DEGRADERS OF GRK2 AND USES THEREOF

Provided herein are compounds (e.g., compounds of Formulae (A-I), (B-I), (C-I)), and pharmaceutically acceptable salts, stereoisomers, tautomers, isotopically labeled derivatives, solvates, hydrates, polymorphs, co-crystals, and prodrugs thereof, pharmaceutical compositions thereof, and kits compris...

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Main Authors Lefker, Bruce Allen, Robinson, Ralph P, Chekler, Eugene L. Piatnitski, Lantermann, Alexandra, Xu, Hua, Kysil, Volodymyr, Sarkar, Sourav, Piizzi, Grazia, Couto, Kiley Marie, Hurov, Jonathan Barry
Format Patent
LanguageEnglish
Published 30.05.2024
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:Provided herein are compounds (e.g., compounds of Formulae (A-I), (B-I), (C-I)), and pharmaceutically acceptable salts, stereoisomers, tautomers, isotopically labeled derivatives, solvates, hydrates, polymorphs, co-crystals, and prodrugs thereof, pharmaceutical compositions thereof, and kits comprising the same. The compounds provided herein are degraders of GRK2 proteins and are therefore useful for, e.g., treating and/or preventing diseases (e.g., cancer) in a subject, for inhibiting tumor growth in a subject, for inhibiting the activity of GRK2 and/or degrading a GRK2 protein in vitro or in vivo, etc. In certain embodiments, the compounds provided herein are selective for GRK2. Also provided herein are methods and synthetic intermediates useful in the preparation of compounds described herein.
Bibliography:Application Number: US202218273755