Baxter International Inc.

Baxter Healthcare Sa

Baxalta Gmbh

Takeda Pharmaceutical Company Limited

Nektar Therapeutics

Baxter Aktiengesellschaft

Lipoxen Technologies Incorporated

Baxter Healthcare Inc.

Juergen Siekmann

Peter Turecek

Hanspeter Rottensteiner

Stefan Haider

Friedrich Scheiflinger

Katalin Varadi

Herbert Gritsch

Zhihao Fang

Mary J Bossard

Ping Zhang

Gayle Stephenson

Harold Zappe

Stacy Mitchell

Andreas Ivens

Hans-Peter Schwarz

Johann J Eibl

Sanjay Jain

Gregory Gregoriadis

Alfred Weber

Christian R Noe

Susanne Vejda

Michel Canavaggio

Oliver Zoechling

Gerhard Stoiber

Srijit Nath

Archana Dwivedi

Friedrich Dorner

Bernhard Fischer

Artur Mitterer

Hartmut Ehrlich

Hans Peter Schwarz

Birgit Maria Reipert

Joris Hoefinghoff

Christian Lubich

Richard Sheinecker

Richard Scheinecker

Christian Noe

The invention relates to materials and methods of conjugating a water soluble polymer to an oxidized carbohydrate moiety of a therapeutic 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 or hydrazone linkage is formed between the oxidized carbohydrate moiety and the active aminooxy group on the water soluble polymer, and wherein the conjugation is carried out in the presence of a nucleophilic catalyst.

Nucleophilic catalysts for oxime linkage

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 NaCNBHto form an alkoxyamine linkage.

Blood coagulation protein conjugates

The invention is a proteinaceous construct comprising a Factor VIII molecule which is conjugated to a water-soluble polymer via carbohydrate moieties of Factor VIII, and methods of preparing same.

Factor VIII polymer conjugates

A water soluble polymer, in particular polysialic acid (PSA) or a modified PSA (mPSA), is conjugated to an oxidized carbohydrate moiety of a glycoprotein other than a blood coagulation protein or to a ganglioside or drug delivery system by contacting the oxidized carbohydrate moiety with the water soluble polymer, wherein said water soluble polymer contains an aminooxy group and an oxime linkage is formed between the oxidized carbohydrate moiety and the aminooxy group on the water soluble polymer or wherein said water soluble polymer contains a hydrazide group and a hydrazone linkage is formed between the oxidized carbohydrate moiety and the hydrazide group on the water soluble polymer. Conjugates of aminooxy- or hydrazide-water soluble polymer, such as PSA and mPSA, are thus obtained in which the PSA or mPSA is attached via a carbohydrate moiety.

Glycopolysialylation of non-blood coagulation proteins

The present invention relates to a proteinaceous construct comprising plasmatic or recombinant factor VIIa (FVIIa) or biologically active derivatives thereof, which are bound to a carbohydrate moiety comprising 1-4 sialic acid units, wherein the in vivo half-life of the proteinaceous construct is substantially prolonged in the blood of a mammal, as compared to the in vivo half-life of a FVIIa molecule not bound to a carbohydrate moiety. The invention also provides a method for controlling bleeding in a mammal having a bleeding disorder due to functional defects or deficiencies of FVIIa, FVIII, or FIX. The invention also provides a method for controlling bleeding in a mammal during surgery or trauma.

Factor VIIa-polysialic acid conjugates having prolonged in vivo half-life

The present invention relates to a method for determining the amount of a physiologically acceptable polymer molecule bound to a protein, an antibody or other composition being capable of specifically binding to a physiologically acceptable polymer molecule, and a kit containing said antibody or composition.

Method and compositions for specifically detecting physiologically acceptable polymer molecules

The present invention provides von Willebrand Factor-polymer conjugates and Factor VIII-polymer conjugates, each having a releasable linkage. Methods of making conjugates, methods for administering conjugates, are also provided.

Von willebrand factor- and factor VIII-polymer conjugates having a releasable linkage

The invention relates to materials and methods of conjugating a water soluble fatty acid derivative to a therapeutic protein comprising contacting the therapeutic protein with an activated water soluble fatty acid derivative under conditions that allow conjugation.

Materials and methods for conjugating a water soluble fatty acid derivative to a protein

A novel process for the production of Fmoc (9H-fluoren-9-ylmethoxycarbonyl)-based compounds is provided, wherein a protecting group for the 9-hydroxymethyl group of the fluorene ring system is utilized. These compounds are useful for the modification of protein and peptide drugs.

Method for preparing FMOC-based hydrolysable linkers

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Vienna, Austria

Juergen Siekmann