Claims
- 1. A compound of the formula
- 2. A compound of the formula
- 3. A compound of the formula
- 4. A compound of claim 1 wherein X1 is fluoro and X2 is hydrogen.
- 5. A compound of claim 1 wherein X1 is hydrogen and X2 is fluoro.
- 6. A compound of claim 2 or 3 wherein R is hydrogen.
- 7. A compound of claim 1, 2 or 3 wherein V is oxy.
- 8. A compound of claim 1, 2 or 3 wherein Z is hydrogen.
- 9. A compound of claim 1, 2 or 3 wherein Y1 is a CH group.
- 10. A compound of claim 1, 2 or 3 wherein Y2 is nitrogen.
- 11. A compound of claim 1, 2 or 3 wherein Y3 is nitrogen.
- 12. A compound of claim 1, 2 or 3 wherein Z is hydrogen.
- 13. A compound of claim 1, 2 or 3 wherein Y2 is a CH group.
- 14. A method of treating a patient afflicted with a neoplastic disease state comprising the administration thereto of a therapeutically effective antineoplastic amount of a compound of claim 1, 2 or 3.
- 15. A method of treating a patient afflicted with a viral infection comprising the administration thereto of a therapeutically effective antiviral amount of a compound of claim 1, 2 or 3.
- 16. A method of controlling the growth of a neoplasm in a patient afflicted with a neoplastic disease state comprising administration thereto of a therapeutically effective antineoplastic amount of a compound of claim 1, 2 or 3.
- 17. A method of controlling a viral infection in a patient afflicted therewith comprising administration thereto of a therapeutically effective antiviral amount of a compound of claim 1, 2 or 3.
- 18. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 1, 2 or 3 in admixture or otherwise in association with one or more pharmaceutically acceptable carriers or excipients.
- 19. A compound of claim 1 wherein the compound is 2′-deoxy-2′-difluoromethylidene-cytidine.
- 20. The compound of claim 1 wherein the compound is 2′-deoxy-2′-difluoromethylidene-uridine.
- 21. The compound of claim 1 wherein the compound is 2′-deoxy-2′-difluoromethylidene-guanosine.
- 22. A compound of claim 1 wherein the compound is (E)-2′-deoxy-2′-fluoromethylidene-cytidine.
- 23. A compound of claim 1 wherein the compound is (Z)-2′-deoxy-2′-fluoromethylidene-cytidine.
- 24. A compound of claim 1 wherein the compound is (Z) or (E)-2′-deoxy-2′-fluoromethylidene-uridine.
- 25. A compound of claim 1 wherein the compound is (z) or (E) 2′-deoxy-2′-fluoromethylidene-guanosine.
- 26. The compound of claim 2 wherein the compound is 2′-deoxy-2′-ethenylidene-cytidine.
- 27. The compound of claim 2 wherein the compound is 2′-deoxy-2′-ethenylidene-uridine.
- 28. A compound of claim 2 wherein the compound is 2′-deoxy-2′-ethenylidene-guanosine.
- 29. A compound of claim 3 wherein the compound is 2′-deoxy-2′ (R or S)-ethynyl-cytidine.
- 30. A compound of claim 3 wherein the compound is 2′-deoxy-2′ (R or S)-ethynyl-uridine.
- 31. A compound of claim 3 wherein the compound is 2′-deoxy-2′ (R or S)-ethynyl-guanosine.
- 32. A compound of the formula
- 33. A compound of claim 32 wherein Ar is phenyl.
- 34. A compound of claim 33 wherein XHAL is fluorine.
- 35. A composition comprising a compound of claim 1, 2, 3, or 32 in admixture or otherwise in association with an inert carrier.
Parent Case Info
[0001] This is a continuation-in-part of application Ser. No. 271,479, filed Nov. 15, 1988. The present invention relates to novel 2′-halomethylidene, 2′-ethenylidene and 2′-ethynyl cytidine, uridine and guanosine derivatives which are useful as anti-viral and anti-neoplastic agents.
Divisions (1)
|
Number |
Date |
Country |
Parent |
08113505 |
Aug 1993 |
US |
Child |
08304744 |
Sep 1994 |
US |
Continuations (4)
|
Number |
Date |
Country |
Parent |
08869511 |
Jun 1997 |
US |
Child |
10164848 |
Jun 2002 |
US |
Parent |
08565237 |
Nov 1995 |
US |
Child |
08869511 |
Jun 1997 |
US |
Parent |
08304744 |
Sep 1994 |
US |
Child |
08565237 |
Nov 1995 |
US |
Parent |
07563470 |
Aug 1990 |
US |
Child |
08113505 |
Aug 1993 |
US |
Continuation in Parts (1)
|
Number |
Date |
Country |
Parent |
07271479 |
Nov 1988 |
US |
Child |
07563470 |
Aug 1990 |
US |