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US 11,723,981 B2Granted
Conjugates of tumor necrosis factor inhibitors to functionalized polymers
AssigneeQuiaPEG Pharmaceuticals AB
InventorMarek Kwiatkowski
Life of this patent
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Abstract
This document relates to conjugates of TNF inhibitors or derivatives thereof and 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 conjugates.
Claims20
A method of making a TNF inhibitor conjugate, said method comprising reacting a TNF inhibitor with 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 each bonded at a different terminus of said polymer;
- E and E′ are each O;
- K is selected from:
- alkylene, alkyleneoxyalkylene, and oligomeric alkyleneoxyalkylene;
- G is selected from:
- hydrogen, alkoxy, and a hydrophobic separation handle;
- Z1 and Z2 are each O;
- L is selected from:
- a divalent radical of nucleoside, alkylene, alkyleneoxyalkylene, oligomeric alkyleneoxyalkylene, and unsubstituted and substituted arylene;
- M is selected from a protected group that when deprotected is reactive with the TNF inhibitor or a group reactive with the TNF inhibitor;
- M2 is O;
- and
- R is absent, a protecting group, a hydrophobic separation handle, or an activating group;
- R2 is hydrogen or a protecting group;
- wherein when M is a protected group that when deprotected is reactive with the TNF inhibitor, then R is a protecting group or a hydrophobic separation handle;
- and
- wherein when M is a group reactive with a TNF inhibitor, R is absent, hydrogen, or an activating group.
15 more elements
Dependencies are inferred from the claim text.