Invention Grant
- Patent Title: Antiestrogen compounds
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Application No.: US17251771Application Date: 2019-06-11
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Publication No.: US11667621B2Publication Date: 2023-06-06
- Inventor: Abhishek Sharma , Sarat Chandarlapaty , Lucia Wang , Shengjia Lin , Weiyi Toy , John Katzenellenbogen
- Applicant: STEVENS INSTITUTE OF TECHNOLOGY , MEMORIAL SLOAN-KETTERING CANCER CENTER , THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
- Applicant Address: US NJ Hoboken
- Assignee: STEVENS INSTITUTE OF TECHNOLOGY,THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS,MEMORIAL SLOAN-KETTERING CANCER CENTER
- Current Assignee: STEVENS INSTITUTE OF TECHNOLOGY,THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS,MEMORIAL SLOAN-KETTERING CANCER CENTER
- Current Assignee Address: US NJ Hoboken; US IL Urbana; US NY New York
- Agency: Lewis Roca Rothgerber Christie LLP
- International Application: PCT/US2019/036526 2019.06.11
- International Announcement: WO2019/241231A 2019.12.19
- Date entered country: 2020-12-11
- Main IPC: C07D401/04
- IPC: C07D401/04 ; C07C233/20 ; C07C233/21 ; C07D209/12 ; C07D333/64 ; C07D409/14

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.
Public/Granted literature
- US20210130320A1 ANTIESTROGEN COMPOUNDS Public/Granted day:2021-05-06
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