Semi-synthetic glycosaminoglycans with heparin or heparan struct

Details Semi-synthetic glycosaminoglycans with heparin or heparan struct Semi-synthetic glycosaminoglycans with heparin or heparan struct

1993-04-13

1995-07-04

Robinson, Douglas W.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

536124, 514 8, 514 56, 530322, 530345, C08B 3710, A61K 31725

Patent

active

054301335

ABSTRACT:
New heparin and heparan sulfate derivatives having antithrombotic activity, also endowed with reduced haemorrhagic and anticoagulant activity, are obtained by nucleophilic addition to heparin and heparan sulfate derivatives containing 2,3-anhydrogulonic acid residues. The compounds have the formula IV ##STR1## The glycosaminoglycan derivatives obtained through this treatment show a structural modification in the unit of .alpha.-L-iduronic acid 2-O-sulfate with the partial or total selective substitution of the O-sulfate group in position 2 with a nucleophilic residue. The structural modifications produce an improvement of the biological properties of the heparin and heparan sulfate, substantially keeping the antithrombotic activity while diminishing the haemorragic effect in vivo and the anticoagulant activity in vitro.

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The Merck Index, Merck and Co., Inc. 1989, Eleventh Edition, monograph No. 4571, p. 4575.
Carey, F. A.; Sundberg, R. J. "Advanced Organic Chemistry--Part B: Reactions and Synthesis" 2nd ed. Plenum Press, New York 1983, pp. 498-501.
Morrison, R. T.; Boyd, R. N. "Organic Chemistry" 4th ed. Allyn and Bacon, Boston 1983, pp. 549-550.
Jaseja et al. Can. J. Chem. 1989, 67, 1449-1456.

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