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US 10,207,007 B2Granted
Conjugates of tumor necrosis factor inhibitors to functionalized polymers
AssigneeQuiaPEG Pharmaceuticals AB
InventorMarek Kwiatkowski
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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 conjugate, or a pharmaceutically acceptable salt thereof, comprising a structure of formula (10):
- 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 and E1 are independently 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;
- each pair of Z1 and Z2 and Z3 and Z4 are independently selected from O and NH, wherein only one of each pair of Z1 and Z2 and Z3 and Z4 can be NH;
- L and L1 are independently selected from the group consisting of:
- a divalent radical of a nucleoside, alkylene, alkyleneoxyalkylene, oligomeric alkyleneoxyalkylene, and unsubstituted and substituted arylene;
- L2 is a covalent linking moiety between L on the polymer backbone and B;
- L3 is a covalent linking moiety between L on the polymer backbone and B1;
- and
- B and B1 are independently a TNF inhibitor, a derivative of a TNF inhibitor, a biologic other than a TNF inhibitor, a drug, a detectable group, a separation moiety, wherein at least one of B and B1 is a TNF inhibitor or a derivative of a TNF inhibitor.
12 more elements
Dependencies are inferred from the claim text.