Functionalized polymers
AssigneeQuiaPEG Pharmaceuticals AB
InventorMarek Kwiatkowski
Life of this patent
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Abstract
This document relates to functionalized (e.g., mono- or bi-functional) polymers (e.g., polyethylene glycol and related polymers) as well as methods and materials for making and using such functionalized polymers.
Claims19
A conjugate, or a pharmaceutically acceptable salt thereof, comprising a water-soluble, non-peptidic, and non-nucleotidic polymer backbone having at least one terminus covalently bonded to a structure of formula (7):
- wherein:
- A is the point of covalent bonding to the terminus of the polymer backbone, wherein the polymer backbone is poly(ethylene glycol), wherein said poly(ethylene glycol) has an average molecular weight from about 500 Da to about 100,000 Da;
- E is O;
- Y represents an optionally substituted residue selected from the group consisting of alkyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl;
- Z1 and Z2 are O;
- L is selected from the group consisting of:
- a divalent radical of a nucleoside, alkylene, alkyleneoxyalkylene, oligomeric alkyleneoxyalkylene, and unsubstituted and substituted arylene;
- and
- M is a biologically active molecule or a detectable functional group.
A method of preparing a conjugate, or a pharmaceutically acceptable salt thereof, comprising a water-soluble, non-peptidic, and non-nucleotidic polymer backbone having at least one terminus covalently bonded to a structure of formula (7):
- or a salt thereof,
- wherein:
- A is the point of covalent bonding to the terminus of the polymer backbone, wherein the polymer backbone is poly(ethylene glycol), wherein said poly(ethylene glycol) has an average molecular weight from about 500 Da to about 100,000 Da;
- E is O;
- Y represents an optionally substituted residue selected from the group consisting of alkyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl;
- Z1 and Z2 are O;
- L is selected from the group consisting of:
- a divalent radical of a nucleoside, alkylene, alkyleneoxyalkylene, oligomeric alkyleneoxyalkylene, and unsubstituted and substituted arylene;
- and
- M is a biologically active molecule;
- comprising the steps of:
- (a) providing a compound of formula (8):
- wherein:
- A is the point of covalent bonding to the terminus of the polymer backbone, wherein the polymer backbone is poly(ethylene glycol), wherein said poly(ethylene glycol) has an average molecular weight from about 500 Da to about 100,000 Da;
- E is O;
- Y represents an optionally substituted residue selected from the group consisting of alkyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl;
- Z1 and Z2 are O;
- L is selected from the group consisting of:
- a divalent radical of a nucleoside, alkylene, alkyleneoxyalkylene, oligomeric alkyleneoxyalkylene, and unsubstituted and substituted arylene
- M is a protected group that when deprotected is reactive with a biologically active molecule;
- R is a hydrophobic separation handle;
- R1 is absent or a hydrophobic separation handle;
- (b) removing the hydrophobic separation handle(s);
- (c) optionally reacting the compound obtained in step (b) with an activating agent;
- and
- (d) reacting the compound obtained in step (b), or, optionally in step (c), with a biologically active molecule to prepare the conjugate.
Dependencies are inferred from the claim text.