Proteolysis Targeting Chimera Compounds and Methods of Preparing and Using Same

摘要

The present invention includes novel compounds and methods for preventing or treating diseases associated with and/or caused by overexpression and/or uncontrolled activation of a tyrosine kinase in a subject in need thereof. In certain embodiments, the compounds of the present invention comprise a tyrosine kinase inhibitor, a linker and a ubiquitin ligase binder. The methods of the present invention comprise administering to the subject an pharmaceutically effective amount of at least one compound of the invention.

主权项

1. A compound of formula (I):
TKI-L-(ULM)k  (I), wherein: TKI is a tyrosine kinase inhibitor, L is a linker, each ULM is independently a ubiquitin ligase binder, and k is an integer ranging from 1 to 4,wherein TKI is covalently linked to L and wherein each ULM is covalently linked to L;or a salt, enantiomer, stereoisomer, solvate, polymorph or N-oxide thereof.