Deuterium-enriched pirfenidone and method of use thereof
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- PURETECH LYT 100 INC
- Filing Date
- 2026-03-11
- Publication Date
- 2026-06-23
Smart Images
Figure 2026102734000001_ABST
Abstract
Claims
1. A method for treating edema, and a structure for the person who needs it: 【Chemistry 1】 The administration of an effective amount of deuterium-enriched pirfenidone or a pharmaceutically acceptable salt thereof having the following characteristics: wherein, R １ , R ２ , R ３ , R ４ , R ５ , R ６ , R ７ , R ８ , R ９ , R １０ , and R １１ are selected from hydrogen and deuterium, R １ , R ２ , R ３ , R ４ , R ５ , R ６ , R ７ , R ８、 R ９ , R １０ and R １１ At least one of them is deuterium, R ７ , R ８ , R ９ , R １０ , and R １１ If it is deuterium, then R １ , R ２ , R ３ , R ４ , R ５ , and R ６ At least one of them is deuterium, Edema is treated in the aforementioned subjects, by the method described above.
2. The deuterium-enriched pirfenidone has the following structure: 【Chemistry 2】 The method according to claim 1, or having a pharmaceutically acceptable salt thereof.
3. The method according to claim 1 or 2, wherein the edema is lymphedema.
4. The method according to claim 3, wherein the lymphedema is secondary lymphedema.
5. The method according to any of the prior claims, wherein the subject has received treatment for cancer, and the lymphedema is related to the treatment or diagnosis of the cancer.
6. The method according to any one of the prior claims, wherein the subject has breast cancer-related arm lymphedema.
7. The method according to any one of the prior claims, wherein the subject has mild to moderate breast cancer-related lymphedema.
8. The method according to any of the prior claims, wherein the subject is receiving or has received chemotherapy or radiotherapy.
9. The method according to any of the prior claims, wherein at least one of the positions represented as D independently has a deuterium enrichment of about 95% or more.
10. The method according to any of the prior claims, wherein at least one of the positions represented as D independently has a deuterium enrichment of about 98% or more.
11. The method according to any of the prior claims, wherein at least one of the positions represented as D independently has a deuterium enrichment of about 99% or more.
12. The method according to any one of the prior claims, wherein the deuterium-enriched pirfenidone is administered orally at a total daily dose of 250 to 2500 mg.
13. The method according to claim 12, wherein the deuterium-enriched pirfenidone is administered orally in a total daily dose of 500 to 1500 mg.
14. The method according to claim 13, wherein the deuterium-enriched pirfenidone is administered orally at a total daily dose of 750 to 1000 mg.
15. The method according to claim 13, wherein the deuterium-enriched pirfenidone is administered orally twice a day at a total daily dose of 1500 mg.
16. The method according to claim 13, wherein the deuterium-enriched pirfenidone is administered orally twice a day at a total daily dose of 1000 mg.
17. The method according to claim 13, wherein the deuterium-enriched pirfenidone is administered orally twice a day at a total daily dose of 500 mg.
18. The method according to claim 13, wherein the deuterium-enriched pirfenidone is administered orally once daily at a total daily dose of 1500 mg.
19. The method according to claim 13, wherein the deuterium-enriched pirfenidone is administered orally once daily at a total daily dose of 1000 mg.
20. The method according to claim 13, wherein the deuterium-enriched pirfenidone is administered orally once daily at a total daily dose of 750 mg.
21. The method according to claim 13, wherein the deuterium-enriched pirfenidone is administered orally once daily at a total daily dose of 500 mg.
22. The method according to any one of the prior claims, wherein the deuterium-enriched pirfenidone is administered together with food.
23. The method according to any one of the prior claims, wherein the deuterium-enriched pirfenidone is administered without food.
24. The method according to any one of the prior claims, wherein the deuterium-enriched pirfenidone is in tablet form.
25. A method for treating interstitial lung disease (ILD), structured for those who need it: 【Transformation 3】 The administration of an effective amount of deuterium-enriched pirfenidone or a pharmaceutically acceptable salt thereof having the following characteristics: In the formula, R １ , R ２ , R ３ , R ４ , R ５ , R ６ , R ７ , R ８ , R ９ , R １０ , and R １１ It is selected from hydrogen and deuterium, R １ , R ２ , R ３ , R ４ , R ５ , R ６ , R ７ , R ８ , R ９ , R １０ and R １１ At least one of them is deuterium, R ７ , R ８ , R ９ , R １０ , and R １１ If it is deuterium, then R １ , R ２ , R ３ , R ４ , R ５ , and R ６ At least one of them is deuterium, ILD is treated in the aforementioned subjects by the method described above.
26. The deuterium-enriched pirfenidone has the following structure: 【Chemistry 4】 The method according to claim 18, or having a pharmaceutically acceptable salt thereof.
27. The method according to claim 25 or 26, wherein the ILD is idiopathic pulmonary fibrosis (IPF).
28. The method according to any one of claims 25 to 27, wherein at least one of the positions represented as D independently has a deuterium enrichment of about 95% or more.
29. The method according to any one of claims 25 to 28, wherein at least one of the positions represented as D independently has a deuterium enrichment of about 98% or more.
30. The method according to any one of claims 25 to 29, wherein at least one of the positions represented as D independently has about 99% or more deuterium enrichment.
31. The method according to any one of claims 25 to 30, wherein the deuterium-enriched pirfenidone is administered orally at a total daily dose of 250 to 2500 mg.
32. The method according to any one of claims 25 to 30, wherein the deuterium-enriched pirfenidone is administered orally in a total daily dose of 500 to 1500 mg.
33. The method according to any one of claims 25 to 30, wherein the deuterium-enriched pirfenidone is administered orally in a total daily dose of 750 to 1000 mg.
34. The deuterium-enriched pirfenidone is administered orally at a total daily dose of 1500 mg. The method according to any one of claims 25 to 30.
35. The method according to any one of claims 25 to 30, wherein the deuterium-enriched pirfenidone is administered orally at a total daily dose of 1000 mg.
36. The method according to any one of claims 25 to 30, wherein the deuterium-enriched pirfenidone is administered orally at a total daily dose of 500 mg.
37. The method according to any one of claims 25 to 30, wherein the deuterium-enriched pirfenidone is administered orally at a total daily dose of 1500 mg.
38. The method according to any one of claims 25 to 30, wherein the deuterium-enriched pirfenidone is administered orally at a total daily dose of 1000 mg.
39. The method according to any one of claims 25 to 30, wherein the deuterium-enriched pirfenidone is administered orally at a total daily dose of 750 mg.
40. The method according to any one of claims 25 to 30, wherein the deuterium-enriched pirfenidone is administered orally at a total daily dose of 500 mg.
41. The method according to any one of claims 25 to 40, wherein the deuterium-enriched pirfenidone is administered together with food.
42. The method according to any one of claims 25 to 40, wherein the deuterium-enriched pirfenidone is administered without food.
43. The method according to any one of claims 25 to 42, wherein the deuterium-enriched pirfenidone is in tablet form.
44. A method for treating fibrotic disorders or collagen infiltration disorders, provided to subjects requiring it, structure: 【Transformation 5】 The administration of an effective amount of deuterium-enriched pirfenidone, or a pharmaceutically acceptable salt thereof, comprising: In the formula, R １ , R ２ , R ３ , R ４ , R ５ , R ６ , R ７ , R ８ , R ９ , R １０ , and R １１ It is selected from hydrogen and deuterium, R １ 、R ２ 、R ３ 、R ４ 、R ５ 、R ６ 、R ７ 、R ８ 、R ９ 、R １０ and R １１ at least one of which is deuterium, R ７ 、R ８ 、R ９ 、R １０ 、and R １１ are deuterium, if R １ 、R ２ 、R ３ 、R ４ 、R ５ 、and R ６ at least one of which is deuterium, A method for treating the aforementioned fibrotic disorder or collagen infiltration disorder in the subject.
45. The deuterium-enriched pirfenidone has the following structure: 【Transformation 6】 The method according to claim 24, or having a pharmaceutically acceptable salt thereof.
46. The method according to any one of claims 44 to 45, wherein at least one of the positions represented as D independently has a deuterium enrichment of about 95% or more.
47. The method according to claim 46, wherein at least one of the positions represented as D independently has a deuterium enrichment of about 98% or more.
48. The method according to claim 47, wherein at least one of the positions represented as D independently has a deuterium enrichment of about 99% or more.
49. The method according to any one of claims 44 to 48, wherein the deuterium-enriched pirfenidone is administered orally at a total daily dose of 250 to 2500 mg.
50. The method according to any one of claims 44 to 48, wherein the deuterium-enriched pirfenidone is administered orally in a total daily dose of 500 to 1500 mg.
51. The method according to any one of claims 44 to 48, wherein the deuterium-enriched pirfenidone is administered orally in a total daily dose of 750 to 1000 mg.
52. The method according to any one of claims 44 to 48, wherein the deuterium-enriched pirfenidone is administered orally at a total daily dose of 1500 mg.
53. The method according to any one of claims 44 to 48, wherein the deuterium-enriched pirfenidone is administered orally at a total daily dose of 1000 mg.
54. The method according to any one of claims 44 to 48, wherein the deuterium-enriched pirfenidone is administered orally at a total daily dose of 500 mg.
55. The method according to any one of claims 44 to 48, wherein the deuterium-enriched pirfenidone is administered orally at a total daily dose of 1500 mg.
56. The method according to any one of claims 44 to 48, wherein the deuterium-enriched pirfenidone is administered orally at a total daily dose of 1000 mg.
57. The method according to any one of claims 44 to 48, wherein the deuterium-enriched pirfenidone is administered orally at a total daily dose of 750 mg.
58. The method according to any one of claims 44 to 48, wherein the deuterium-enriched pirfenidone is administered orally at a total daily dose of 500 mg.
59. The deuterium-enriched pirfenidone is administered together with food, according to claims 44 to 58. The method described in item 1.
60. The method according to any one of claims 44 to 58, wherein the deuterium-enriched pirfenidone is administered without food.
61. The method according to any one of claims 44 to 60, wherein the deuterium-enriched pirfenidone is in tablet form.