Endotarget Inc.

Xianyou Peng

Guangdi Wang

Hongjoong Kim

Borui Kang

The present disclosure relates to compounds having the structure of Formula (I) that serve as degraders (and/or inhibitors) of Bruton's tyrosine kinase (BTK). In the present disclosure, the said compounds, which contain a target protein (BTK) binding moiety and a E3 ubiquitin ligase (CRBN) binding moiety, are directed to bind to both the BTK and CRBN, such that the BTK is placed in close proximity to the E3 ligase to mediate ubiquitylation of the target protein followed by degradation of the target protein by the proteasome. The present disclosure provides methods for synthesizing the herein disclosed said compounds, and their pharmacological activities associated with degradation or inhibition of the target protein. Further, the present disclosure teaches the utilization of such compounds in a treatment for proliferative diseases and autoimmune disorders, including hematological cancers and rheumatoid arthritis, particularly non-Hodgkin lymphoma, and especially chronic lymphocytic leukemia (CLL) and mantle cell lymphoma.

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New Orleans, LA, United States of America

Xianyou Peng