Invention Grant
- Patent Title: Bivalent bromodomain inhibitors and uses thereof
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Application No.: US15778831Application Date: 2016-11-23
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Publication No.: US10913752B2Publication Date: 2021-02-09
- Inventor: James E. Bradner , Jun Qi , Minoru Tanaka , Justin M. Roberts
- Applicant: Dana-Farber Cancer Institute, Inc.
- Applicant Address: US MA Boston
- Assignee: Dana-Farber Cancer Institute, Inc.
- Current Assignee: Dana-Farber Cancer Institute, Inc.
- Current Assignee Address: US MA Boston
- Agency: Wolf, Greenfield & Sacks, P.C.
- International Application: PCT/US2016/063502 WO 20161123
- International Announcement: WO2017/091673 WO 20170601
- Main IPC: C07D519/00
- IPC: C07D519/00 ; A61K31/551 ; A61P15/16

Abstract:
The present invention provides bivalent inhibitors of BET bromodomains, such as compounds of Formulae (I), (II), (III), (IV), (V), and (VI). Some bromdomain-containing proteins (e.g., BRD4) have a tandem bromodomain primary structure comprising more than one bromodomain binding site (e.g., BRD4 comprises BD1 and BD2). Bivalent inhibitors of BET bromodomains provided herein can target bromodomains through advantageous multivalent interactions, and can therefore can be to treat diseases or conditions associated with bromodomain-containing proteins. The present also provides pharmaceutical compositions and kits comprising the inventive compounds, as well as methods of using the inventive compounds.
Public/Granted literature
- US20200172553A9 BIVALENT BROMODOMAIN INHIBITORS AND USES THEREOF Public/Granted day:2020-06-04
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