Semi-synthetic glycosaminoglycans with heparin or heparan structure of .alpha.-L-iduronic-2-O-sulfate acid modified in position 2
US5430133A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Apr 13, 1993 |
| Grant date | Jul 4, 1995 |
| Priority date | — |
| Expiry date | Apr 13, 2013 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC08B37/0075
- WIPO fieldMacromolecular chemistry, polymers
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.