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US 2021/0230144 A1Published application
Irak degraders and uses thereof
AssigneeDana-Farber Cancer Institute, Inc.
InventorsNathanael S. Gray, John Hatcher
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Abstract
The present invention relates to heterobifunctional compounds (degraders), compositions and methods for treating diseases or conditions mediated by Interleukin Receptor-Associated Kinases (IRAKs).
Claims25
A bifunctional compound having a structure represented by formula I:
- wherein the targeting ligand represents a moiety that binds Interleukin-1 receptor kinase 1 (IRAK1), interleukin-1 receptor kinase 4 (IRAK4) or both IRAK1 and IRAK4 (IRAK/4), the degron represents a moiety that binds an E3 ubiquitin ligase, and the linker represents a moiety that covalently connects the degron and the targeting ligand, or a pharmaceutically acceptable salt or stereoisomer thereof.
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A bifunctional compound, which is represented by any one of structures 1-6:
- or a pharmaceutically acceptable salt or stereoisomer thereof.
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Dependencies are inferred from the claim text.