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US 8,846,941 B2Granted
Functionalized polymers
AssigneeQuiaPEG 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.
Claims35
A compound 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;
- 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 and Z2 are independently O;
- L is a divalent radical of an alkylene;
- M is a protected carboxyl moiety;
- R is selected from the group consisting of:
- a protecting group and a hydrophobic separation handle;
- R1 is absent or a hydrophobic separation handle;
- and
- wherein no more than one of R, R1, and G is a hydrophobic separation handle.
13 more elements
A preparation comprising a compound comprising a water-soluble, non-peptidic, and non-nucleotidic polymer backbone having at least one termini covalently bonded to a structure of formula (1):
- or a salt thereof,
- wherein:
- A is the point of bonding to the terminus of the polymer backbone;
- 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 and Z2 are independently O;
- L is a divalent radical of an alkylene;
- M is a protected carboxyl moiety;
- R is selected from the group consisting of:
- a protecting group and a hydrophobic separation handle;
- R1 is absent or a hydrophobic separation handle;
- provided that only one of R and R1 is a hydrophobic separation handle or the hydrophobicity of one of R or R1 is higher than the other;
- wherein said preparation comprises at least 50% by weight of said compound;
- and
- wherein no more than one of R, R1, and G is a hydrophobic separation handle.
15 more elements
A compound of formula (2):
- or a salt form thereof,
- wherein:
- polymer is a linear, water-soluble, non-peptidic, and non-nucleotidic polymer backbone, wherein each linking group is bonded at a different terminus of said polymer;
- E is O;
- and
- 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 and Z2 independently are O;
- Z3 and Z4 are independently selected from O and NH, wherein no more than one of Z3 and Z4 is NH;
- L is a divalent radical of a alkylene;
- L1 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 carboxyl moiety;
- M1 is selected from a protected group that when deprotected is reactive with a biologically active molecule, a group reactive with a biologically active molecule, or a detectable functional group;
- wherein M and M1 are different;
- R is a protecting group;
- R1 is absent, hydrogen, a protecting group, or an activating group;
- wherein when M1 is a protected group that when deprotected is reactive with a biologically active molecule, then R1 is a protecting group or a hydrophobic separation handle;
- wherein when M1 is a group reactive with a biologically active molecule, R1 is absent, hydrogen, or an activating group;
- and
- wherein when M1 is a detectable functional group, R1 is absent or hydrogen.
21 more elements
A preparation comprising a compound of formula (2):
- or a salt form thereof,
- wherein:
- polymer is a linear, water-soluble, non-peptidic, and non-nucleotidic polymer backbone, wherein each phosphonate-derived functional group is bonded at a different terminus of said polymer;
- E is O;
- and
- 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 and Z2 independently are O;
- Z3 and Z4 are independently selected from O and NH, wherein no more than one of Z3 and Z4 is NH;
- L is a divalent radical of a alkylene;
- L1 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 carboxyl moiety;
- M1 is selected from a protected group that when deprotected is reactive with a biologically active molecule, a group reactive with a biologically active molecule, or a detectable functional group;
- wherein M and M1 are different;
- R is a protecting group;
- R1 is absent, hydrogen, a protecting group, or an activating group;
- wherein when M1 is a protected group that when deprotected is reactive with a biologically active molecule, then R1 is a protecting group or a hydrophobic separation handle;
- wherein when M1 is a group reactive with a biologically active molecule, R1 is absent, hydrogen, or an activating group;
- and
- wherein when M1 is a detectable functional group, R1 is absent or hydrogen;
- and
- wherein said preparation comprises at least 50% by weight of said compound.
23 more elements
A compound of formula (3):
- or a salt form thereof,
- wherein:
- polymer is a linear, water-soluble, non-peptidic, and non-nucleotidic polymer backbone, wherein M2 and the phosphonate-derived functional group are bonded at a different terminus of said polymer;
- 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 and Z2 are independently O;
- L is a divalent radical of an alkylene;
- M is a protected carboxyl moiety;
- M2 is selected from O, S or NH;
- and
- R is a protecting group or a hydrophobic separation handle;
- R2 is hydrogen or a protecting group.
13 more elements
A preparation comprising a compound of formula (3):
- or a salt form thereof,
- wherein:
- polymer is a linear, water-soluble, non-peptidic, and non-nucleotidic polymer backbone, wherein M2 and the phosphonate-derived functional group are bonded at a different terminus of said polymer;
- E is O and 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 and Z2 are independently O;
- L is a divalent radical of an alkylene;
- M is a protected carboxyl moiety;
- M2 is selected from O, S or NH;
- and
- R is a protecting group or a hydrophobic separation handle;
- R2 is hydrogen or a protecting group;
- and
- wherein said preparation comprises at least 50% of said compound.
14 more elements
Dependencies are inferred from the claim text.