C - Chemistry – Metallurgy – 08 – G
Patent
C - Chemistry, Metallurgy
08
G
C08G 65/333 (2006.01) A61K 47/48 (2006.01)
Patent
CA 2515612
The present invention relates to the preparation of polyethylene glycol carbonate active esters useful for the PEGylation of biological active and pharmaceutically useful peptides and proteins. The invention involves the use of activated oxalate esters in the formation of polyethylene glycol mixed carbonate active esters that then react with a linker or directly with a target peptide or protein. In particular N, N~-disuccinimidyl oxalate or 1, 1~- bis [6- (trifluoromethyl) benzotriazolyl] oxalate is used.
L'invention concerne la préparation d'esters de carbonate actif de polyéthylèneglycol utiles dans la PEGylation de peptides et de protéines actifs sur le plan biologique et utiles sur le plan pharmaceutique. L'invention concerne également l'utilisation d'esters d'oxalate et de carbonate activés dans la formation d'esters de carbonate actif mélangés à du polyéthylèneglycol réagissant ensuite en présence d'un liant ou directement avec un peptide ou une protéine cible.
Pharmacia Corporation
Sim & Mcburney
LandOfFree
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