Method for controlling o-desulfation of heparin and compositions

Details Method for controlling o-desulfation of heparin and compositions Method for controlling o-desulfation of heparin and compositions

1992-12-22

1994-03-22

Lilling, Herbert J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

514 54, 536 21, A61K 31725, C08R 3710

Patent

active

052964710

ABSTRACT:
Methods of making and using, as prophylatics or therapeutics for preventing or treating certain diseases including cancer, O-desulfated heparin compositions, preferably 2-O, 3-O desulfated heparin compositions, wherein the methods permit regulating the degree of 2-O, 3-O desulfation to produce compositions that are variably desulfated including about 99% and 75% desulfated at the 2-O and 3-O positions, respectively.

REFERENCES:
patent: 5010063 (1991-04-01), Piani et al.
patent: 5104860 (1992-04-01), Piani et al.
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Bar-Ner et al. Blood 70(2) 1987 pp. 551-557.
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Stokes et al. Lab Invest 63(5) 1990 pp. 657-668.
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Article by Jaseja, et al., entitled "Novel Regio-and Stereoselective Modifications of Heparin in Alkaline Solution. Nuclear Magnetic Resonance Spectroscopic Evidence" published by Can. J. Chem., 67:1449-1456 (1989).
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Article by Fraidenraich, et al., entitled "Selective O-desulphation of Heparin in Triethylamine" published by Elsevier Science Publishers, Ltd., Carbohydrate Polymers, pp. 111-114 (1991).
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Article by Ishihara, et al., entitled "A Cell-Based Assay for Evaluating the Interaction of Heparin-like Molecules and Basic Fibroblast Growth Factor" published by Academic Press, Inc., 202:310-315 (1992).

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