Claims
- 1. A pentasaccharide in acidic form and its pharmaceutically acceptable salts, the anionic form of which has the formula: in which:R represents hydrogen or an —SO3−, (C1-C3)alkyl or (C2-C3)acyl group; T represents hydrogen or an ethyl group; and n represents 1 or 2.
- 2. A pentasaccharide according to claim 1, in the form of the sodium salt or the potassium salt.
- 3. A pentasaccharide according to claim 2 selected from the group consisting of:Methyl O-(2,3,4-tri-O-methyl-6-O-sulpho-α-D-glucopyranosyl)-(1→4)-O-(2,3-di-O-methyl-β-D-glucopyranosyluronic acid)-(1→4)-O-(2,3,6-tri-O-sulpho-α-D-glucopyranosyl)-(1→4)-O-(2,6-anhydro-5-C-carboxy-3-O-methyl-β-D-mannopyranosyl(1→4)-2,3,6-tri-O-sulpho-α-D-glucopyranoside, sodium salt; Methyl O-(2,3,4-tri-O-methyl-6-O-sulpho-α-D-glucopyranosyl)-(1→4)-O-(5-C-ethyl-2,3-di-O-methyl-β-D-glucopyranosyluronic acid)-(1→4)-O-(2,3,6-tri-O-sulpho-α-D-glucopyranosyl)-(1→4)-O-(2,6-anhydro-5-C-carboxy-3-O-methyl-β-D-mannopyranosyl)-(1→4)-2,3,6-tri-O-sulpho-α-D-glucopyranoside, sodium salt; Methyl O-(2,3,4-tri-O-methyl-6-O-sulpho-α-D-glucopyranosyl)-(1→4)-O-(2,3-di-O-methyl-β-D-glucopyranosyluronic acid)-(1→4)-O-(2,3,6-tri-O-sulpho-α-D-glucopyranosyl)-(1→4)-O-(2,6-anhydro-5-C-carboxy-3-O-methyl-β-D-mannopyranosyl)-(1→4)-2-O-sulpho-3,6-di-O-methyl-α-D-glucopyranoside, sodium salt; Methyl O-(2,3,4-tri-O-methyl-6-O-sulpho-α-D-glucopyranosyl)-(1→4)-O-(2,3-di-O-methyl-β-D-glucopyranosyluronic acid)-(1→4)-O-(2,3,6-tri-O-sulpho-α-D-glucopyranosyl)-(1→4)-O-(2,6-anhydro-5-C-carboxy-3-O-methyl-β-D-mannopyranosyl)-(1→4)-2,3-di-O-sulpho-6-O-methyl-α-D-glucopyranoside, sodium salt; Methyl O-(2,3,4-tri-O-methyl-6-O-sulpho-α-D-glucopyranosyl)-(1→4)-O-(2,3-di-O-methyl-β-D-glucopyranosyluronic acid)-(1→4)-O-(2,3,6-tri-O-sulpho-α-D-glucopyranosyl)-(1→4)-O-(2,6-anhydro-5-C-carboxy-3-O-methyl-β-D-mannopyranosyl)-(1→4)-2,6-di-O-sulpho-3-O-methyl-α-D-glucopyranoside, sodium salt; and Methyl O-(2,3 ,4-tri-O-methyl-6-O-sulpho-α-D-glucopyranosyl)-(1→4)-O-(2,3-di-O-methyl-β-D-glucopyranosyluronic acid)-(1→4)-O-(2,3,6-tri-O-sulpho-α-D-glucopyranosyl)-(1→4)-O-(2,7-anhydro-5-C-carboxy-6-deoxy-3-O-methyl-β-D-mannoheptopyranosyl)-(1→4)-2,3,6-tri-O-sulpho-α-D-glucopyranoside, sodium salt.
- 4. A pharmaceutical composition containing, as active principle, a pentasaccharide according to claim 1, in the form of a salt with a pharmaceutically acceptable base or in acidic form, combined with or mixed with a pharmaceutically acceptable, non-toxic inert excipient.
- 5. A pharmaceutical composition according to claim 4, in the form of a dosage unit containing from about 0.1 to about 100 mg of active principle.
- 6. A pharmaceutical composition according to claim 5, in which each dosage unit contains from about 0.5 to about 50 mg of active principle.
- 7. A pharmaceutical composition according to claim 4 wherein the pentasaccharide is in the form of a sodium or potassium salt.
- 8. A pharmaceutical composition containing, as active principle, a pentasaccharide according to claim 3.
- 9. A pharmaceutical composition according to claim 7 in the form of a dosage unit containing from about 0.1 to about 100 mg of active principle.
- 10. A pharmaceutical composition according to claim 8 in the form of a dosage unit containing form about 0.1 to about 100 mg of active principle.
- 11. A pharmaceutical composition according to claim 9 in which each dosage unit contains from about 0.5 to about 50 mg of active principle.
- 12. A pharmaceutical composition according to claim 10 in which each dosage unit contains from about 0.5 to about 50 mg of active principle.
- 13. A method for the treatment of pathologies associated with a clotting dysfunction which comprises administering to a patient in need of such treatment a polysaccharide according to claim 1.
- 14. A method according to claim 13 wherein the polysaccharide is in the form of a sodium or potassium salt.
- 15. A method for the treatment of pathologies associated with a clotting dysfunction which comprises administering to a patient in need of such treatment a polysaccharide according to claim 3.
Priority Claims (1)
Number |
Date |
Country |
Kind |
98 00514 |
Jan 1998 |
FR |
|
Parent Case Info
This is the National Phase Application of PCT/FR99/00045, filed Jan. 13, 1999.
PCT Information
Filing Document |
Filing Date |
Country |
Kind |
PCT/FR99/00045 |
|
WO |
00 |
Publishing Document |
Publishing Date |
Country |
Kind |
WO99/36428 |
7/22/1999 |
WO |
A |
Foreign Referenced Citations (1)
Number |
Date |
Country |
WO 9803554 |
Jul 1997 |
WO |
Non-Patent Literature Citations (2)
Entry |
Sakairi, et al., Chem. Euro. J. 2(8), 1007-1013 (1996); “Synthesis of a Conformationally Constrained Heparin-Like Pentasaccharide”. |
Ragazzi et al., Carbohydrate Research 195(2), 169-186 (1990); “Conformation Of The Pentasaccharide Corresponding To The Binding Site Of Heparin for Antithrombin III”. |