Claims
- 1. A method for treating a patient with leukemia comprising;administering to said patient having chronic myelogenous leukemia or acute myelogenous leukemia, a therapeutically effective amount of a compound having the formula I: wherein B is cytosine or 5-fluorocytosine and R is selected from H, monophosphate, diphosphate, triphosphate, carbonyl substituted with a C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-10 aryl, and wherein each Rc is independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl and hydroxy protecting groups; wherein said compound is substantially in the form of the (−) enantiomer; wherein the step of administering comprises administering to a patient that has been previously treated with Ara-C; and wherein said compound of formula I is at least 95% free of the (+) form.
- 2. The method according to claim 1, wherein R is H.
- 3. The method according to claim 1, wherein B is cytosine.
- 4. The method according to claim 3, wherein said compound of formula I is at least 97% free of the (+) form.
- 5. The method according to claim 3, wherein said compound of formula I is at least 99% free of the (+) form.
- 6. The method according to claim 1, wherein R is H and B is cytosine.
- 7. The method according to claim 6, wherein said compound of formula I is at least 97% free of the (+) form.
- 8. The method according to claim 6, wherein said compound of formula I is at least 99% free of the (+) form.
- 9. The method of claim 1, wherein the leukemia is a chronic myelogenous leukemia.
- 10. The method of claim 1, wherein the leukemia is an acute myelogenous leukemia.
- 11. The method according to claim 1, wherein said compound of formula I is at least 97% free of the (+) form.
- 12. The method according to claim 1, wherein said compound of formula I is at least 99% free of the (+) form.
- 13. A method according to claim 1, wherein said hydroxy protecting groups are acetyl-2-thioethyl ester, pivaloyloxymethyl ester, and isopropyloxycarbonyloxymethyl ester.
- 14. A method according to claim 1, wherein said compound is administered in an amount of 0.1-750 mg/kg of bodyweight per day.
- 15. A method according to claim 1, wherein said compound is administered in an amount of 0.5-60 mg/kg of bodyweight per day.
- 16. A method according to claim 1, wherein said compound is administered in an amount of 1-20 mg/kg of bodyweight per day.
- 17. A method according to claim 1, wherein said compound is administered in a daily amount of 1.08 mg/m2-1.62 mg/m2.
- 18. A method according to claim 1, wherein said compound is administered in a unit dosage form containing 10-1500 mg of said compound.
- 19. A method according to claim 1, wherein said compound is administered in a unit dosage form containing 20-1000 mg of said compound.
- 20. A method according to claim 1, wherein said compound is administered in a unit dosage form containing 50-700 mg of said compound.
- 21. A method for treating a patient with leukemia comprising:administering to said patient having chronic myelogenous leukemia or acute myelogenous leukemia, a therapeutically effective amount of a compound having the formula I: wherein B is cytosine or 5-fluorocytosine and R is selected from H, monophosphate, diphosphate, triphosphate, carbonyl substituted with a C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-10 aryl, and wherein each Rc is independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl and hydroxy protecting groups; wherein said compound is substantially in the form of the (−) enantiomer; wherein said patient is suffering from a leukemia which is non-responsive to treatment with other chemotherapeutic agents; and wherein said compound of formula I is at least 95% free of the (+) form.
- 22. The method according to claim 21, wherein R is H.
- 23. The method according to claim 21, wherein B is cytosine.
- 24. The method according to claim 21, wherein R is H and B is cytosine.
- 25. The method according to claim 24, wherein said compound of formula I is at least 97% free of the (+) form.
- 26. The method according to claim 24, wherein said compound of formula I is at least 99% free of the (+) form.
- 27. The method according to claim 21, wherein said compound of formula I is at least 97% free of the (+) form.
- 28. The method according to claim 21, wherein said compound of formula I is at least 99% free of the (+) form.
- 29. A method according to claim 21, wherein said hydroxy protecting groups are acetyl-2-thioethyl ester, pivaloyloxymethyl ester, and isopropyloxycarbonyloxymethyl ester.
- 30. A method according to claim 21, wherein said compound is administered in an amount of 0.1-750 mg/kg of bodyweight per day.
- 31. A method according to claim 21, wherein said compound is administered in an amount of 0.5-60 mg/kg of bodyweight per day.
- 32. A method according to claim 21, wherein said compound is administered in an amount of 1-20 mg/kg of bodyweight per day.
- 33. A method according to claim 21, wherein said compound is administered in a daily amount of 1.08 mg/m2-1.62 mg/m2.
- 34. A method according to claim 21, wherein said compound is administered in a unit dosage form containing 10-1500 mg of said compound.
- 35. A method according to claim 21, wherein said compound is administered in a unit dosage form containing 20-1000 mg of said compound.
- 36. A method according to claim 21, wherein said compound is administered in a unit dosage form containing 50-700 mg of said compound.
Parent Case Info
This application claims the benefit of U.S. Provisional Application No. 60/126,734, filed Mar. 29, 2000, and U.S. Provisional Application No. 60/126,813, filed Mar. 30, 2000, both of which are hereby incorporated by reference in their entirety.
US Referenced Citations (3)
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Date |
Kind |
5041449 |
Belleau et al. |
Aug 1991 |
A |
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Belleau et al. |
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Provisional Applications (2)
|
Number |
Date |
Country |
|
60/126734 |
Mar 2000 |
US |
|
60/126813 |
Mar 2000 |
US |