Cytotoxicity targeting chimeras for cxcr3-expressing cells
AssigneeGlaxoSmithKline Intellectual Property Development Limited
InventorsBrandon James Turunen, Cunyu Zhang
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Abstract
The present disclosure relates to heterobifunctional molecules, referred to as cytotoxicity targeting chimeras (CyTaCs) or antibody recruiting molecules (ARMs) that are able to simultaneously bind a target cell-surface protein as well as an exogenous antibody protein. The present disclosure also relates to agents capable of binding to a receptor on a surface of a pathogenic cell and inducing the depletion of the pathogenic cell in a subject for use in the treatment of cancer, inflammatory diseases, or autoimmune diseases.
Claims29
A compound of Formula (I):
- or a pharmaceutically acceptable salt thereof,
- wherein:
- R1 is C1-4 alkyl or C3-6 cycloalkyl;
- L is a divalent linker of Formula (L-a) or (L-e):
- or a stereoisomer thereof,
- wherein:
- Ring A and Ring B are each independently C4-6 cycloalkylene;
- L1a is C3-5 linear alkylene, wherein 1 or 2 methylene units are replaced with —O— or —NRa—;
- each Ra is independently hydrogen or C1-3 alkyl;
- and
- L2a is —O—, —NHC(O)—, or —CH2—O—;
- or
- wherein n is an integer of 3 to 50;
- wherein each represents a covalent bond to the Y group of Formula (I), or when Y is a bond, a covalent bond to the N atom of Formula (I), and each represents a covalent bond to the methylene group of Formula (I);
- and
- Y is a bond or a divalent spacer moiety of one to twelve atoms in length.
A compound selected from the group consisting of:
- or a pharmaceutically acceptable salt thereof.
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Dependencies are inferred from the claim text.