Alfa Wassermann, Inc.

Piani Silvano

Marchi Egidio

Tamagnone Gianfranco

Ungarelli Fabrizio

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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Bologna, Italy

Piani Silvano