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US4933326A Expired / Lapsed US ⏱️ 0.0 years remaining

Oligosaccharides obtained by heparin depolymerization having antiatherosclerotic activity

Assignee: Opocrin SpA
•
Filing: 1988-09-21
•
Granted: 1990-06-12
•
Expires: 2008-09-21
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Abstract

Abstract Heparin fractions which are a mixture of oligosaccharides containing 6-12 monosaccharides are described. The oligosaccharides contain reducing end groups composed of iduronic acid 2-sulfate or glucosamine N, 6-disulfate. The end group monosaccharides contain the reducing anomeric carbons. The SO 3 - /COO - ratio is essentially the same as in heparin. The method of preparation is a depolymerization initiated by free radicals. One fraction is a heparin fragment with a molecular weight (MWw) of 2,100 daltons (+10%). The compound contains 6-8 monosaccharides, has the same SO 3 - /COO - ratio as the parent heparin and has platelet anti-aggregating activity, arterial and venous antithrombotic action, fibrinolytic and antiatherosclerotic activity. It exhibits poor anti factor Xa activity and no anticoagulant action.

Inventors

  • 👤 Pietro Bianchini
  • 👤 Giuseppe Mascellani

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 15:53
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: 8
Claim 1
Independent Claim 50 words
An heparin fraction of molecular weight 2100-3570 which is a mixture of oligosaccharides containing an average of 6-8 monosaccharides, said oligosaccharides containing end groups composed of iduronic acid 2-sulfate or glucosamine N, 6-disulfate, said end group monosaccharides containing the reducing anomeric carbons, said oligosaccharides being constituted of multiples of monosaccharides.
Claim 2
Dependent Claim 50 words
An heparin fraction of molecular weight 2100-3570 which is a mixture of oligosaccharides containing an average of 6-8 monosaccharides, said oligosaccharides containing end groups composed of iduronic acid 2-sulfate or glucosamine N, 6-disulfate, said end group monosaccharides containing the reducing anomeric carbons, said oligosaccharides being constituted of multiples of monosaccharides.
Claim 3
Dependent Claim 22 words
The heparin fraction according to claim 1 wherein the SO 3 - /COO - ratio is essentially the same as in heparin.
Claim 4
Dependent Claim 22 words
Heparin fraction in accordance with claim 1 having molecular weight 2100-2300 and the same SO 3 - /COO - ratio as heparin.
Claim 5
Dependent Claim 16 words
The heparin fraction according to claim 1 which produces NMR signals at 92.7 and 94.4 ppm.
Claim 6
Dependent Claim 30 words
The heparin fraction according to claim 1 which is free of anticoagulant activity and which exhibits high antithrombotic activity in arterial thrombosis and venous thrombosis and which inhibits platelet aggregation.
Claim 7
Dependent Claim 50 words
A pharmaceutical composition with an antiatherosclerotic activity, anti-platelet aggregation activity and fibrinolytic activity, containing as the active ingredient the heparin fraction according to claim 1 in an amount sufficient to administer a dose of 3-15 mg/Kg daily, and excipients, in the form of capsules, tablets or syrups for oral administration.
Claim 8
Dependent Claim 46 words
A pharmaceutical composition with an antiatherosclerotic activity, anti-platelet aggregation activity and fibrinolytic activity, containing as the active ingredient the heparin fraction according to claim 1 in an amount sufficient to administer 1-5 mg/Kg daily in the form of a sterile solution, suitable for injection and excipients.

References Cited (Backward Citations)

US4500519A Cited
US4303651A Cited
US4351938A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1993-06-11 1993-12-11 1994-06-12 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1997-06-11 1997-12-11 1998-06-12 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2001-06-11 2001-12-11 2002-06-12 $7700.00 Window Closed / Lapsed

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