Heparins including at least one covalent bond with biotin or a biotin derivative, method for preparing same and use thereof
AssigneeSanofi-Aventis
InventorsChristian VISKOV, Philippe HUBERT, Pierre MOURIER
Life of this patent
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Abstract
The invention relates to biotinylated heparins comprising constituent polysaccharides having at their reducing ends at least one covalent bond with biotin or a biotin derivative, and also to the process for preparing them, to pharmaceutical compositions containing them and to their therapeutic use. The biotinylated polysaccharides are of the formula (I) with the variables as defined herein.
Claims17
A biotinylated heparin, comprising constituent polysaccharides, wherein the constituent polysaccharides have at their reducing ends a covalent bond to a group —(R1)i-Biot and correspond to the formula (I):
- in which:
- i is equal to 0 or 1,
- R1 represents a sequence of formula (a) or (b):
- in which j and k, which may be identical or different, are integers that may take any value from 1 to 10,
- Biot represents a biotin group or a biotin derivative,
- n represents an integer with a mean value of about 25 for a heparin with an average molecular mass of 15 000 Da,
- X represents H or SO3Na,
- Y represents COCH3 or SO3Na, and
- the wavy line denotes a bond located either below or above the plane of the pyranose ring to which it is attached,
- or the pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.