Chromobox protein inhibitors and uses thereof

Patent metadata

Field	Value
Publication number	US-12129248-B2
Application number	US-201716335951-A
Country	US
Kind code	B2
Filing date	Sep 25, 2017
Priority date	Sep 26, 2016
Publication date	Oct 29, 2024
Grant date	Oct 29, 2024

Abstract

Provided herein are compounds useful as inhibitors of CBX. Also described are pharmaceutical compositions and medical uses of these compounds.

First claim

The invention claimed is:

1. A compound having a structure of Formula I or a pharmaceutically acceptable salt thereof:

wherein
R 1 is

R 2 is H, halo, optionally substituted aryl, or optionally substituted heteroaryl;
L 1 is optionally substituted —C(O)NH-alkylene- or —C(O)NHNCH—; and

A is

2. The compound of claim 1 , wherein R 1 is

3. The compound of claim 1 , wherein R 2 is Br.

4. The compound of claim 1 , wherein R 2 is

5. The compound of claim 1 , wherein L 1 is

6. The compound of claim 5 , wherein L 1 -A is

7. The compound of claim 1 , wherein L 1 is

8. The compound of claim 7 , wherein L 1 -A is

9. A compound selected from

or a pharmaceutically acceptable salt thereof.

10. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.

Assignees

• Dana Farber Cancer Inst Inc

Inventors

• Bradner James
• Qi Jun
• Federation Alexander
• Jacobson Zoe
• Varca Anthony

Classifications

• C07D471/04

  Ortho-condensed systems · CPC title

• C07D417/14

  containing three or more hetero rings · CPC title

• C07D405/04

  directly linked by a ring-member-to-ring-member bond · CPC title

• C07D277/54

  Nitrogen and either oxygen or sulfur atoms · CPC title

• A61P35/00

  Antineoplastic agents · CPC title