Antithrombotic agent

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

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536 21, 514822, A61K 31725, C08B 3710

Patent

active

045335494

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.

REFERENCES:
patent: 3766167 (1973-10-01), Lasker
patent: 4119774 (1978-10-01), Andersson et al.
patent: 4122250 (1978-10-01), Schmer
patent: 4175182 (1979-11-01), Schmer
patent: 4281108 (1981-07-01), Fussi
Lasker, Adv. Exp. Med. Biol., vol. 52, pp. 119-130, 1975.
Lasker, Federation Proceedings, vol. 36, pp. 92-97, 1977.
Andersson et al., Thrombosis Research, vol. 9, pp. 575-583, 1976.
Hook et al., FEBS Letters, vol. 66, pp. 90-93, 1976.

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