Semi-synthetic glycosaminoglycans containing .alpha.-L-galacturo

Details Semi-synthetic glycosaminoglycans containing .alpha.-L-galacturo Semi-synthetic glycosaminoglycans containing .alpha.-L-galacturo

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

054301327

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 new products have the formula IV ##STR1## and show a structural modification of the unit of .alpha.-L-iduronic acid 2-O-sulfate with the partial or total selective modification to .alpha.-L-galacturonic acid in which the hydroxyl group in position 3 is replaced with a nucleophilic residue. This structural modification produces 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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Carey, F. A.; Sundberg, R. J. "Advanced Organic Chemistry--Part B: Reactions and Synthesis" 2nd ed. Plenum Press, N.Y. 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.
The Merck Index, Merck and Co., Inc. 1989, Eleventh Edition, Monograph No. 4571, p. 4575.

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