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US4533549A Expired / Lapsed US ⏱️ 0.0 years remaining

Antithrombotic agent

Assignee: Individual
•
Filing: 1984-02-17
•
Granted: 1985-08-06
•
Expires: 2004-02-17
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Abstract

Abstract The object of the invention is to provide a new antithrombotic agent. Coagulation of blood acts through a cascade of stages, the mechanisms and interaction of which have not been fully clarified. The present invention provides a derivative of heparin which can be administered orally, topically, or parenterally to antagonize the effect of factor Xa to a greater extent than commercial porcine heparin. In addition, the derivative has insignificant USP anticoagulant and platelet aggregating activities. The heparin derivative according to the invention, has a molecular weight of from about 2,500 to about 4,000 daltons, gives a positive metachromatic test for sulfated polysaccharides. Preferably, when isolated as the sodium salt, the derivative contains by elemental analysis about 26.2% carbon, 4.33% hydrogen, 1.98% nitrogen, 7.1% sulfur, and 9.8% sodium, the molar ratio C:N:S:Na being about 10:1.5:2:4.

Inventors

  • 👤 Sigmund E. Lasker

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 14:51
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/70; A61K31/715; C; C08; C08B; C08B37/00; C08B37/006; C08B37/0063; C08B37/0075

Claims Analysis

Total Claims: 10
Claim 1
Independent Claim 84 words
An antithrombotic agent derived from heparin having an anticoagulant activity of less than 20 USP XVIII units and insignificant platelet aggregating activity, and an anti-activated coagulation factor Xa activity of from about 150 to about 190 units/mg, said agent being a pharmacologically acceptable salt of a mucopolysaccharide soluble in water, insoluble in acetone and ethanol, containing glucosamine, glucuronic acid and iduronic acid, having a weight average molecular weight of from about 2,500 to about 4,000 daltons, giving a positive metachromatic test for sulfated polysaccharides.
Claim 2
Dependent Claim 84 words
An antithrombotic agent derived from heparin having an anticoagulant activity of less than 20 USP XVIII units and insignificant platelet aggregating activity, and an anti-activated coagulation factor Xa activity of from about 150 to about 190 units/mg, said agent being a pharmacologically acceptable salt of a mucopolysaccharide soluble in water, insoluble in acetone and ethanol, containing glucosamine, glucuronic acid and iduronic acid, having a weight average molecular weight of from about 2,500 to about 4,000 daltons, giving a positive metachromatic test for sulfated polysaccharides.
Claim 3
Dependent Claim 17 words
An antithrombotic agent according to claim 1 having an anticoagulant activity of about 13 USP XVIII units.
Claim 4
Dependent Claim 28 words
An antithrombotic agent according to claim 1 which is derived from a member selected from the group consisting of porcine heparin, bovine heparin, heparin residues and marine heparinoids.
Claim 5
Dependent Claim 13 words
An antithrombotic agent according to claim 3 which is derived from porcine heparin.
Claim 6
Dependent Claim 17 words
An antithrombotic agent according to claim 1 wherein the weight average molecular weight is about 3,500 daltons.
Claim 7
Dependent Claim 37 words
An antithrombotic agent according to claim 1 which, when isolated as a sodium salt, contains by elemental analysis about 26.2% carbon, 4.33% hydrogen, 1.98% nitrogen, 7.1% sulfur, and 9.8% sodium, the molar ratio C:N:S:Na being about 10:1.5:2:4.
Claim 8
Dependent Claim 26 words
A dosage form of the antithrombotic agent of claim 1 comprising from about 100 to about 500 mg. of said agent in a pharmaceutically acceptable carrier.
Claim 9
Dependent Claim 15 words
A dosage form according to claim 7 wherein the carrier comprises a solid, water-soluble excipient.
Claim 10
Dependent Claim 13 words
A dosage form according to claim 7 wherein the carrier comprises sterile water.

References Cited (Backward Citations)

US3766167A Cited
US4119774A Cited
US4122250A Cited
US4175182A Cited
US4281108A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1988-08-05 1989-02-04 1989-08-06 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1992-08-05 1993-02-04 1993-08-06 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1996-08-05 1997-02-04 1997-08-06 $7700.00 Window Closed / Lapsed

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