Claims
- 1. 8, 10-dideazatetrahydro folic acid compounds having the formula: ##STR17## where R.sub.1 and R.sub.2 are selected from hydrogen and alkyl having from one to about eight carbon atoms; and the carboxylate and acid addition salts thereof.
- 2. 8, 10-dideazatetrahydro folic acid compounds according to claim 1 in which R.sub.1 is hydrogen and R.sub.2 is alkyl.
- 3. 8, 10-dideazatetrahydro folic acid compounds according to claim 2 in which the alkyl is methyl.
- 4. 8, 10-dideazatetrahydro folic acid compounds according to claim 1 in which R.sub.1 and R.sub.2 are each hydrogen.
- 5. 8, 10-dideazatetrahydro folic acid compounds according to claim 1 in which R.sub.1 and R.sub.2 are each alkyl.
- 6. A pharmaceutical composition in dosage unit form for treating leukemia or an ascites tumor comprising an amount per dosage unit within the range from about 0.1 to about 500 mg of an 8, 10-dideazatetrahydro folic acid compound according to claim 1, therapeutically effective to treat leukemia or the ascites tumor, together with a pharmaceutically acceptable nontoxic carrier or diluent therefor.
- 7. A pharmaceutical composition according to claim 6 in which the 8, 10-dideazatetrahydro folic acid is in the form of a pharmaceutically acceptable acid addition salt.
- 8. A pharmaceutical composition according to claim 6 in which the 8, 10-dideazatetrahydro folic acid is in the form of a pharmaceutically acceptable carboxylate.
- 9. A pharmaceutical composition according to claim 6 in tablet form.
- 10. A pharmaceutical composition according to claim 6 in capsule form.
- 11. A pharmaceutical composition according to claim 6 in suppository form.
- 12. A pharmaceutical composition according to claim 6 in cachet form.
- 13. A pharmaceutical composition according to claim 6 in sterile aqueous form.
- 14. A process for treating leukemia and ascites tumors which comprises administering to a warm-blooded animal having an abnormal proportion of leukocytes constituting a leukemic state, a therapeutic and relatively nontoxic dosage unit amount within the range from about 0.1 mg to about 500 mg per day of an 8, 10-dideazatetrahydro folic acid compound according to claim 1, effective to treat leukemia or ascites tumors.
- 15. A process according to claim 14 in which the 8, 10-dideazatetrahydro folic acid compound is administered as a pharmaceutically acceptable acid addition salt thereof.
- 16. A process according to claim 14 in which the 8, 10-dideazatetrahydro folic acid compound is administered as a pharmaceutically acceptable carboxylate.
- 17. A process according to claim 14 in which the 8, 10-dideazatetrahydro folic acid compound is administered in an amount within the range from about 0.1 to about 500 mg per day.
- 18. A process according to claim 14 in which the 8, 10-dideazatetrahydro folic acid compound is administered with an inert diluent or carrier.
- 19. A process according to claim 14 in which the 8, 10-dideazatetrahydro folic acid compound is administered orally.
- 20. A process according to claim 14 in which the 8, 10-dideazatetrahydro folic acid compound is administered parenterally.
Parent Case Info
This application is a continuation-in-part of Ser. No. 245,831, filed Sep. 16, 1988, and now abandoned.
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 (1)
Number |
Name |
Date |
Kind |
4684653 |
Taylor et al. |
Aug 1987 |
|
Non-Patent Literature Citations (1)
Entry |
"Synthesis and Biological Activity of L-5-Deazafolic Acid and L-5-Deazaaminopterin: Synthetic Strategies to 5-Deazapteridine's"; Taylor et al., Journal of Organic Chemistry, pp. 4852-4860, 1983. |
Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
245831 |
Sep 1988 |
|