发明名称 |
Glycopegylated factor IX |
摘要 |
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. |
申请公布号 |
US8791070(B2) |
申请公布日期 |
2014.07.29 |
申请号 |
US201314052442 |
申请日期 |
2013.10.11 |
申请人 |
Novo Nordisk A/S |
发明人 |
DeFrees Shawn;Bayer Robert J.;Bowe Caryn;Paneerselvam Krishnasamy |
分类号 |
A61K38/00;A61P7/00;C12N9/64 |
主分类号 |
A61K38/00 |
代理机构 |
|
代理人 |
Brignati Michael J. |
主权项 |
1. 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; andG is R1-L-
wherein
L is C(O)CH2NHC(O); andR1 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. |
地址 |
Bagsvaerd DK |