RU2000119750A

RU2000119750A - NEW PENTACCHARIDES, METHODS OF THEIR PRODUCTION AND CONTAINING THEIR PHARMACEUTICAL COMPOSITIONS

Info

Publication number: RU2000119750A
Application number: RU2000119750/04A
Authority: RU
Inventors: Морис ПТИТУ
Original assignee: Санофи-Синтелябо; Акзо Нобел Н.В.
Priority date: 1998-01-19
Filing date: 1999-01-13
Publication date: 2002-06-10

Claims

1. Pentasaccharide in acid form and its pharmaceutically acceptable salts, the anionic form of which has the formula (see graphic part)
where R ₁ represents (C ₁ -C ₃ ) alkyl;
- R represents hydrogen or -SO ₃ , (C ₁ -C ₃ ) alkyl or (C ₂ -C ₃ ) acyl group;
T represents hydrogen or ethyl group;
n represents 1 or 2.

2. Pentasaccharide according to claim 1 in the form of sodium salt or potassium salt.

3. Pentasaccharide according to any one of paragraphs. 1 and 2, selected from:
Methyl-O- (2,3,4-tri-O-methyl-6-O-sulfo-α-D-glucopyranosyl) - (1 -> 4) -O- (2,6-anhydro-5-C -carboxy-3-O-methyl-β-D-mannopyranosyl) - (1 -> 4) -O- (2,3,6-tri-O-sulfo-α-D-glucopyranosyl) - (1-- > 4) -O- (2,6'-anhydro-3-O-methyl-α-L-idopyranosyluronic acid) - (1 -> 4) -2,3,6-tri-O-sulfo-α- D-glucopyranoside sodium salt.

Methyl-O- (2,3,4-tri-O-methyl-6-O-sulfo-α-D-glucopyranosyl) - (1 -> 4) -O- (5-С-ethyl-2,3 -di-O-methyl-β-D-glucopyranosyluronic acid) - (1 -> 4) -O- (2,3,6-tri-O-sulfo-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-sulfo α-D-glucopyranoside sodium salt.

Methyl-O- (2,3,4-tri-O-methyl-6-O-sulfo-α-D-glucopyranosyl) - (1 -> 4) -O- (2,3-di-O-methyl -β-D-glucopyranosyluronic acid) - (1 -> 4) -O- (2,3,6-tri-O-sulfo-α-D-glucopyranosyl) - (1 -> 4) -O- ( 2,6-anhydro-5-C-carboxy-3-O-methyl-β-D-mannopyranosyl) - (1 -> 4) -2-O-sulfo-3,6-di-O-methyl-α -D-glucopyranoside sodium salt.

Methyl-O- (2,3,4-tri-O-methyl-6-O-sulfo-α-D-glucopyranosyl) - (1 -> 4) -O- (2,3-di-O-methyl -β-D-glucopyranosyluronic acid) - (1 -> 4) -O- (2,3,6-tri-O-sulfo-α-D-glucopyranosyl) - (1 -> 4) -O- ( 2,6-anhydro-5-C-carboxy-3-O-methyl-β-D-mannopyranosyl) - (1 -> 4) -2,3-di-O-sulfo-6-O-methyl-α -D-glucopyranoside sodium salt.

Methyl-O- (2,3,4-tri-O-methyl-6-O-sulfo-α-D-glucopyranosyl) - (1 -> 4) -O- (2,3-di-O-methyl -β-D-glucopyranosyluronic acid) - (1 -> 4) -O- (2,3,6-tri-O-sulfo-α-D-glucopyranosyl) - (1 -> 4) -O- ( 2,6-anhydro-5-C-carboxy-3-O-methyl-β-D-mannopyranosyl) - (1 -> 4) -2,6-di-O-sulfo-3-O-methyl-α -D-glucopyranoside sodium salt.

Methyl-O- (2,3,4-tri-O-methyl-6-O-sulfo-α-D-glucopyranosyl) - (1 -> 4) -O- (2,3-di-O-methyl -β-D-glucopyranosyluronic acid) - (1 -> 4) -O- (2,3,6-tri-O-sulfo-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-sulfo-α -D-glucopyranoside sodium salt.

4. Pharmaceutical compositions containing as active principle pentasaccharide according to any one of paragraphs. 1-3 in salt form with a pharmaceutically acceptable base or in acid form, combined or mixed with a pharmaceutically acceptable non-toxic inert excipient.

5. A pharmaceutical composition according to claim 4 in the form of dosage units, where the active principle is mixed with at least one pharmaceutical excipient.

6. The composition according to claim 5, where each dosage unit contains from 0.1 to 100 mg of active principle.

7. The composition according to claim 6, where each dosage unit contains from 0.5 to 50 mg of active principle.

8. The use of polysaccharide on PP. 1-3 for the preparation of drugs that are useful in pathologies associated with coagulation dysfunction.