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Last Updated: May 9, 2024

Claims for Patent: 11,306,106


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Summary for Patent: 11,306,106
Title:Pharmaceutical compositions containing substituted polycyclic pyridone derivatives and prodrug thereof
Abstract: The present invention provides a pharmaceutical composition containing the following compound having antiviral action: ##STR00001## wherein each of the symbols is defined in the specification.
Inventor(s): Kawai; Makoto (Osaka, JP)
Assignee: Shionogi & Co., Ltd. (Osaka, JP)
Application Number:16/937,877
Patent Claims: 1. A method for treating a disease caused by a virus having cap-dependent endonuclease comprising administering to a patient in need thereof a crystal of the compound of the following formula: ##STR00239## wherein the crystal is selected from the group consisting of: (i) crystal Form I having two or more peaks in diffraction angles (2.theta.) selected from 8.6.+-.0.2.degree., 14.1.+-.0.2.degree., 17.4.+-.0.2.degree., 20.0.+-.0.2.degree., 24.0.+-.0.2.degree., 26.3.+-.0.2.degree., 29.6.+-.0.2.degree. and 35.4.+-.0.2.degree. in an X-ray powder diffraction spectrum, (ii) crystal Form II having two or more peaks in diffraction angles (2.theta.) selected from 4.4.+-.0.2.degree., 8.9.+-.0.2.degree., 11.7.+-.0.2.degree., 14.9.+-.0.2.degree., 22.3.+-.0.2.degree., 24.4.+-.0.2.degree., 28.0.+-.0.2.degree. and 31.5.+-.0.2.degree. in an X-ray powder diffraction spectrum, and (iii) crystal Form III having two or more peaks in diffraction angles (2.theta.) selected from 4.4.+-.0.2.degree., 8.7.+-.0.2.degree., 10.6.+-.0.2.degree., 17.3.+-.0.2.degree., 17.5.+-.0.2.degree., 22.0.+-.0.2.degree., 24.0.+-.0.2.degree., 24.1.+-.0.2.degree. and 31.0.+-.0.2.degree. in an X-ray powder diffraction spectrum.

2. The method according to claim 1, wherein the crystal is (i) crystal Form I having peaks in diffraction angles (2.theta.) of 8.6.+-.0.2.degree., 14.1.+-.0.2.degree., 17.4.+-.0.2.degree., 20.0.+-.0.2.degree., 24.0.+-.0.2.degree., 26.3.+-.0.2.degree., 29.6.+-.0.2.degree. and 35.4.+-.0.2.degree. in an X-ray powder diffraction spectrum.

3. The method according to claim 1, wherein the (i) crystal Form I is administered orally in a single dose.

4. The method according to claim 1, wherein 40 mg or 80 mg of the (i) crystal Form I is administered in a single dose.

5. The method according to claim 1, wherein 5 to 40 mg of the (i) crystal Form I is administered in a single dose depending on the body weight of the patient.

6. The method according to claim 1, wherein 40 mg of the (i) crystal Form I is administered in two tablets of 20 mg per tablet.

7. The method according to claim 1, wherein the (i) crystal Form I is administered and the patient is a human 12 years old or older.

8. The method according to claim 1, wherein the crystal is (ii) crystal Form II having peaks in diffraction angles (2.theta.) of 4.4.+-.0.2.degree., 8.9.+-.0.2.degree., 11.7.+-.0.2.degree., 14.9.+-.0.2.degree., 22.3.+-.0.2.degree., 24.4.+-.0.2.degree., 28.0.+-.0.2.degree. and 31.5.+-.0.2.degree. in an X-ray powder diffraction spectrum.

9. The method according to claim 1, wherein the (ii) crystal Form II is administered orally in a single dose.

10. The method according to claim 1, wherein 40 mg or 80 mg of the (ii) crystal Form II is administered in a single dose.

11. The method according to claim 1, wherein 5 to 40 mg of the (ii) crystal Form II is administered in a single dose depending on the body weight of the patient.

12. The method according to claim 1, wherein 40 mg of the (ii) crystal Form II is administered in two tablets of 20 mg per tablet.

13. The method according to claim 1, wherein the (ii) crystal Form II is administered and the patient is a human 12 years old or older.

14. The method according to claim 1, wherein the crystal is (iii) crystal Form III having peaks in diffraction angles (2.theta.) of 4.4.+-.0.2.degree., 8.7.+-.0.2.degree., 10.6.+-.0.2.degree., 17.3.+-.0.2.degree., 17.5.+-.0.2.degree., 22.0.+-.0.2.degree., 24.0.+-.0.2.degree., 24.1.+-.0.2.degree. and 31.0.+-.0.2.degree. in an X-ray powder diffraction spectrum.

15. The method according to claim 1, wherein the (iii) crystal Form III is administered orally in a single dose.

16. The method according to claim 1, wherein 40 mg or 80 mg of the (iii) crystal Form III is administered in a single dose.

17. The method according to claim 1, wherein 5 to 40 mg of the (iii) crystal Form III is administered in a single dose depending on the body weight of the patient.

18. The method according to claim 1, wherein 40 mg of the (iii) crystal Form III is administered in two tablets of 20 mg per tablet.

19. The method according to claim 1, wherein the (iii) crystal Form III is administered and the patient is a human 12 years old or older.

20. A method for treating influenza comprising administering to a patient in need thereof a crystal of the compound of the following formula: ##STR00240## wherein the crystal is selected from the group consisting of: (i) crystal Form I having two or more peaks in diffraction angles (2.theta.) selected from 8.6.+-.0.2.degree., 14.1.+-.0.2.degree., 17.4.+-.0.2.degree., 20.0.+-.0.2.degree., 24.0.+-.0.2.degree., 26.3.+-.0.2.degree., 29.6.+-.0.2.degree. and 35.4.+-.0.2.degree. in an X-ray powder diffraction spectrum, (ii) crystal Form II having two or more peaks in diffraction angles (2.theta.) selected from 4.4.+-.0.2.degree., 8.9.+-.0.2.degree., 11.7.+-.0.2.degree., 14.9.+-.0.2.degree., 22.3.+-.0.2.degree., 24.4.+-.0.2.degree., 28.0.+-.0.2.degree. and 31.5.+-.0.2.degree. in an X-ray powder diffraction spectrum, and (iii) crystal Form III having two or more peaks in diffraction angles (2.theta.) selected from 4.4.+-.0.2.degree., 8.7.+-.0.2.degree., 10.6.+-.0.2.degree., 17.3.+-.0.2.degree., 17.5.+-.0.2.degree., 22.0.+-.0.2.degree., 24.0.+-.0.2.degree., 24.1.+-.0.2.degree. and 31.0.+-.0.2.degree. in an X-ray powder diffraction spectrum.

21. The method according to claim 20, wherein the crystal is (i) crystal Form I having peaks in diffraction angles (2.theta.) of 8.6.+-.0.2.degree., 14.1.+-.0.2.degree., 17.4.+-.0.2.degree., 20.0.+-.0.2.degree., 24.0.+-.0.2.degree., 26.3.+-.0.2.degree., 29.6.+-.0.2.degree. and 35.4.+-.0.2.degree. in an X-ray powder diffraction spectrum.

22. The method according to claim 20, wherein the (i) crystal Form I is administered orally in a single dose.

23. The method according to claim 20, wherein 40 mg or 80 mg of the (i) crystal Form I is administered in a single dose.

24. The method according to claim 20, wherein 5 to 40 mg of the (i) crystal Form I is administered in a single dose depending on the body weight of the patient.

25. The method according to claim 20, wherein 40 mg of the (i) crystal Form I is administered in two tablets of 20 mg per tablet.

26. The method according to claim 20, wherein the (i) crystal Form I is administered and the patient is a human 12 years old or older.

27. The method according to claim 20, wherein the crystal is (ii) crystal Form II having peaks in diffraction angles (2.theta.) of 4.4.+-.0.2.degree., 8.9.+-.0.2.degree., 11.7.+-.0.2.degree., 14.9.+-.0.2.degree., 22.3.+-.0.2.degree., 24.4.+-.0.2.degree., 28.0.+-.0.2.degree. and 31.5.+-.0.2.degree. in an X-ray powder diffraction spectrum.

28. The method according to claim 20, wherein the (ii) crystal Form II is administered orally in a single dose.

29. The method according to claim 20, wherein 40 mg or 80 mg of the (ii) crystal Form II is administered in a single dose.

30. The method according to claim 20, wherein 5 to 40 mg of the (ii) crystal Form II is administered in a single dose depending on the body weight of the patient.

31. The method according to claim 20, wherein 40 mg of the (ii) crystal Form II is administered in two tablets of 20 mg per tablet.

32. The method according to claim 20, wherein the (ii) crystal Form II is administered and the patient is a human 12 years old or older.

33. The method according to claim 20, wherein the crystal is (iii) crystal Form III having peaks in diffraction angles (2.theta.) of 4.4.+-.0.2.degree., 8.7.+-.0.2.degree., 10.6.+-.0.2.degree., 17.3.+-.0.2.degree., 17.5.+-.0.2.degree., 22.0.+-.0.2.degree., 24.0.+-.0.2.degree., 24.1.+-.0.2.degree. and 31.0.+-.0.2.degree. in an X-ray powder diffraction spectrum.

34. The method according to claim 20, wherein the (iii) crystal Form III is administered orally in a single dose.

35. The method according to claim 20, wherein 40 mg or 80 mg of the (iii) crystal Form III is administered in a single dose.

36. The method according to claim 20, wherein 5 to 40 mg of the (iii) crystal Form III is administered in a single dose depending on the body weight of the patient.

37. The method according to claim 20, wherein 40 mg of the (iii) crystal Form III is administered in two tablets of 20 mg per tablet.

38. The method according to claim 20, wherein the (iii) crystal Form III is administered and the patient is a human 12 years old or older.

39. A method for preventing influenza comprising administering to a patient in need thereof a crystal of the compound of the following formula: ##STR00241## wherein the crystal is selected from the group consisting of: (i) crystal Form I having two or more peaks in diffraction angles (2.theta.) selected from 8.6.+-.0.2.degree., 14.1.+-.0.2.degree., 17.4.+-.0.2.degree., 20.0.+-.0.2.degree., 24.0.+-.0.2.degree., 26.3.+-.0.2.degree., 29.6.+-.0.2.degree. and 35.4.+-.0.2.degree. in an X-ray powder diffraction spectrum, (ii) crystal Form II having two or more peaks in diffraction angles (2.theta.) selected from 4.4.+-.0.2.degree., 8.9.+-.0.2.degree., 11.7.+-.0.2.degree., 14.9.+-.0.2.degree., 22.3.+-.0.2.degree., 24.4.+-.0.2.degree., 28.0.+-.0.2.degree. and 31.5.+-.0.2.degree. in an X-ray powder diffraction spectrum, and (iii) crystal Form III having two or more peaks in diffraction angles (2.theta.) selected from 4.4.+-.0.2.degree., 8.7.+-.0.2.degree., 10.6.+-.0.2.degree., 17.3.+-.0.2.degree., 17.5.+-.0.2.degree., 22.0.+-.0.2.degree., 24.0.+-.0.2.degree., 24.1.+-.0.2.degree. and 31.0.+-.0.2.degree. in an X-ray powder diffraction spectrum.

40. The method according to claim 39, wherein the crystal is (i) crystal Form I having peaks in diffraction angles (2.theta.) of 8.6.+-.0.2.degree., 14.1.+-.0.2.degree., 17.4.+-.0.2.degree., 20.0.+-.0.2.degree., 24.0.+-.0.2.degree., 26.3.+-.0.2.degree., 29.6.+-.0.2.degree. and 35.4.+-.0.2.degree. in an X-ray powder diffraction spectrum.

41. The method according to claim 39, wherein the (i) crystal Form I is administered orally in a single dose.

42. The method according to claim 39, wherein 40 mg or 80 mg of the (i) crystal Form I is administered in a single dose.

43. The method according to claim 39, wherein 5 to 40 mg of the (i) crystal Form I is administered in a single dose depending on the body weight of the patient.

44. The method according to claim 39, wherein 40 mg of the (i) crystal Form I is administered in two tablets of 20 mg per tablet.

45. The method according to claim 39, wherein the (i) crystal Form I is administered and the patient is a human 12 years old or older.

46. The method according to claim 39, wherein the crystal is (ii) crystal Form II having peaks in diffraction angles (2.theta.) of 4.4.+-.0.2.degree., 8.9.+-.0.2.degree., 11.7.+-.0.2.degree., 14.9.+-.0.2.degree., 22.3.+-.0.2.degree., 24.4.+-.0.2.degree., 28.0.+-.0.2.degree. and 31.5.+-.0.2.degree. in an X-ray powder diffraction spectrum.

47. The method according to claim 39, wherein the (ii) crystal Form II is administered orally in a single dose.

48. The method according to claim 39, wherein 40 mg or 80 mg of the (ii) crystal Form II is administered in a single dose.

49. The method according to claim 39, wherein 5 to 40 mg of the (ii) crystal Form II is administered in a single dose depending on the body weight of the patient.

50. The method according to claim 39, wherein 40 mg of the (ii) crystal Form II is administered in two tablets of 20 mg per tablet.

51. The method according to claim 39, wherein the (ii) crystal Form II is administered and the patient is a human 12 years old or older.

52. The method according to claim 39, wherein the crystal is (iii) crystal Form III having peaks in diffraction angles (2.theta.) of 4.4.+-.0.2.degree., 8.7.+-.0.2.degree., 10.6.+-.0.2.degree., 17.3.+-.0.2.degree., 17.5.+-.0.2.degree., 22.0.+-.0.2.degree., 24.0.+-.0.2.degree., 24.1.+-.0.2.degree. and 31.0.+-.0.2.degree. in an X-ray powder diffraction spectrum.

53. The method according to claim 39, wherein the (iii) crystal Form III is administered orally in a single dose.

54. The method according to claim 39, wherein 40 mg or 80 mg of the (iii) crystal Form III is administered in a single dose.

55. The method according to claim 39, wherein 5 to 40 mg of the (iii) crystal Form III is administered in a single dose depending on the body weight of the patient.

56. The method according to claim 39, wherein 40 mg of the (iii) crystal Form III is administered in two tablets of 20 mg per tablet.

57. The method according to claim 39, wherein the (iii) crystal Form III is administered and the patient is a human 12 years old or older.

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