Heparin derivatives and process for their preparation

Details Heparin derivatives and process for their preparation Heparin derivatives and process for their preparation

1989-05-26

1991-04-23

Griffin, Ronald W.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

514 54, 514 62, 514822, 536 21, A61K 31725, C08B 3710

Patent

active

050100637

ABSTRACT:
New heparin derivatives having antithrombotic activity, also endowed with reduced hemorrhagic and anticoagulant activity, obtained by treating in a basic medium heparins of various origin, optionally in the presence of alkali metal salts and of a reducing agent.
The heparin derivatives obtained through this treatment show peculiar chimico-physical characteristics, like new signals at about 53 and 54 p.p.m. in the .sup.13 C-NMR spectrum and an increase of the specific rotatory power, compared to that of the starting heparins, to values between +50.degree. to +90.degree..
Said structural modifications produce an improvement of the biological properties of the heparin, substantially keeping the antithrombotic activity while diminishing the hemorrhagic effect in vivo and the anticoagulant activity in vitro.

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patent: 4816446 (1989-03-01), Feller et al.
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Ogren et al.; Chemical Abstracts 76:57073z (1972).
Fransson et al.; Biochem. J. 175:299-309 (1978).
Gatti et al.; Macromolecules 12(5):1001-1007 (1979).
Kosakai et al.; J. Biochem. 86:147-153 (1979).
Ayotte et al.; Carbohydrate Res. 145:267-277 (1986).

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