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1. WO2020191502 - USE OF EMOXYPINE AND DERIVATIVES THEREOF FOR TREATING KIDNEY DISORDERS AND INFLAMMATORY BOWEL DISEASE

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[ EN ]

What is claimed is:

1. Use of Emoxypine or a derivative thereof for the treatment or prophylaxis of renal fibrosis or kidney disease in a subject.

2. The use of claim 1, wherein the Emoxypine derivative has the following

chemical structure:


3. The use of claim 2, wherein each R3 to R5 is independently a hydrogen, an optionally substituted Ci to C4 alkyl, or optionally substituted phenyl.

4. The use of claim 1 or 2, wherein R6 is a hydrogen, an optionally substituted Ci to C4 alkyl, or is -NR^2, wherein

R1 is a hydrogen, a Ci to C4 alkyl, or a phenyl,

R2 is hydroxy(Ci to Ciejalkyl, a (5-hydroxy-trimethylpyridin-2-yloxy)- (C2 to C4)alkyl, a C3 to C7 cycloalkyl, a benzyl, a phenyl, a (Ci to C4 alkyljphenyl, a nitrophenyl, a halophenyl, a benzo[d][l,3]-dioxol-5-yl, or a pyridine-2-yl; or

R1 and R2 are linked to each other to form a 5-membered ring or a 6- membered ring, thereby forming a heterocyclic compound, and are any one selected from pyrrolidine-l-yl, 4-methylpiperazine-l-yl, morpholino, and 1H- pyrrol-l-yl.

5. The use of any one of claims 1-4, wherein the amount of Emoxypine or

derivative thereof is between 120 to 200 mg per kg of the subject.

6. The use of claim 5, wherein the amount of Emoxypine or derivative thereof is between 140 to 180 mg per kg of the subject.

7. The use of claim 6, wherein the amount of Emoxypine or derivative thereof is between 150 to 170 mg per kg of the subject.

8. The use of claim 7, wherein the amount of Emoxypine or derivative thereof between 155 to 165 mg per kg of the subject.

9. The use of claim 8, wherein the amount of Emoxypine or derivative thereof is about 160 mg per kg of the subject.

10. The use of any one of claims 1-9, wherein the kidney disease is chronic

kidney disease.

11. A method for the treatment or prophylaxis of renal fibrosis or kidney

disease in a subject, the method comprising :

administering a therapeutically effective amount of Emoxypine or a derivative thereof to the subject.

12. The method of claim 11, wherein the Emoxypine derivative has the following chemical structure:


13. The method of claim 12, wherein each R3 to R5 is independently a hydrogen, an optionally substituted Ci to C4 alkyl, or optionally substituted phenyl. 14. The method of claim 12 or 13, wherein R6 is a hydrogen, an optionally substituted Ci to C4 alkyl, or is -NR^2, wherein

R1 is a hydrogen, a Ci to C4 alkyl, or a phenyl,

R2 is hydroxy(Ci to Ciejalkyl, a (5-hydroxy-trimethylpyridin-2-yloxy)- (C2 to C4)alkyl, a C3 to C7 cycloalkyl, a benzyl, a phenyl, a (Ci to C4 alkyl)phenyl, a nitrophenyl, a halophenyl, a benzo[d][l,3]-dioxol-5-yl, or a pyridine-2-yl; or

R1 and R2 are linked to each other to form a 5-membered ring or a 6- membered ring, thereby forming a heterocyclic compound, and are any one selected from pyrrolidine-l-yl, 4-methylpiperazine-l-yl, morpholino, and 1H- pyrrol-l-yl.

15. The method of any one of claims 11-14, wherein the amount of Emoxypine or derivative thereof is between 120 to 200 mg per kg of the subject.

16. The method of claim 15, wherein the amount of Emoxypine or derivative thereof is between 140 to 180 mg per kg of the subject.

17. The method of claim 16, wherein the amount of Emoxypine or derivative thereof is between 150 to 170 mg per kg of the subject.

18. The method of claim 17, wherein the amount of Emoxypine or derivative thereof between 155 to 165 mg per kg of the subject.

19. The method of claim 18, wherein the amount of Emoxypine or derivative thereof is about 160 mg per kg of the subject.

20. The method of any one of claims 11-19, wherein the kidney disease is

chronic kidney disease.

21. The method of any one of claims 11-20, in combination with administering a therapeutically effective amount of one or more of cenicriviroc, telmisartan, a cholesterol lowering drug, an antihypertension drug, or erythropoietin.

22. Use of Emoxypine or a derivative thereof for the treatment or prophylaxis of colitis or inflammatory bowel disease (IBD) in a subject.

23. The use of claim 22, wherein the Emoxypine derivative has the following chemical structure:


24. The use of claim 23, wherein each R3 to R5 is independently a hydrogen, an optionally substituted Ci to C4 alkyl, or optionally substituted phenyl.

25. The use of claim 23 or 24, wherein R6 is a hydrogen, an optionally

substituted Ci to C4 alkyl, or is -NR^2, wherein

R1 is a hydrogen, a Ci to C4 alkyl, or a phenyl,

R2 is hydroxy(Ci to Ciejalkyl, a (5-hydroxy-trimethylpyridin-2-yloxy)- (C2 to C4)alkyl, a C3 to C7 cycloalkyl, a benzyl, a phenyl, a (Ci to C4 alkyljphenyl, a nitrophenyl, a halophenyl, a benzo[d][l,3]-dioxol-5-yl, or a pyridine-2-yl; or

R1 and R2 are linked to each other to form a 5-membered ring or a 6- membered ring, thereby forming a heterocyclic compound, and are any one selected from pyrrolidine-l-yl, 4-methylpiperazine-l-yl, morpholino, and 1H- pyrrol-l-yl.

26. The use of any one of claims 22-25, wherein the amount of Emoxypine or derivative thereof is between 0.5 to 50 mg per kg of the subject.

27. The use of claim 26, wherein the amount of Emoxypine or derivative thereof is between 1 to 30 mg per kg of the subject.

28. The use of claim 27, wherein the amount of Emoxypine or derivative thereof is between 5 to 20 mg per kg of the subject.

29. The use of claim 28, wherein the amount of Emoxypine or derivative thereof is between 10 to 15 mg per kg of the subject.

30. The use of claim 29, wherein the amount of Emoxypine or derivative thereof is about 13 mg per kg of the subject.

31. The use of any one of claims 22-30, wherein the inflammatory bowel disease is Crohn's disease.

32. The use of any one of claims 22-30, wherein the inflammatory bowel disease is ulcerative colitis.

33. A method for the treatment or prophylaxis of colitis or inflammatory

bowel disease (IBD) in a subject, the method comprising :

administering a therapeutically effective amount of Emoxypine or a derivative thereof to the subject.

34. The method of claim 33, wherein the Emoxypine derivative has the following chemical structure:


35. The method of claim 34, wherein each R3 to R5 is independently a hydrogen, an optionally substituted Ci to C4 alkyl, or optionally substituted phenyl.

36. The method of claim 34 or 35, wherein R6 is a hydrogen, an optionally

substituted Ci to C4 alkyl, or is -NR^2, wherein

R1 is a hydrogen, a Ci to C4 alkyl, or a phenyl,

R2 is hydroxy(Ci to Ciejalkyl, a (5-hydroxy-trimethylpyridin-2-yloxy)- (C2 to C4)alkyl, a C3 to C7 cycloalkyl, a benzyl, a phenyl, a (Ci to C4 alkyl)phenyl, a nitrophenyl, a halophenyl, a benzo[d][l,3]-dioxol-5-yl, or a pyridine-2-yl; or

R1 and R2 are linked to each other to form a 5-membered ring or a 6- membered ring, thereby forming a heterocyclic compound, and are any one selected from pyrrolidine-l-yl, 4-methylpiperazine-l-yl, morpholino, and 1H- pyrrol-l-yl.

37. The method of any one of claims 33-36, wherein between 0.5 to 50 mg of Emoxypine or derivative thereof per kg of the subject is administered to the subject.

38. The method of claim 37, wherein between 1 to 30 mg of Emoxypine or

derivative thereof per kg of the subject is administered to the subject.

39. The method of claim 38, wherein between 5 to 20 mg of Emoxypine or

derivative thereof per kg of the subject is administered to the subject.

40. The method of claim 39, wherein between 10 to 15 mg of Emoxypine or derivative thereof per kg of the subject is administered to the subject.

41. The method of claim 40, wherein about 13 mg of Emoxypine or derivative thereof per kg of the subject is administered to the subject.

42. The method of any one of claims 33-41, wherein the inflammatory bowel disease is Crohn's disease.

43. The method of any one of claims 33-41, wherein the inflammatory bowel disease is ulcerative colitis.