US 2014/0154230 A1Published application

Glycopegylated Factor IX

AssigneeNovo Nordisk A/S

InventorsShawn DeFrees, Robert J. Bayer, Caryn Bowe, Panneerselvam Krishnasamy

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Abstract

Conjugates between Factor IX and PEG moieties. are disclosed in the present application. The conjugates are linked via a glycosyl linking group interposed between and covalently attached to the peptide and the modifying group. 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.

Claims5

Dependent claims

A PEGylated Factor IX protein comprising SEQ ID NO:1 and a poly(ethylene glycol) moiety, wherein the poly(ethylene glycol) moiety is conjugated to an amino acid selected from Asn 157 and Asn 167 of SEQ ID NO:1 via a glycosyl linking group of a glycosyl residue, and having a composition according to the formula:

wherein
R2 is COOH;
R3 is H;
R4 is OH;
D is OH;
and
G is R1-L-
wherein
L is a substituted heteroalkyl linker comprising C(O)CH2NH;
R1 is the poly(ethylene glycol) moiety, wherein the poly(ethylene glycol) moiety comprises a branched poly(ethylene glycol) having a core glycerol moiety, and wherein the branched poly(ethylene glycol) has a molecular weight of about 40 kDa.

7 more elements

Dependencies are inferred from the claim text.

Facts

Application: 14/055,971Filed 17 Oct 2013
Priority: 25 May 2005
Published: 5 Jun 2014
Term ends: Not estimatedThe source records don’t support an estimate.

Classification10 codes

A61K 38/4846
Serine endopeptidases: factor VII ; Factor IX ; Factor Xa ; Factor XI ; Factor XII
A61K 47/549
The modifying agent being an organic compound: sugars, nucleosides, nucleotides or nucleic acids
A61K 47/60
Obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes: the organic…
A61P 7/04
Drugs for disorders of the blood or the extracellular fluid: antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents

Family

Application60/684,729Us provisional application · filed 25 May 2005
Application60/707,994Us provisional application · filed 12 Aug 2005
Application60/710,535Us provisional application · filed 23 Aug 2005
Application11/915,239Continuation · filed 21 May 2008
Application14/055,971Continuation
US 2008/0255026 A1Published application
US 2014/0154230 A1This patent

From the US filing history. Foreign family members aren’t listed.

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