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US 2013/0095548 A1Published application
Activated sialic acid derivatives for protein derivatisation and conjugation
AssigneeLipoxen Technologies Limited
InventorsSanjay JAIN, Ioannis PAPAIOANNOU, Smita THOBHANI
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Abstract
Derivatives of PSAs are synthesised, in which a reducing and/or non-reducing end terminal sialic acid unit is transformed into a N-hydroxysuccinimide (NHS) group. The derivatives may be reacted with substrates, for instance substrates containing amine or hydrazine groups, to form non-cross-linked/crosslinked polysialylated compounds. The substrates may, for instance, be therapeutically useful drugs, peptides or proteins or drug delivery systems.
Claims14
-2. (canceled)
A compound having the general formula I, II or III
- in which R1 is H or sulfo;
- R2 is a linking group;
- A is NR5, NR5NR6, O or S wherein R5 and R6 are independently selected from H, C1-4 alkyl and aryl;
- SylO is a sialyl group;
- n is 1-100 and m is 0-100;
- R3 is hydrogen or;
- and
- R4 is hydrogen.
5 more elements
-12. (canceled)
Dependencies are inferred from the claim text.