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US 10,781,286 B2Granted
Functionalized polymers
AssigneeQuiaPEG Pharmaceuticals AB
InventorMarek Kwiatkowski
Life of this patent
Estimating the term…
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.
Claims20
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 (1):
- 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);
- E is O;
- K is selected from the group consisting of:
- alkylene, alkyleneoxyalkylene, and oligomeric alkyleneoxyalkylene;
- G is selected from the group consisting of:
- hydrogen, alkoxy, and a hydrophobic separation handle;
- Z1 is O;
- Z2 is O;
- L is selected from the group consisting of:
- a divalent radical of a nucleoside, alkylene, alkyleneoxyalkylene, oligomeric alkyleneoxyalkylene, and unsubstituted and substituted arylene;
- R1 is absent or a hydrophobic separation handle;
- M is a biologically active molecule;
- and
- R is absent.
13 more elements
A conjugate, or a pharmaceutically acceptable salt thereof, comprising a compound of formula (2):
- or a salt form thereof,
- wherein:
- polymer is a linear poly(ethylene glycol), wherein each linking group is bonded at a different terminus of said poly(ethylene glycol);
- E is O;
- E1 is O or S;
- K and K1 are independently selected from the group consisting of:
- alkylene, alkyleneoxyalkylene, and oligomeric alkyleneoxyalkylene;
- G and G1 are independently absent or are selected from the group consisting of:
- alkoxy and a hydrophobic separation handle;
- Z1 is O;
- Z2 is O;
- Z3 and Z4 are independently selected from 0 and NH, wherein no more than one of Z3 and Z4 is NH;
- L is a divalent radical of an alkylene;
- L1 is selected from the group consisting of:
- a divalent radical of a nucleoside, alkylene, alkyleneoxyalkylene, oligomeric alkyleneoxyalkylene, and unsubstituted and substituted arylene;
- R and R1 are absent;
- M is a biologically active molecule;
- and
- M1 is a biologically active molecule.
16 more elements
A conjugate, or a pharmaceutically acceptable salt thereof, comprising a compound of formula (3):
- or a salt form thereof,
- wherein:
- polymer is a linear poly(ethylene glycol), wherein M2 and the phosphonate-derived functional group are bonded at a different terminus of said poly(ethylene glycol);
- E is O;
- E1 is O or S;
- K is selected from the group consisting of:
- alkylene, alkyleneoxyalkylene, and oligomeric alkyleneoxyalkylene;
- G is selected from the group consisting of:
- hydrogen, alkoxy, and a hydrophobic separation handle;
- Z1 is O;
- Z2 is O;
- L is selected from the group consisting of:
- a divalent radical of nucleoside, alkylene, alkyleneoxyalkylene, oligomeric alkyleneoxyalkylene, and unsubstituted and substituted arylene;
- M is a biologically active molecule;
- M2 is selected from O, S or NH;
- and
- R is absent;
- and
- R2 is hydrogen or a protecting group.
16 more elements
Dependencies are inferred from the claim text.