Polymer-conjugated glycosylated neublastin

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 17/08 (2006.01) A61K 38/18 (2006.01) A61K 47/48 (2006.01) A61P 43/00 (2006.01) C07K 14/475 (2006.01)

Patent

CA 2522364

The following class of molecule is disclosed: a dimer containing a first neublastin polypeptide and a second neublastin polypeptide, wherein: (a) at least one of the polypeptides is glycosylated; (b) at least one of the polypeptides is conjugated at its N-terminus to a water-soluble synthetic polymer; and (c) neither of the polypeptides is conjugated to a water-soluble synthetic polymer at a position other than the N-terminus. Such dimers possess the biological activity of wild-type neublastin while displaying enhanced serum half-life and enhanced potency relative to wild-type neublastin.

L'invention porte sur la classe suivante d'une molécule: un dimère contenant un premier polypeptide de neublastine et un second polypeptide de neublastine: (a) au moins un des polypeptides est glycosylé; (b) au moins un des polypeptides est conjugué au niveau de son extrémité N-terminale à un polymère synthétique soluble dans l'eau; et (c) l'un et l'autre des polypeptides sont conjugués à un polymère synthétique soluble dans l'eau à une position autre que celle de l'extrémité N-terminale. Ces dimères possèdent l'activité biologique de la neublastine de type sauvage tout en présentant une demi-vie sérique accrue et une capacité accrue par rapport à la neublastine de type sauvage.

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