Neose Technologies, Inc.

Novo Nordisk A/s

Neose Pharmaceuticals, Inc.

Ratiopharm Gmbh

Biogenerix Ag

David A Zopf

Shawn DeFrees

Robert J Bayer

Caryn Bowe

David James Hakes

Xi Chelsea Chen

Paul M Simon

Henrik Clausen

Stephen A Roth

Edward J McGuire

Zhi-Guang Wang

Dennis H Langer

Walter Scott Willett

Karl Frank Johnson

Michael Partsch

Roger A Barthelson

John P McCauley, Jr

Lei Lu

Barry Brian

Marc Pelletier

William A Barker

Susann Taudte

David Jennings Hakes

Heinz Lubenau

Michael Felo

Ruye Xing

Jichao Kang

Matthew Kalo

Bingyuan Wu

Ming He

Daotian Fu

Marc Schwartz

Walter S Willett

Xi Chen

The present invention provides a glycopegylated G-CSF that is therapeutically active and which has pharmacokinetic parameters and properties that are improved relative to an identical, or closely analogous, G-CSF peptide that is not glycopegylated. Furthermore, the invention provides methods for mobilizing hematopoiesis in a subject, particularly a subject who has received or will receive radiation or chemotherapy treatment. The methods and compositions of the invention can further be used to prevent, alleviate and treat the myelosuppressive effects such therapies.

Methods of treatment using glycopegylated G-CSF

The invention relates to methods of preparing and purifying conjugates between Granulocyte Colony Stimulating Factor and PEG moieties. The conjugates are linked via an intact glycosyl linking group that is interposed between and covalently attached to the peptide and the modifying group. The conjugates are purified using various chromatography methods.

Glycopegylated granulocyte colony stimulating factor

The present invention provides conjugates between erythropoietin and PEG moieties. The conjugates are linked via an intact glycosyl linking group interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from glycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto a glycosyl residue on the peptide. Also provided are methods for preparing the conjugates, methods for treating various disease conditions with the conjugates, and pharmaceutical formulations including the conjugates.

Glycopegylated erythropoietin

The present invention provides conjugates between peptides and PEG moieties. The conjugates are linked via an intact glycosyl linking group that is interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from both glycosylated and unglycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto either an amino acid or glycosyl residue on the peptide. Also provided are pharmaceutical formulations including the conjugates. Methods for preparing the conjugates are also within the scope of the invention.

One pot desialylation and glycopegylation of therapeutic peptides

The invention includes methods and compositions for remodeling a peptide molecule, including the addition or deletion of one or more glycosyl groups to a peptide, and/or the addition of a modifying group to a peptide.

Glycopegylation methods and proteins/peptides produced by the methods

Erythropoietin: remodeling and glycoconjugation of erythropoietin

Granulocyte colony stimulating factor: remodeling and glycoconjugation G-CSF

The present invention provides polypeptides that include an O-linked glycosylation site that is not present in the wild-type peptide. The polypeptides of the invention include glycoconjugates in which a species such as a water-soluble polymer, a therapeutic agent of a biomolecule is covalently linked through an intact O-linked glycosyl residue to the polypeptide. Also provided are methods of making the peptides of the invention and methods, pharmaceutical compositions containing the peptides and methods of treating, ameliorating or preventing diseased in mammals by administering an amount of a peptide of the invention sufficient to achieve the desired response.

O-linked glycosylation of peptides

The present invention provides IFN-&#x3b1; conjugates including IFN-&#x3b1; peptides and modifying groups such as PEG moieties. The IFN-&#x3b1; peptide and modifying group are linked via an intact glycosyl linking group interposed between and covalently attached to the IFN-&#x3b1; peptide and the modifying group. The IFN-&#x3b1; conjugates are formed from glycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar onto an amino acid or a glycosyl residue on the IFN-&#x3b1; peptide. Also provided are methods for preparing the IFN-&#x3b1; conjugates, methods for treating various disease conditions with the IFN-&#x3b1; conjugates, and pharmaceutical formulations including the IFN-&#x3b1; conjugates.

Glycopegylated interferon &#x3b1;

Factor VIII: remodeling and glycoconjugation of factor VIII

Factor VII: remodeling and glycoconjugation of Factor VII

The present invention provides conjugates between Granulocyte Colony Stimulating Factor and PEG moieties. The conjugates are linked via an intact glycosyl linking group that is interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from both glycosylated and unglycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto either an amino acid or glycosyl residue on the peptide. Also provided are pharmaceutical formulations including the conjugates. Methods for preparing the conjugates are also within the scope of the invention.

Glycopegylated erythropoietin formulations

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Wayne, PA, United States of America

David A Zopf