Glycopegylated erythropoietin

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 17/08 (2006.01) A61K 38/00 (2006.01) A61K 47/48 (2006.01) C07K 7/00 (2006.01) C07K 14/505 (2006.01) C12P 21/02 (2006.01) A61K 38/18 (2006.01) C07K 17/10 (2006.01)

Patent

CA 2547140

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.

La présente invention concerne des conjugués d'érythropoiétine et de fragment PEG. Ces conjugués sont liés par l'intermédiaire d'un groupe de liaison glycosyl interposé entre le peptide et le groupe modificateur et relié par covalence au peptide et au groupe modificateur. Les conjugués sont formés à partir de peptides glycosylés par l'action d'une glycosyltransférase. La glycosyltransférase ligature un fragment de sucre modifié sur un reste de glycosyl sur le peptide. En outre, cette invention concerne des procédés permettant de préparer les conjugués, des méthodes permettant de traiter divers états pathologiques avec ces conjugués, ainsi que des préparations pharmaceutiques comprenant de tels conjugués.

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