C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 14/00 (2006.01) A61K 47/48 (2006.01) C07H 9/06 (2006.01) C07H 13/04 (2006.01) C07H 15/04 (2006.01) C07H 15/12 (2006.01)
Patent
CA 2081665
This invention relates to a method of producing peracetyloxazolines from peracetyl saccharides. The method involves reacting the starting material, a peracetyl saccharide, with a reagent combination, to directly produce the peracetyl oxazoline. This method maybe used for the activation of oligosaccharides, wherein an oligosaccharide containing a reducing GIcNAc terminus is activated by the formation of an oxazoline at the terminal GIcNAc, and then coupled with a bifunctional spacer to provide an oli- gosaccharide-spacer conjugate. The activated oligosaccharide-spacer conjugate is then coupled to a protein, such as granulocyte colony stimulating factor or .gamma.-interferon, providing a neoglycoprotein conjugate. The invention provides a method for forming neoglycoprotein conjugates which may improve biological and physiochemical properties of the protein. For example, serum life- time or efficiency of drug delivery of the peptide to a target organ or cell may be improved.
Borowski Marianne
Colon Marcelo
Davis Jeffrey T.
Hirani Shirish
Rasmussen James R.
Genzyme Corporation
Gowling Lafleur Henderson Llp
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