The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Nov. 12, 2024

Filed:

Aug. 17, 2022
Applicants:

Endotarget Inc., New Orleans, LA (US);

Enhancedbio Inc., Seoul, KR;

Inventors:

Guangdi Wang, New Orleans, LA (US);

Xianyou Peng, New Orleans, LA (US);

Borui Kang, New Orleans, LA (US);

HongJoong Kim, Seoul, KR;

Assignee:
Attorney:
Primary Examiner:
Int. Cl.
CPC ...
A61K 31/519 (2006.01); C07D 487/04 (2006.01);
U.S. Cl.
CPC ...
C07D 487/04 (2013.01);
Abstract

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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