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Title:
BLOOD COAGULATION PROTEIN CONJUGATES
Document Type and Number:
WIPO Patent Application WO/2011/017055
Kind Code:
A3
Abstract:
The invention relates to materials and methods of conjugating a water soluble polymer to an oxidized carbohydrate moiety of a blood coagulation protein comprising contacting the oxidized carbohydrate moiety with an activated water soluble polymer under conditions that allow conjugation. More specifically, the present invention relates to the aforementioned materials and methods wherein the water soluble polymer contains an active aminooxy group and wherein an oxime linkage is formed between the oxidized carbohydrate moiety and the active aminooxy group on the water soluble polymer. In one embodiment of the invention the conjugation is carried out in the presence of the nucleophilic catalyst aniline. In addition the generated oxime linkage can be stabilized by reduction with NaCNBH3 to form an alkoxyamine linkage.

Inventors:
SIEKMANN JUERGEN (AT)
HAIDER STEFAN (AT)
ROTTENSTEINER HANSPETER (AT)
TURECEK PETER (AT)
Application Number:
PCT/US2010/043242
Publication Date:
April 07, 2011
Filing Date:
July 26, 2010
Export Citation:
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Assignee:
BAXTER INT (US)
BAXTER HEALTHCARE SA (CH)
SIEKMANN JUERGEN (AT)
HAIDER STEFAN (AT)
ROTTENSTEINER HANSPETER (AT)
TURECEK PETER (AT)
International Classes:
A61K47/48
Domestic Patent References:
WO2008025856A22008-03-06
WO2005014024A22005-02-17
WO2009000522A12008-12-31
WO2008074032A12008-06-19
WO1994029370A11994-12-22
Foreign References:
US20090076237A12009-03-19
Other References:
ZENG YING ET AL: "High-efficiency labeling of sialylated glycoproteins on living cells", NATURE METHODS, vol. 6, no. 3, March 2009 (2009-03-01), pages 207 - 209, XP002605857, ISSN: 1548-7091
GREGORIADIS ET AL: "Improving the therapeutic efficacy of peptides and proteins: A role for polysialic acids", INTERNATIONAL JOURNAL OF PHARMACEUTICS, ELSEVIER BV, NL LNKD- DOI:10.1016/J.IJPHARM.2005.06.007, vol. 300, no. 1-2, 26 August 2005 (2005-08-26), pages 125 - 130, XP005013268, ISSN: 0378-5173
SANJAY JAIN ET AL: "Polysialylation: the natural way to improve the stability and pharmacokinetics of protein and peptide drugs", INTERNET CITATION, July 2004 (2004-07-01), XP007902391, Retrieved from the Internet [retrieved on 20070522]
Attorney, Agent or Firm:
BRUSCA, Eric, M. et al. (Gerstein & Borun LLP233 S. Wacker Drive,6300 Willis Towe, Chicago IL, US)
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