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.
Claims50
A process of making an activated polysialic acid (PSA) molecule comprising a terminal sialic acid unit at the reducing end, the process comprising:
- a) reducing the reducing terminal sialic acid unit to form a vicinal diol group;
- b) selectively oxidizing the vicinal diol group of step (a) to form an aldehyde group;
- c) aminating the aldehyde group of step (b) to form an amine group;
- and
- d) reacting the amine group of step (c) with a bifunctional reagent comprising two amine-reactive functional groups to form an activated PSA molecule, the activated PSA molecule being monofunctional and comprising an amine-reactive group at the reducing end.
Dependencies are inferred from the claim text.