Azophenols as ERG oncogene inhibitors

Patent metadata

Field	Value
Publication number	US-10238639-B2
Application number	US-201615561626-A
Country	US
Kind code	B2
Filing date	Sep 9, 2016
Priority date	Sep 10, 2015
Publication date	Mar 26, 2019
Grant date	Mar 26, 2019

Abstract

Selective azophenol inhibitors of a wild type or an altered ERG protein expression are described, where the inhibitors represent a compound of Formula (I) or Formula (II)

wherein X, X 1 , X 2 , X 3 , X 4 and X 5 , R 1 through R 4 and R 9 are as described.

First claim

We claim:

1. A method for treating a disease associated with overexpression of wild type ERG protein, an altered ERG protein, ERG gene transcription or ERG mRNA translation selected from the group consisting of prostate cancer and colon cancer in a subject suffering therefrom, comprising administering to the subject a therapeutically effective amount of a compound selected from the group consisting of Compounds 1-7:

or a pharmaceutically acceptable salt thereof.

2. The method according to claim 1 , wherein the disease is prostate cancer.

3. The method according to claim 1 , wherein the disease is colon cancer.

4. The method according to claim 1 , wherein the compound is present in a pharmaceutical composition further comprising an excipient.

5. The method according to claim 1 , wherein the compound is Compound 1.

6. The method according to claim 1 , wherein the compound is Compound 2.

7. The method according to claim 1 , wherein the compound is Compound 3.

8. The method according to claim 1 , wherein the compound is Compound 4.

9. The method according to claim 1 , wherein the compound is Compound 5.

10. The method according to claim 1 , wherein the compound is Compound 6.

11. The method according to claim 1 , wherein the compound is Compound 7.

12. The method according to claim 5 , wherein the compound is present in a pharmaceutical composition further comprising an excipient.

13. The method according to claim 6 , wherein the compound is present in a pharmaceutical composition further comprising an excipient.

14. The method according to claim 7 , wherein the compound is present in a pharmaceutical composition further comprising an excipient.

15. The method according to claim 8 , wherein the compound is present in a pharmaceutical composition further comprising an excipient.

16. The method according to claim 9 , wherein the compound is present in a pharmaceutical composition further comprising an excipient.

17. The method according to claim 10 , wherein the compound is present in a pharmaceutical composition further comprising an excipient.

18. The method according to claim 11 , wherein the compound is present in a pharmaceutical composition further comprising an excipient.

Assignees

• Henry M Jackson Found Advancement Military Medicine Inc

Inventors

• Dobi Albert L
• Dalgard Clifton L
• Srivastava Shiv K

Classifications

• A61K31/4402

  only substituted in position 2, e.g. pheniramine, bisacodyl · CPC title

• C07C245/02

  Azo compounds, i.e. compounds having the free valencies of —N=N— groups attached to different atoms, e.g. diazohydroxides · CPC title

• C07C245/00

  Compounds containing chains of at least two nitrogen atoms with at least one nitrogen-to-nitrogen multiple bond (azoxy compounds C07C291/08) · CPC title

• C07C245/04

  with nitrogen atoms of azo groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings · CPC title

• A61P35/00

  Antineoplastic agents · CPC title