Back to results
US 2024/0075151 A1Published application
Conjugates of tumor necrosis factor inhibitors to functionalized polymers
AssigneeQuiaPEG Pharmaceuticals AB
InventorMarek Kwiatkowski
Life of this patent
Estimating the term…
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.
Claims21
(canceled)
A preparation comprising a compound of formula (2):
- or a salt 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;
- M and M1 are independently selected from a protected group that when deprotected is reactive with a TNF inhibitor or said derivative or a group reactive with a TNF inhibitor or said derivative, wherein M and M1 are different;
- and
- R and R1 are independently absent, hydrogen, a protecting group, or an activating group;
- wherein when M is a protected group that when deprotected is reactive with a TNF inhibitor or said derivative, then R is a protecting group or a hydrophobic separation handle;
- wherein when M is a group reactive with a TNF inhibitor or said derivative, R is absent, hydrogen, or an activating group;
- wherein when M1 is a protected group that when deprotected is reactive with a TNF inhibitor or said derivative, then R1 is a protecting group or a hydrophobic separation handle;
- and
- wherein when M1 is a group reactive with a TNF inhibitor or said derivative, R1 is absent, hydrogen, or an activating group.
15 more elements
Dependencies are inferred from the claim text.