Methylquinazolinone derivatives

Patent metadata

Field	Value
Publication number	US-12116349-B2
Application number	US-202217835245-A
Country	US
Kind code	B2
Filing date	Jun 8, 2022
Priority date	Dec 10, 2019
Publication date	Oct 15, 2024
Grant date	Oct 15, 2024

Abstract

The invention provides a novel compound having the general formula (I)

or a pharmaceutically acceptable salt thereof. The compound of formula (I) can be used as a medicament.

First claim

The invention claimed is:

1. A compound of Formula (I):

or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising the compound according to claim 1 , or a pharmaceutically acceptable salt thereof, and a therapeutically inert carrier.

3. A method of treating a cancer selected from thyroid cancer, colorectal cancer, brain cancer, melanoma, and non-small cell lung cancer (NSCLC), the method comprising administering an effective amount of the compound according to claim 1 , or a pharmaceutically acceptable salt thereof, to a patient in need thereof.

4. The method of claim 3 , wherein the cancer is colorectal cancer.

5. The method of claim 3 , wherein the cancer is melanoma.

6. The method of claim 3 , wherein the cancer is non-small cell lung cancer (NSCLC).

7. The compound of claim 1 , wherein the compound is the compound of formula (I):

8. A pharmaceutical composition comprising the compound according to claim 7 , and a therapeutically inert carrier.

9. A method of treating a cancer selected from thyroid cancer, colorectal cancer, brain cancer, melanoma, and non-small cell lung cancer (NSCLC), the method comprising administering an effective amount of the compound according to claim 7 , to a patient in need thereof.

10. The method of claim 9 , wherein the cancer is colorectal cancer.

11. The method of claim 9 , wherein the cancer is melanoma.

12. The method of claim 9 , wherein the cancer is non-small cell lung cancer (NSCLC).

13. The compound of claim 1 , wherein the compound is the pharmaceutically acceptable salt of the compound of formula (I).

14. A pharmaceutical composition comprising the compound according to claim 13 , and a therapeutically inert carrier.

15. A method of treating a cancer selected from thyroid cancer, colorectal cancer, brain cancer, melanoma, and non-small cell lung cancer (NSCLC), the method comprising administering an effective amount of the compound according to claim 13 , to a patient in need thereof.

16. The method of claim 15 , wherein the cancer is colorectal cancer.

17. The method of claim 15 , wherein the cancer is melanoma.

18. The method of claim 15 , wherein the cancer is non-small cell lung cancer (NSCLC).

19. A compound of Formula (Ia):

or a pharmaceutically acceptable salt thereof.

20. A pharmaceutical composition comprising the compound according to claim 19 , or a pharmaceutically acceptable salt thereof, and a therapeutically inert carrier.

21. A method of treating a cancer selected from thyroid cancer, colorectal cancer, brain cancer, melanoma, and non-small cell lung cancer (NSCLC), the method comprising administering an effective amount of the compound according to claim 19 , or a pharmaceutically acceptable salt thereof, to a patient in need thereof.

22. The method of claim 21 , wherein the cancer is colorectal cancer.

23. The method of claim 21 , wherein the cancer is melanoma.

24. The method of claim 21 , wherein the cancer is non-small cell lung cancer (NSCLC).

25. The compound of claim 19 , wherein the compound is the compound of formula (Ia):

26. A pharmaceutical composition comprising the compound according to claim 25 , and a therapeutically inert carrier.

27. A method of treating a cancer selected from thyroid cancer, colorectal cancer, brain cancer, melanoma, and non-small cell lung cancer (NSCLC), the method comprising administering an effective amount of the compound according to claim 25 , to a patient in need thereof.

28. The method of claim 27 , wherein the cancer is colorectal cancer.

29. The method of claim 27 , wherein the cancer is melanoma.

30. The method of claim 27 , wherein the cancer is non-small cell lung cancer (NSCLC).

31. The compound of claim 19 , wherein the compound is the pharmaceutically acceptable salt of the compound of formula (Ia).

32. A pharmaceutical composition comprising the compound according to claim 31 , and a therapeutically inert carrier.

33. A method of treating a cancer selected from thyroid cancer, colorectal cancer, brain cancer, melanoma, and non-small cell lung cancer (NSCLC), the method comprising administering an effective amount of the compound according to claim 31 , to a patient in need thereof.

34. The method of claim 33 , wherein the cancer is colorectal cancer.

35. The method of claim 33 , wherein the cancer is melanoma.

36. The method of claim 33 , wherein the cancer is non-small cell lung cancer (NSCLC).

37. A compound of Formula (Ib):

or a pharmaceutically acceptable salt thereof.

38. A pharmaceutical composition comprising the compound according to claim 37 , or a pharmaceutically acceptable salt thereof, and a therapeutically inert carrier.

39. A method of treating a cancer selected from thyroid cancer, colorectal cancer, brain cancer, melanoma, and non-small cell lung cancer (NSCLC), the method comprising administering an effective amount of the compound according to claim 37 , or a pharmaceutically acceptable salt thereof, to a patient in need thereof.

40. The method of claim 39 , wherein the cancer is colorectal cancer.

41. The method of claim 39 , wherein the cancer is melanoma.

42. The method of claim 39 , wherein the cancer is non-small cell lung cancer (NSCLC).

43. The compound of claim 37 , wherein the compound is the compound of formula (Ib):

44. A pharmaceutical composition comprising the compound according to claim 43 , and a therapeutically inert carrier.

45. A method of treating a cancer selected from thyroid cancer, colorectal cancer, brain cancer, melanoma, and non-small cell lung cancer (NSCLC), the method comprising administering an effective amount of the compound according to claim 43 , to a patient in need thereof.

46. The method of claim 45 , wherein the cancer is colorectal cancer.

47. The method of claim 45 , wherein the cancer is melanoma.

48. The method of claim 45 , wherein the cancer is non-small cell lung cancer (NSCLC).

49. The compound of claim 37 , wherein the compound is the pharmaceutically acceptable salt of the compound of formula (Ib).

50. A pharmaceutical composition comprising the compound according to claim 49 , and a therapeutically inert carrier.

51. A method of treating a cancer selected from thyroid cancer, colorectal cancer, brain cancer, melanoma, and non-small cell lung cancer (NSCLC

Assignees

• Hoffmann La Roche

Inventors

• Dolente Cosimo
• Hewings David Stephen
• Hunziker Daniel
• Krummenacher Daniela
• Pettazzoni Piergiorgio Francesco Tommaso
• Wichmann Juergen

Classifications

• C07D207/48

  Sulfur atoms · CPC title

• A61P35/00 Primary

  Antineoplastic agents · CPC title

• C07D405/12 Primary

  linked by a chain containing hetero atoms as chain links · CPC title

• C07D403/12 Primary

  linked by a chain containing hetero atoms as chain links · CPC title

• A61K31/517

  ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine · CPC title