Glycopegylated factor vii and factor viia

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 14/745 (2006.01) C12P 19/00 (2006.01)

Patent

CA 2619969

The present invention provides conjugates between Factor VII or Factor Vila 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.

La présente invention concerne des conjugués entre des peptides du facteur VII ou du facteur VIIa et des fractions de PEG. Les conjugués sont liés par le biais d'un groupe de liaison glycosyle intact qui est interposé entre le peptide et le groupe modificateur et fixé par covalence à ceux-ci. Les conjugués sont formés à partir de peptides à la fois glycosylés et non glycosylés sous l'action d'une glycosyltransférase. La glycosyltransférase ligature une fraction sucre modifiée sur soit un acide aminé, soit un résidu de glycosyle sur le peptide. Cette invention concerne également des formulations pharmaceutiques renfermant les conjugués. Cette invention concerne en outre des procédés de préparation de ces conjugués.

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