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1. (WO2010027428) PLATINUM ( IV) COMPLEXES FOR USE IN DUAL MODE PHARMACEUTICAL THERAPY
Note: Text based on automatic Optical Character Recognition processes. Please use the PDF version for legal matters

CLAIMS

1. A composition of matter, comprising: a compound having the formula,


wherein:

R1, R2, R3, and R4 can be the same or different and each is a group comprising at least one of ammonia, an amine, an aryl group, a heterocycle including at least one nitrogen, or a leaving group, any being optionally substituted, or, any two or three of R1, R2, R3 and R4 can be joined together to form a bidentate ligand or tridentate ligand, any being optionally substituted; and

R3 and R6 can be the same or different and at least one acts as a therapeutically active compound, or a precursor of a therapeutically active compound, when dissociated from platinum, wherein the therapeutically active compound selectively affects a cellular pathway of a cancer cell and is substantially inactive toward non-cancerous cells.

2. A composition of matter, comprising: a compound having the formula,


wherein:

R1 and R2 can be the same or different and each is a group comprising at least one of ammonia, an amine, an aryl group, or a heterocycle including at least one nitrogen, any being optionally substituted, or, R1 and R2 can be joined together to form a bidentate ligand, any being optionally substituted; and R3, R4, R5, and R6 can be the same or different and at least one acts as a therapeutically active compound, or a precursor of a therapeutically active compound, when dissociated from platinum, wherein the therapeutically active compound selectively affects a cellular pathway of a cancer cell and is substantially inactive toward non-cancerous cells.

3. The composition of claim 1 or 2, wherein the composition, prior to uptake into a cell, is substantially therapeutically inactive.

4. The composition of claim 1 or 2, wherein the at least one of R5 or R6 which acts as a therapeutically active compound, or a precursor of a therapeutically active compound, when dissociated from platinum, has a molecular weight of less than about 800 g/mol.

5. The composition of claim 1 or 2, wherein the at least one of R5 or R6, which acts as a therapeutically active compound, or a precursor of a therapeutically active compound, when dissociated from platinum, has a molecular weight of less than about 600 g/mol.

6. The composition of claim 1 or 2, wherein the at least one of R5 or R6, which acts as a therapeutically active compound, or a precursor of a therapeutically active compound, when dissociated from platinum, has a molecular weight of less than about 400 g/mol.

7. The composition of claim 1 or 2, wherein the at least one of R5 or R6, which acts as a therapeutically active compound, or a precursor of a therapeutically active compound, when dissociated from platinum, has a molecular weight of less than about 300 g/mol.

8. The composition of claim 1 or 2, wherein the at least one of R5 or R6, which acts as a therapeutically active compound, or a precursor of a therapeutically active compound, when dissociated from platinum, has a molecular weight of less than about 200 g/mol.

9. The composition of claim 1 or 2, wherein the at least one of R5 or R6, which acts as a therapeutically active compound, or a precursor of a therapeutically active compound, when dissociated from platinum, has a molecular weight of less than about lOO g/mol.

10. The composition of claim 1 or 2, wherein the at least one of R5 or R6, which acts as a therapeutically active compound, or a precursor of a therapeutically active compound, when dissociated from platinum, is directly associated with platinum center.

1 1. The composition of claim 1 or 2, wherein the at least one of R5 or R6, which acts as a therapeutically active compound, or a precursor of a therapeutically active compound, when dissociated from platinum, is associated with platinum center through a tether.

12. The composition of claim 1 or 2, wherein the at least one of RD or R6 which acts as a therapeutically active compound, or a precursor of a therapeutically active compound, when dissociated from platinum, comprises the group, -OC(O)(CHCl2).

13. The composition of claim 1, wherein each of R5 and R6 comprise the group, -OC(O)(CHCl2).

14. The composition of claim 2, wherein the at least one of R3, R4, R5, or R6 which acts as a therapeutically active compound, or a precursor of a therapeutically active compound, when dissociated from platinum, comprises the group, -OC(O)(CHCl2).

15. The composition of claim 2, wherein each of R3, R4, R5, and R6 comprise the group, -OC(O)(CHCl2).

16. The composition of claim 1, wherein each of R1 and R2 comprise the group, NH3.

17. The composition of claim 2, wherein each of R1 and R2 comprise the group, NH3.

18. The composition of claim 1 or 2, wherein the therapeutically active agent is dissociated from the platinum center upon reduction of the platinum center.

19. The composition of claim 1 or 2, wherein the dissociation of R5 and R6 from the platinum center forms a compound having the formula,


20. The composition of claim 19, wherein the compound is a therapeutically active compound.

21. The composition of claim 19, wherein the compound comprises cisplatin, carboplatin, or oxaliplatin.

22. The composition of claim 19, wherein the compound comprises a precursor to cisplatin.

23. The composition of claim 19, wherein the compound is active towards cancer.

24. The composition of claim 19, wherein the platinum center is reduced from Pt(IV) to Pt(II).

25. The composition of claim 1 or 2, wherein the composition is prepared from a compound having the formula,


26. A kit for the treatment of cancer, comprising: a composition as in claim 1 or 2; and instructions for use of the composition for treatment of cancer.

27. A pharmaceutical composition, comprising: a composition as in claim 1 or 2, or a pharmaceutically acceptable salt, thereof; and one or more pharmaceutically acceptable carriers, additives and/or diluents.

28. The composition of claim 1 or 2, wherein the compound has the formula


wherein:

X is a counterion; and n and m are 1 or n and m are 2.

29. The composition of claim 1 or 2, wherein the composition has the formula:


30. A method of treating a patient in need of a therapeutic protocol, comprising: administering to the patient a composition comprising at least a first component comprising a precursor of a therapeutically active platinum agent and a second component comprising a precursor of a second therapeutically active agent, wherein, upon uptake of the composition into a cell, the first component and the second component dissociate from each other to form a first therapeutically active platinum agent or a second generation precursor to a therapeutically active agent and a second therapeutically active agent or a second generation precursor to a therapeutically active agent, wherein the second therapeutically active agent targets a specific cellular pathway of a cancer cell and is substantially inactive toward non-cancerous cells.

31. The method of claim 30, wherein the composition, prior to uptake into a cell, is substantially therapeutically inactive.

32. The method of claim 30, wherein the second therapeutically active agent or second generation precursor to a therapeutically active agent has a molecular weight of less than about 800 g/mol.

33. The method of claim 30, wherein the second therapeutically active agent or second generation precursor to a therapeutically active agent has a molecular weight of less than about 600 g/mol.

34. The method of claim 30, wherein the second therapeutically active agent or second generation precursor to a therapeutically active agent has a molecular weight of less than about 400 g/mol.

35. The method of claim 30, wherein the second therapeutically active agent or second generation precursor to a therapeutically active agent has a molecular weight of less than about 300 g/mol.

36. The method of claim 30, wherein the second therapeutically active agent or second generation precursor to a therapeutically active agent has a molecular weight of less than about 200 g/mol.

37. The method of claim 30, wherein the second therapeutically active agent or second generation precursor to a therapeutically active agent has a molecular weight of less than about 100 g/mol.

38. The method of claim 30, wherein the precursor of a second therapeutically active agent is directly bound to the platinum comprised in the precursor to the therapeutically active platinum agent.

39. The method of claim 30, wherein the precursor of a second therapeutically active agent is associated with the platinum comprised in the precursor to the therapeutically active platinum agent through a tether.

40. The method of claim 30, wherein the second therapeutically active agent or second generation precursor to a therapeutically active agent comprises dichloroacetic acid.

41. The method of claim 30, wherein the first component and the second component dissociate from each other by reduction of the platinum comprised in the precursor of a therapeutically active platinum agent.

42. The method of claim 41, wherein the platinum is reduced from platinum(IV) to platinum(II).

43. The method of claim 30, wherein the first therapeutically active platinum agent comprises cisplatin, carboplatin, or oxaliplatin.

44. The method of claim 30, wherein the composition has the formula: