Bifunctional polyethylene glycol derivatives

• Main Authors: NHO KWANG, ROSEN PERRY
• Format: Patent
• Language: English
• Published: 15.05.2007
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; COMPOSITIONS BASED THEREON; COMPOSITIONS OF MACROMOLECULAR COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVINGCARBON-TO-CARBON UNSATURATED BONDS; MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONSONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; ORGANIC MACROMOLECULAR COMPOUNDS; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; THEIR PREPARATION OR CHEMICAL WORKING-UP

The present invention provides novel heterobifunctional and monobifunctional polyethylene glycol derivatives for the pegylation of therapeutically active proteins. The heterobifunctional PEGs which bear two different functional groups as well as the monobifunctional PEGs which contain two similar functional groups, may be used for cross-linking purposes. The cross-linking may be intramolecular between two areas within the same molecule or intermolecular between two separate molecules. The pegylated protein conjugates that are produced, retain a substantial portion of their therapeutic activity and are less immunogenic than the protein from which the conjugate is derived. New syntheses for preparing such bifunctional derivatives are described.