Method for preparing a site-specific physiologically active...

C - Chemistry – Metallurgy – 07 – K

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C07K 1/14 (2006.01) C07K 1/10 (2006.01) C07K 1/18 (2006.01)

Patent

CA 2755395

The present invention provides a method for preparing a site-specific physiologically active polypeptide conjugate in a high yield by treating a physiologically active polypeptide with a non- peptidyl polymer in the presence of an alcohol at a spe-cific pH, which can be desirably employed in the development of long acting formulations of various peptide drugs having high in-vivo activity and markedly prolonged in-blood half-life.

La présente invention concerne un procédé de préparation d'un conjugué de polypeptide physiologiquement actif et spécifique d'un site en un rendement élevé par traitement d'un polypeptide physiologiquement actif avec un polymère non peptidique en présence d'un alcool à un pH spécifique, et qui peut de manière souhaitable être utilisé dans la mise au moins de formulations à action prolongée de différents médicaments peptidiques ayant une grande activité in vivo et une demi-vie dans le sang remarquablement prolongée.

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