Dihydrobenzimidazolones for medical treatment

Patent metadata

Field	Value
Publication number	US-11787802-B2
Application number	US-202217576582-A
Country	US
Kind code	B2
Filing date	Jan 14, 2022
Priority date	Sep 4, 2017
Publication date	Oct 17, 2023
Grant date	Oct 17, 2023

Abstract

The present invention provides selected dihydrobenzimidazolones which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.

First claim

We claim:

1. A method for the treatment of a cancer in a human responsive to a cereblon-binding drug therapy comprising administering an effective amount of a compound or a pharmaceutically acceptable salt thereof to a human patient wherein the compound is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein the compound is selected from the group consisting of

or a pharmaceutically acceptable salt thereof.

3. The method of claim 1 , wherein the compound is selected from the group consisting of

or a pharmaceutically acceptable salt thereof.

4. The method of claim 1 , wherein the compound is selected from the group consisting of

or a pharmaceutically acceptable salt thereof.

5. The method of claim 1 , wherein the compound is selected from the group consisting of

or a pharmaceutically acceptable salt thereof.

6. The method of claim 1 , wherein the compound is selected from the group consisting of

or a pharmaceutically acceptable salt thereof.

7. The method of claim 1 , wherein the compound is selected from the group consisting of

or a pharmaceutically acceptable salt thereof.

8. The method of claim 1 , wherein the compound is selected from the group consisting of

or a pharmaceutically acceptable salt thereof.

9. A method for the treatment of a cancer in a human responsive to a cereblon-binding drug therapy comprising administering an effective amount of a compound or a pharmaceutically acceptable salt thereof to a human patient wherein the compound is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

10. The method of claim 9 , wherein the compound is selected from the group consisting of

or a pharmaceutically acceptable salt thereof.

11. The method of claim 9 , wherein the compound is selected from the group consisting of

or a pharmaceutically acceptable salt thereof.

12. The method of claim 9 , wherein the compound is selected from the group consisting of

or a pharmaceutically acceptable salt thereof.

13. The method of claim 9 , wherein the compound is selected from the group consisting of

or a pharmaceutically acceptable salt thereof.

14. A method for the treatment of a cancer in a human responsive to a cereblon-binding drug therapy comprising administering an effective amount of a compound or a pharmaceutically acceptable salt thereof to a human patient wherein the compound is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

15. The method of claim 14 , wherein the compound is selected from the group consisting of

or a pharmaceutically acceptable salt thereof.

16. The method of claim 14 , wherein the compound is selected from the group consisting of

or a pharmaceutically acceptable salt thereof.

17. The method of claim 14 , wherein the compound is selected from the group consisting of

or a pharmaceutically acceptable salt thereof.

18. The method of claim 14 , wherein the compound is selected from the group consisting of

or a pharmaceutically acceptable salt thereof.

19. The method of claim 14 , wherein the compound is selected from the group consisting of

or a pharmaceutically acceptable salt thereof.

Assignees

• C4 Therapeutics Inc

Inventors

• Norcross Roger
• Goergler Annick
• Dey Fabian
• Kusznir Eric Andre

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• C07D487/08

  Bridged systems · CPC title

• C07D403/04

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

• C07D417/04

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

• C07D401/04

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