IP Library Granted Patent US 10,308,596
Granted Patent B2
US 10,308,596 · App. 15/042,012 · Granted Jun 4, 2019

HDAC8 inhibitors for treating cancer

Inventors: Ya-Huei Kuo (Duarte, CA); Wei-Jan Huang (Taipei, TW); Chung-I Chang (Taipei, TW)
Assignees: CITY OF HOPE; TAIPEI MEDICAL UNIVERSITY; ACADEMIA SINICA
C07C259/06C07D209/08C07D209/18C07D213/56C07D213/74C07D215/14C07D217/16C07D217/20C07D307/91C07D317/60C07D333/24
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Quick Facts
Patent No.
US 10,308,596
App. No.
15/042,012
Granted
Jun 4, 2019
Kind
B2
Abstract

Provided herein, inter alia, are compound and methods of treating cancer by inhibiting HDAC8.

Claims (14)

1. A compound having the formula (I):

wherein:

R 1 is substituted or unsubstituted 2 to 20 membered heteroalkyl, substituted or unsubstituted C 3 -C 7 cycloalkyl, substituted or unsubstituted 3 to 7 membered heterocycloalkyl, substituted or unsubstituted C 3 -C 7 aryl, or substituted or unsubstituted 3 to 7 membered heteroaryl; and

R 2 is substituted or unsubstituted C 1 -C 20 alkyl, substituted or unsubstituted 2 to 20 membered heteroalkyl, substituted or unsubstituted C 3 -C 7 cycloalkyl, substituted or unsubstituted 3 to 7 membered heterocycloalkyl, substituted or unsubstituted C 3 -C 7 aryl, or substituted or unsubstituted 3 to 7 membered heteroaryl.

2. The compound of claim 1 , wherein R 1 is substituted or unsubstituted C 1 -C 4 alkoxy and R 2 is a substituted or unsubstituted C 4 -C 6 aryl.

3. The compound of claim 2 , wherein R 1 is unsubstituted C 1 -C 2 alkoxy and R 2 is unsubstituted C6 aryl.

4. The compound of claim 1 , wherein the compound has formula (II):

5. A compound selected from the group consisting of:

6. A method of inhibiting HDAC8 mediated deacetylation of p53, the method comprising contacting HDAC8 with the compound of claim 1 in the presence of p53, thereby inhibiting HDAC8 deacetylation of p53.

7. A method of activating p53 in vivo, the method comprising contacting a cell with the compound of claim 1 in the presence of HDAC8; wherein the cell is an AML cell.

8. The method of claim 7 , wherein the AML cell is an AML stem cell.

9. The compound of claim 1 , wherein:

R 1 is substituted or unsubstituted 2 to 20 membered heteroalkyl, substituted or unsubstituted C 3 -C 7 cycloalkyl, substituted or unsubstituted 3 to 7 membered heterocycloalkyl, substituted or unsubstituted C 6 -C 7 aryl, or substituted or unsubstituted 3 to 7 membered heteroaryl; and

R 2 is substituted or unsubstituted C 1 -C 20 alkyl, substituted or unsubstituted 2 to 20 membered heteroalkyl, substituted or unsubstituted C 3 -C 7 cycloalkyl, substituted or unsubstituted 3 to 7 membered heterocycloalkyl, substituted or unsubstituted C 6 -C 7 aryl, or substituted or unsubstituted 3 to 7 membered heteroaryl.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 30, 2018
From: CHANG, CHUNG-I
To: ACADEMIA SINICA
Reel/Frame 045938/0042 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 30, 2018
From: HUANG, WEI-JAN
To: TAIPEI MEDICAL UNIVERSITY
Reel/Frame 045938/0061 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 30, 2018
From: KUO, YA-HUEI
To: CITY OF HOPE
Reel/Frame 046268/0025 →
Continuity (4)
Continuation PCTUS2014051876 · Aug 20, 2014
Provisional Application 61868073 · Aug 20, 2013
Related Publication 20160237027A1 · Aug 18, 2016
Related Publication 20170050922A2 · Feb 23, 2017