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US 12,729,236 B2Granted
Hydrophilic linkers for antibody or DARPin conjugates
AssigneeValitor, Inc.
InventorsWesley M. Jackson, Amy A. Twite, Livia Wilz Brier
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Abstract
The present disclosure is directed to peptide-polymer conjugates utilizing hydrophilic linkers, and their use in treating diseases or disorders. In one embodiment, the present invention provides a conjugate of Formula I: (X—Y)n-Z Formula (I) wherein each X is independently a peptide having a molecular weight of from about 5 kDa to about 200 kDa; each Y is independently a hydrophilic linker; Z is a biocompatible polymer having a molecular weight of from about 0.1 MDa to about 3 MDa; and subscript n is an integer from 10 to 1000.
Claims18
A conjugate of Formula I:
- (
- X
- -
- Y
- )
- n
- -
- Z
- Formula
-
- (
- I
- )
- wherein
- each X is independently a peptide, wherein the peptide is an antibody or a DARPin;
- each Y is independently a hydrophilic linker, wherein the hydrophilic linker corresponds to any one of the following:
- 1-[3-({[2-(3-Hydrazino-3-oxopropoxy)ethoxy]methyl}amino)-3-oxopropyl]-1H-pyrrole-2,5-dione,
- 1-(3-{2-[2-(3-Hydrazino-3-oxopropoxy)ethoxy]ethylamino}-3-oxopropyl)-1H-pyrrole-2,5-dione, or
- 1-[3-(2-{2-[2-(2-Aminoethoxy)ethoxy]ethoxy}ethylamino)-3-oxopropyl]-1H-pyrrole-2,5-dione;
- Z is a biocompatible polymer having a molecular weight of from about 0.8 MDa to about 3 MDa, wherein the biocompatible polymer is hyaluronic acid;
- and
- subscript n is an integer from 10 to 1000.
19 more elements
Dependencies are inferred from the claim text.