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:
Jun. 06, 2023

Filed:

Jun. 11, 2019
Applicants:

Stevens Institute of Technology, Hoboken, NJ (US);

Memorial Sloan-kettering Cancer Center, New York, NY (US);

The Board of Trustees of the University of Illinois, Urbana, IL (US);

Inventors:

Abhishek Sharma, Edison, NJ (US);

Sarat Chandarlapaty, New York, NY (US);

Lucia Wang, Jersey City, NJ (US);

Shengjia Lin, Secaucus, NJ (US);

Weiyi Toy, New York, NY (US);

John Katzenellenbogen, Urbana, IL (US);

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 401/04 (2006.01); C07C 233/20 (2006.01); C07C 233/21 (2006.01); C07D 209/12 (2006.01); C07D 333/64 (2006.01); C07D 409/14 (2006.01);
U.S. Cl.
CPC ...
C07D 401/04 (2013.01); C07C 233/20 (2013.01); C07C 233/21 (2013.01); C07D 209/12 (2013.01); C07D 333/64 (2013.01); C07D 409/14 (2013.01);
Abstract

A genus of proteolysis-targeting chimeras (PROTACs)-type compounds/antiestrogens has now been found that act as selective estrogen receptor degraders (SERDs) and estrogen receptor antagonists by degrading and antagonizing ERa in breast cancer cells. The compounds are of the following genus: The compounds described herein exhibit anti-proliferative effects, and are potentially useful, alone or in combination with other therapies, for the treatment of breast cancer. In general, these compounds combine a tight binding ERa targeting ligand tethered to a recognition motif or degron. Once bound, the degron recruits destructive cellular components and the targeted receptor (i.e., ERa) is degraded (i.e., destroyed) or antagonized.


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