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US 8,946,406 B2Granted
Derivatisation of erythropoietin (EPO)
AssigneeLipoxen Technologies Limited
InventorsSanjay Jain, Peter Laing, Gregory Gregoriadis, Norbert Oskar Rumpf
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Abstract
The present invention relates to a compound which is a polysaccharide derivative of EPO, or of an EPO like protein, wherein the polysaccharide is anionic and comprises between 2 and 200 saccharide units. The present invention also relates to pharmaceutical compositions comprising the novel compounds, and methods for making the novel compounds.
Claims10
A method for producing a polysaccharide derivative of erythropoietin (EPO), comprising:
- reacting the polysaccharide with an amine group of an internal amino acid side chain of EPO, wherein the polysaccharide is anionic and comprises between 2 and 125 saccharide units and wherein the EPO is derivatised by the polysaccharide at the reducing terminal unit of the polysaccharide.
A method for producing the compound of formula (I):
- wherein m is at least one;
- XB is B—XH wherein B is EPO and XH is NH2 and is an amine group of a lysine amino acid side chain of EPO;
- L is a bond or a linking group;
- GlyO is an anionic saccharide unit,
- wherein the linking group, if present, is of the formula
- —Y—C(O)—R1—C(O)—;
- wherein R1 is a difunctional organic radical selected from the group consisting of alkanediyl, arylene, alkarylene, heteroarylene and alkylheteroarylene, any of which is optionally substituted and/or interrupted by carbonyl, ester, sulfide, ether, amide and/or amine linkages;
- and
- wherein Y is NR2 or NR2—NR2 and R2 is H or C1-6 alkyl comprising:
- reacting the polysaccharide with an amine group of an internal amino acid side chain of EPO.
7 more elements
Dependencies are inferred from the claim text.