Claims
- 1. The resolved d,L and l,L-diastereomers of 10-alkyl-10-deazaminopterin compounds having the formula: ##STR6## wherein: R.sub.1 and R.sub.2 are both selected from the group consisting of hydrogen and alkyl having from one to about eight carbon atoms, R.sub.1 is different from R.sub.2, and at least one of R.sub.1 and R.sub.2 is alkyl.
- 2. The resolved d,L and l,L-diastereomers of 10-alkyl-10-deazaminopterin compounds according to claim 1 in which one of R.sub.1 and R.sub.2 is alkyl and the other is hydrogen.
- 3. The resolved d,L and l,L-diastereomers of 10-alkyl-10-deazaminopterin compounds according to claim 2 in which the alkyl is ethyl.
- 4. The resolved d,L and l,L-diastereomers of 10-alkyl-10-deazaminopterin compounds according to claim 2 in which the alkyl is methyl.
- 5. 10-Deazaminopterin compounds according to claim 1 in which both of R.sub.1 and R.sub.2 are different alkyl.
- 6. d,L-10-ethyl-10-deazaminopterin.
- 7. l,L-10-ethyl-10-deazaminopterin.
- 8. A pharmaceutical composition in dosage unit form for treating leukemia or an ascites tumor comprising an amount within the range from about 0.1 to about 500 mg of d,L-10-ethyl-10-deazaminopterin per dosage unit therapeutically effective to ameliorate leukemia or the ascites tumor, together with a pharmaceutically acceptable nontoxic carrier or diluent therefor.
- 9. A pharmaceutical composition according to claim 8 in which the d,L-10-ethyl-10-deazaminopterin is in the form of a pharmaceutically acceptable acid addition salt.
- 10. A pharmaceutical composition in tablet form for treating leukemia or an ascites tumor comprising an amount within the range from about 0.1 to about 500 mg of d,L-10-ethyl-10-deazaminopterin per tablet therapeutically effective to ameliorate leukemia or the ascites tumor, together with a pharmaceutically acceptable nontoxic carrier or diluent therefor.
- 11. A pharmaceutical composition according to claim 10 in which the d,L-10-ethyl-10-deazaminopterin is in the form of a pharmaceutically acceptable acid addition salt.
- 12. A pharmaceutical composition in capsule form for treating leukemia or an ascites tumor comprising an amount within the range from 0.1 to about 500 mg of d,L-10-ethyl-10-deazaminopterin per capsule therapeutically effective to ameliorate leukemia or the ascites tumor, together with a pharmaceutically acceptable nontoxic inert carrier or diluent therefor.
- 13. A pharmaceutical composition according to claim 12 in which the d,L-10-ethyl-10-deazaminopterin is in the form of a pharmaceutically acceptable acid addition salt.
- 14. A pharmaceutical composition in suppository form for treating leukemia or an ascites tumor comprising an amount within the range from about 0.1 to about 500 mg of d,L-10-ethyl-10-deazaminopterin per suppository therapeutically effective to ameliorate leukemia or the ascites tumor, together with a pharmaceutically acceptable nontoxic inert carrier or diluent therefor.
- 15. A pharmaceutical composition according to claim 14 in which the d,L-10-ethyl-10-deazaminopterin is in the form of a pharmaceutically acceptable acid addition salt.
- 16. A pharmaceutical composition in cachet form for treating leukemia or an ascites tumor comprising an amount within the range from about 0.1 to about 500 mg of d,L-10-ethyl-10-deazaminopterin per cachet therapeutically effective to ameliorate leukemia or the ascites tumor, together with a pharmaceutically acceptable nontoxic inert carrier or diluent therefor.
- 17. A pharmaceutical composition according to claim 16 in which the d,L-10-ethyl-10-deazaminopterin is in the form of a pharmaceutically acceptable acid addition salt.
- 18. A pharmaceutical composition in sterile aqueous form for treating leukemia or an ascites tumor comprising an amount within the range from about 0.1 to about 500 mg of d,L-10-ethyl-10-deazaminopterin therapeutically effective to ameliorate leukemia or the ascites tumor, together with a pharmaceutically acceptable nontoxic sterile inert aqueous carrier or diluent therefor.
- 19. A pharmaceutical composition according to claim 18 in which the d,L-10-ethyl-10-deazaminopterin is in the form of a pharmaceutically acceptable acid addition salt.
- 20. A pharmaceutical composition according to claim 18 in aqueous solution form.
- 21. A pharmaceutical composition according to claim 18 in aqueous dispersion form.
- 22. A pharmaceutical composition in dosage unit form for treating leukemia or an ascites tumor comprising an amount within the range from about 0.1 to about 500 mg of l,L-10-ethyl-10-deazaminopterin per dosage unit therapeutically effective to ameliorate leukemia or the ascites tumor, together with a pharmaceutically acceptable nontoxic carrier or diluent therefor.
- 23. A pharmaceutical composition according to claim 22 in which the l,L-10-ethyl-10-deazaminopterin is in the form of a pharmaceutically acceptable acid addition salt.
- 24. A pharmaceutical composition in tablet form for treating leukemia or an ascites tumor comprising an amount within the range from about 0.1 to about 500 mg of l,L-10-ethyl-10-deazaminopterin per tablet therapeutically effective to ameliorate leukemia or the ascites tumor, together with a pharmaceutically acceptable nontoxic carrier or diluent therefor.
- 25. A pharmaceutical composition according to claim 24 in which the l,L-10-ethyl-10-deazaminopterin is in the form of a pharmaceutically acceptable acid addition salt.
- 26. A pharmaceutical composition in capsule form for treating leukemia or an ascites tumor comprising an amount within the range from 0.1 to about 500 mg of l,L-10-ethyl-10-deazaminopterin per capsule therapeutically effective to ameliorate leukemia or the ascites, together with a pharmaceutically acceptable nontoxic inert carrier or diluent therefor.
- 27. A pharmaceutical composition according to claim 26 in which the l,L-10-ethyl-10-deazaminopterin is in the form of a pharmaceutically acceptable acid addition salt.
- 28. A pharmaceutical composition in suppository form for treating leukemia or an ascites tumor comprising an amount within the range from about 0.1 to about 500 mg of l,L-10-ethyl-10-deazaminopterin per suppository therapeutically effective to ameliorate leukemia or the ascites tumor, together with a pharmaceutically acceptable nontoxic inert carrier or diluent therefor.
- 29. A pharmaceutical composition according to claim 28 in which the l,L-10-ethyl-10-deazaminopterin is in the form of a pharmaceutically acceptable acid addition salt.
- 30. A pharmaceutical composition in cachet form for treating leukemia or an ascites tumor comprising an amount within the range from about 0.1 to about 500 mg of l,L-10-ethyl-10-deazaminopterin per cachet therapeutically effective to ameliorate leukemia or the ascites tumor, together with a pharmaceutically acceptable nontoxic inert carrier or diluent therefor.
- 31. A pharmaceutical composition according to claim 30 in which the l,L-10-ethyl-10-deazaminopterin is in the form of a pharmaceutically acceptable acid addition salt.
- 32. A pharmaceutical composition in sterile aqueous form for treating leukemia or an ascites tumor comprising an amount within the range from about 0.1 to about 500 mg of l,L-10-ethyl-10-deazaminopterin therapeutically effective to ameliorate leukemia or the ascites tumor, together with a pharmaceutically acceptable nontoxic sterile inert aqueous carrier or diluent therefor.
- 33. A pharmaceutical composition according to claim 32 in which the l,L-10-ethyl-10-deazaminopterin is in the form of a pharmaceutically acceptable acid addition salt.
- 34. A pharmaceutical composition according to claim 32 in aqueous solution form.
- 35. A pharmaceutical composition according to claim 32 in aqueous dispersion form.
- 36. A process for treating leukemia and ascites tumors which comprises administering to a warm-blooded animal having an abnormal proportion of leukocytes or other evidence of the malignancy, a therapeutic and relatively nontoxic amount of d,L-10-ethyl-10-deazaminopterin, to ameliorate leukemia or ascites tumors.
- 37. A process according to claim 36 in which the d,L-10-ethyl-10-deazaminopterin is administered as a pharmaceutically acceptable salt thereof.
- 38. A process according to claim 36 in which the d,L-10-ethyl-10-deazaminopterin is administered in an amount within the range from about 0.1 to about 500 mg per day.
- 39. A process according to claim 36 in which the d,L-10-ethyl-10-deazaminopterin is administered with an inert diluent or carrier.
- 40. A process according to claim 36 in which the d,L-10-ethyl-10-deazaminopterin is administered orally.
- 41. A process according to claim 36 in which the d,L-10-ethyl-10-deazaminopterin is administered parenterally.
- 42. A process for treating leukemia and ascites tumors which comprises administering to a warm-blooded animal having an abnormal proportion of leukocytes or other evidence of the malignancy, a therapeutic and relatively nontoxic amount of l,L-10-ethyl-10-deazaminopterin, to ameliorate leukemia or ascites tumors.
- 43. A process according to claim 42 in which the l,L-10-ethyl-10-deazaminopterin is administered as a pharmaceutically acceptable salt thereof.
- 44. A process according to claim 42 in which the l,L-10-ethyl-10-deazaminopterin is administered in an amount within the range from about 0.1 to about 500 mg per day.
- 45. A process according to claim 42 in which the l,L-10-ethyl-10-deazaminopterin is administered with an inert diluent or carrier.
- 46. A process according to claim 42 in which the l,L-10-ethyl-10-deazaminopterin is administered orally.
- 47. A process according to claim 42 in which the l,L-10-ethyl-10-deazaminopterin is administered parenterally.
ORIGIN OF INVENTION
The invention described herein was in part made in the course of work under a grant or award from the National Institute of Health, Department of Health, Education and Welfare.
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
4369319 |
DeGraw, Jr. et al. |
Jan 1983 |
|
4393064 |
DeGraw, Jr. et al. |
Jul 1983 |
|