Triazolopyrazine

Patent metadata

Field	Value
Publication number	US-11077107-B2
Application number	US-201916389062-A
Country	US
Kind code	B2
Filing date	Apr 19, 2019
Priority date	Nov 16, 2012
Publication date	Aug 3, 2021
Grant date	Aug 3, 2021

Abstract

Disclosed are compounds of the formula (I)

wherein the groups R 1 to R 3 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.

First claim

The invention claimed is:

1. A compound of the formula:

2. A pharmaceutically acceptable salt of a compound of the formula:

3. A method for inhibiting bromodomain protein 4 activity in a patient, comprising administering to the patient a therapeutically effective amount of a compound according to claim 1 .

4. The method according to claim 3 , wherein the patient has a cancer selected from the group consisting of lung cancer, liver cancer, colon cancer, brain cancer, thyroid cancer, pancreatic cancer, breast cancer, ovarian cancer and prostate cancer.

5. A method for inhibiting bromodomain protein 4 activity in a patient, comprising administering to the patient a therapeutically effective amount of a pharmaceutically acceptable salt according to claim 2 .

6. The method according to claim 5 , wherein the patient has a cancer selected from the group consisting of lung cancer, liver cancer, colon cancer, brain cancer, thyroid cancer, pancreatic cancer, breast cancer, ovarian cancer and prostate cancer.

7. A compound of the formula:

8. A pharmaceutically acceptable salt of a compound of the formula:

9. A method for inhibiting bromodomain protein 4 activity in a patient, comprising administering to the patient a therapeutically effective amount of a compound according to claim 7 .

10. The method according to claim 9 , wherein the patient has a cancer selected from the group consisting of lung cancer, liver cancer, colon cancer, brain cancer, thyroid cancer, pancreatic cancer, breast cancer, ovarian cancer and prostate cancer.

11. A method for inhibiting bromodomain protein 4 activity in a patient, comprising administering to the patient a therapeutically effective amount of a pharmaceutically acceptable salt according to claim 8 .

12. The method according to claim 11 , wherein the patient has a cancer selected from the group consisting of lung cancer, liver cancer, colon cancer, brain cancer, thyroid cancer, pancreatic cancer, breast cancer, ovarian cancer and prostate cancer.

13. A compound of the formula:

14. A pharmaceutically acceptable salt of a compound of the formula:

15. A method for inhibiting bromodomain protein 4 activity in a patient, comprising administering to the patient a therapeutically effective amount of a compound according to claim 13 .

16. The method according to claim 15 , wherein the patient has a cancer selected from the group consisting of lung cancer, liver cancer, colon cancer, brain cancer, thyroid cancer, pancreatic cancer, breast cancer, ovarian cancer and prostate cancer.

17. A method for inhibiting bromodomain protein 4 activity in a patient, comprising administering to the patient a therapeutically effective amount of a pharmaceutically acceptable salt according to claim 14 .

18. The method according to claim 17 , wherein the patient has a cancer selected from the group consisting of lung cancer, liver cancer, colon cancer, brain cancer, thyroid cancer, pancreatic cancer, breast cancer, ovarian cancer and prostate cancer.

19. A compound of the formula:

20. A pharmaceutically acceptable salt of a compound of the formula:

21. A method for inhibiting bromodomain protein 4 activity in a patient, comprising administering to the patient a therapeutically effective amount of a compound according to claim 19 .

22. The method according to claim 21 , wherein the patient has a cancer selected from the group consisting of lung cancer, liver cancer, colon cancer, brain cancer, thyroid cancer, pancreatic cancer, breast cancer, ovarian cancer and prostate cancer.

23. A method for inhibiting bromodomain protein 4 activity in a patient, comprising administering to the patient a therapeutically effective amount of a pharmaceutically acceptable salt according to claim 20 .

24. The method according to claim 23 , wherein the patient has a cancer selected from the group consisting of lung cancer, liver cancer, colon cancer, brain cancer, thyroid cancer, pancreatic cancer, breast cancer, ovarian cancer and prostate cancer.

25. A compound of the formula:

26. A pharmaceutically acceptable salt of a compound of the formula:

27. A method for inhibiting bromodomain protein 4 activity in a patient, comprising administering to the patient a therapeutically effective amount of a compound according to claim 25 .

28. The method according to claim 27 , wherein the patient has a cancer selected from the group consisting of lung cancer, liver cancer, colon cancer, brain cancer, thyroid cancer, pancreatic cancer, breast cancer, ovarian cancer and prostate cancer.

29. A method for inhibiting bromodomain protein 4 activity in a patient, comprising administering to the patient a therapeutically effective amount of a pharmaceutically acceptable salt according to claim 26 .

30. The method according to claim 29 , wherein the patient has a cancer selected from the group consisting of lung cancer, liver cancer, colon cancer, brain cancer, thyroid cancer, pancreatic cancer, breast cancer, ovarian cancer and prostate cancer.

31. A compound of the formula:

32. A pharmaceutically acceptable salt of a compound of the formula:

33. A method for inhibiting bromodomain protein 4 activity in a patient, comprising administering to the patient a therapeutically effective amount of a compound according to claim 31 .

34. The method according to claim 33 , wherein the patient has a cancer selected from the group consisting of lung cancer, liver cancer, colon cancer, brain cancer, thyroid cancer, pancreatic cancer, breast cancer, ovarian cancer and prostate cancer.

35. A method for inhibiting bromodomain protein 4 activity in a patient, comprising administering to the patient a therapeutically effective amount of a pharmaceutically acceptable salt according to claim 32 .

36. The method according to claim 35 , wherein the patient has a cancer selected from the group consisting of lung cancer, liver cancer, colon cancer, brain cancer, thyroid cancer, pancreatic cancer, breast cancer, ovarian cancer and prostate cancer.

Assignees

• Boehringer Ingelheim Int

Inventors

• Engelhardt Harald
• Gianni Davide
• Smethurst Christian

Classifications

• C07C211/50

  with at least two amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton · CPC title

• A61K31/52

  Purines, e.g. adenine · CPC title

• C07D237/04

  having less than three double bonds between ring members or between ring members and non-ring members · CPC title

• A61K31/501

  not condensed and containing further heterocyclic rings · CPC title

• A61K31/519

  ortho- or peri-condensed with heterocyclic rings · CPC title