Erythropoietin conjugates

US7128913B2 · kind B2 · utility

Assignee

• Hoffmann-La Roche Inc. · US

Inventors

• Josef Burg · Weilheim, DE
• Alfred Engel · Tutzing, DE
• Reinhard Franze · Penzberg, DE
• Bernd Hilger · Indianapolis, US
• Hartmut Schurig · Munich, DE
• Wilhelm Tischer · Peißenberg, DE
• Manfred Wozny · Weilheim, DE

Key dates

• Filing date: Dec 11, 2001
• Grant date: Oct 31, 2006
• Expiry date: Apr 6, 2023

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention refers to conjugates of erythropoietin with poly(ethylene glycol) comprising an erythropoietin glycoprotein having an N-terminal α-amino group and having the in vivo biological activity of causing bone marrow cells to increase production of reticulocytes and red blood cells and selected from the group consisting of human erythropoietin and analogs thereof which have the sequence of human erythropoietin modified by the addition of from 1 to 6 glycosylation sites or a rearrangement of at least one glycosylation site; said glycoprotein being covalently linked to one poly(ethylene glycol) group of the formula—CO—(CH2)x—(OCH2CH2)m—ORwherein the —CO of the poly(ethylene glycol) group forms an amide bond with said N-terminal α-amino group; and wherein R is lower alkyl; x is 2 or 3; and m is from about 450 to about 1350.