IP Library Granted Patent US 9,745,613
Granted Patent B2
US 9,745,613 · App. 14/805,867 · Granted Aug 29, 2017

Compounds, substrates and methods related to histone deacetylases

Inventors: Edward Holson (Newton, MA); David Olson (Boston, MA)
Assignee: The Broad Institute, Inc.
C12Q1/34A61K31/00A61K31/185A61K31/365A61K31/397A61K31/404A61K31/4192A61K31/4439A61K31/495C07D209/08C07K7/06G01N2333/98
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Quick Facts
Patent No.
US 9,745,613
App. No.
14/805,867
Granted
Aug 29, 2017
Kind
B2
Abstract

The invention relates to methods for the identification of compounds, peptides and proteins that can act as substrates for histone deacetylases. The invention further relates to compounds of Formula I: F 1 -X 1 -L 1 -X 2 -P 1 -X 3 -G 1   (Formula I) The invention relates to the treatment of diseases or disorders mediated by ARID1A (BAF250A).

Claims (10)

1. A compound of Formula II:

or a pharmaceutically acceptable salt or ester thereof;

wherein R 1 is selected from halogen, C 1 -C 6 alkyl, substituted C 1 -C 6 alkyl, C 1 -C 6 alkenyl, substituted C 1 -C 6 alkenyl, C 1 -C 6 alkynyl and substituted C 1 -C 6 alkynyl; and,

R 2 is selected from —O—C 1 -C 6 alkyl, substituted —O—C 1 -C 6 alkyl, —SC 1 -C 6 alkyl and substituted —SC 1 -C 6 alkyl.

2. The compound of claim 1 having the formula:

or a pharmaceutically acceptable salt or ester thereof;

wherein R 1 is selected from the group consisting of F, Cl, I, methyl, ethyl, propyl, isopropyl, n-butyl, t-butyl and CF 3 ; and

R 2 is OCH 3 or —OCH 2 CH 3 .

3. The compound of claim 1 having the formula:

or a pharmaceutically acceptable salt thereof.

Assignments (2)
CONFIRMATORY LICENSE Recorded Aug 3, 2017
From: BROAD INSTITUTE, INC
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 043420/0271 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 29, 2016
From: HOLSON, EDWARD; OLSON, DAVID
To: THE BROAD INSTITUTE, INC.
Reel/Frame 038119/0846 →
Continuity (2)
Provisional Application 62027776 · Jul 22, 2014
Related Publication 20160060679A1 · Mar 3, 2016