Dependent Claim 41 words
Pharmaceutical compositions, characterised in that they contain heparin fragments of the structure (U-G) n -I-G-(U-G) 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.
Claim 9
Dependent Claim 80 words
A process for the preparation of heparin fragments according to claim 1, characterised by (a) treating heparin with nitrous acid in dimethoxyethane and purifying the material obtained, or (b) periodate-oxidising heparin at low pH and temperature, respectively, or (c) partially depolymerising heparin with heparinase, or (d) partially depolymerising heparin by esterification of carboxyl groups and then subjecting the material obtained to alkaline β-elimination, or (e) partially depolymerising heparin from partial N-desulphatation and then deaminating the material obtained with nitrous acid.

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