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Details for Patent: 5,641,763

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Details for Patent: 5,641,763

Title: N-phosphonylmethoxyalkyl derivatives of pyrimdine and purine bases and a therapeutical composition therefrom with antiviral activity
Abstract:This invention relates to new nucleotide analogues and solves the technical problem of their use as biologically active compounds. The subject of this invention are N-(2-phosphonylmethoxyethyl) and N-(3-hydroxy-2-phosphonylmethoxypropyl) derivatives of pyrimidine and purine bases, easily accessible from heterocyclic bases and their N-(2-hydroxyethyl) or N-(2,3-dihydroxypropyl) derivatives. Some of the compounds, according to this invention, exhibit a marked antiviral activity or can be converted into such active compounds by chemical transformations.
Inventor(s): Holy; Antonin (Horni Pocernice, CS), Rosenberg; Ivan (Prague, CS), De Clercq; Erik D. A. (Louvain, BE)
Assignee: Institute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic (CZ) N/A (BE) Rega Stichting v.z.w. (N/A)
Filing Date:Oct 11, 1994
Application Number:08/320,591
Claims:1. N-Phosphonylmethoxyalkyl derivatives of heterocyclic bases of formula I

wherein B is selected from the group consisting of uracil-1-yl, cytosin-1-yl, thymin-1-yl, 5-halogenouracil-1-yl, adenin-3-yl, hypoxanthin-9-yl, 6-amino-2-methylpurin-9-yl, 6-amino-2-methylthiopurin-9-yl, 2,6-diaminopurin-9-yl, 2-aminopurin-9-yl, 6-dimethylaminopurin-9-yl, 6-amino-8-bromopurin-9-yl, 6-amino-8-hydroxypurin-9-yl, 6-hydroxylaminopurin-9-yl, 6-hydrazinopurin-9-yl, 6-thiopurin-9-yl, purin-9-yl, xanthin-9-yl, 8-halogenopurinyl, 6-alkylpurinyl, 7-deaza-8-azaadenin-9-yl, 7-deaza-8-azahypoxanthin-9-yl, and the water soluble salts thereof.

2. The derivative of claim 1 wherein B is 2,6-diaminopurin.

3. The derivative of claim 1 wherein B is 2-aminopurin-9-yl.

4. The derivative of claim 1 wherein B is 6-thiopurin-9-yl.

5. The derivative of claim 1 wherein B is 6-hydroxylaminopurin-9-yl.

6. The derivative of claim 1 wherein B is 6-amino-8-hydroxypurin-9-yl.

7. The derivative of claim 1 wherein B is 6-dimethylaminopurin-9-yl.

8. The derivative of claim 1 wherein B is 2-methyladenin-9-yl.

9. The derivative of claim 1 wherein B is 6-amino-2-methylthiopurin-9-yl.

10. The derivative of claim 1 wherein B is 6-methylpurin-9-yl.

11. The derivative of claim 1 wherein B is 6-amino-8-bromopurin-9-yl.

12. The derivative of claim 1 wherein B is 6-hydrazinopurin-9-yl.

13. The derivative of claim 1 wherein B is xanthin-9-yl.

14. The derivative of claim 1 wherein B is purin-9-yl.

15. The derivative of claim 1 wherein B is 7-deaza-8-azaadenin-9-yl.

16. The derivative of claim 1 wherein B is 7-deaza-8-azahypoxanthin-9-yl.

17. A therapeutic composition comprising a pharmaceutically acceptable carrier and an antivirally effective amount of one or more compounds of formula I

wherein B is selected from the group consisting of uracil-1-yl, cytosin-1-yl, 5-methylcytosin-1-yl, thymin-1-yl, 5-halogenouracil-1-yl, adenin-3-yl, hypoxanthin-9-yl, 6-amino-2-methylpurin-9-yl, 6-amino-2-methylthiopurin-9-yl, 2,6-diaminopurin-9-yl, 2-aminopurin-9-yl, 6-dimethylaminopurin-9-yl, 6-amino-8-bromopurin-9-yl, 8-hydroxypurin-9-yl, 6-hydroxylaminopurin-9-yl, 6-hydrazinopurin-9-yl, 6-thiopurin-9-yl, purin-9-yl, xanthin-9-yl, 8-halogenopurinyl, 6-alkylpurinyl, 7-deaza-8-azadenin-9-yl, 7-deaza-8-azahypoxanthin-9-yl, and the water soluble salts thereof.

18. The composition of claim 17 wherein B is 6-methylpurin-9-yl.

19. The composition of claim 17 wherein B is 6-amino-2-methylpurin-9-yl.

20. The composition of claim 17 wherein B is 6-amino-8-hydroxypurin-9-yl.

21. The composition of claim 17 wherein B is 6-dimethylaminopurin-9-yl.

22. The composition of claim 17 wherein B is 6-hydroxylaminopurin-9-yl.

23. The composition of claim 17 wherein B is 6-thiopurin-9-yl.

24. The composition of claim 17 wherein B is purin-9-yl.

25. The composition of claim 17 wherein B is xanthin-9-yl.

26. The composition of claim 17 wherein B is 6-amino-2-methylthiopurin-9-yl.

27. The composition of claim 17 wherein B is 7-deaza-8-azaadenin-9-yl.

28. The composition of claim 17 wherein B is 7-deaza-8-azahypoxanthin-9-yl.

29. The composition of claim 17 which is suitable for parenteral or oral administration.

30. The composition of claim 17 wherein B is 2,6-diaminopurin-9-yl.

31. The composition of claim 17 wherein B is 6-amino-8-bromopurin-9-yl.

32. The composition of claim 17 wherein B is 2-aminopurin-9-yl.

33. The composition of claim 17 wherein B is 6-hydrazinopurin-9-yl.

34. N-phosphonylmethoxyalkyl derivatives of heterocyclic bases of structure I

wherein B is a monoaza, monodeaza or monoaza-monodeaza analogue of guanine, adenine or hypoxanthine.

35. The derivative of claim 34 wherein B is monoaza adenine.

36. The derivative of claim 34 wherein B is 7-deaza-8-azaadenin-9-yl.

37. A therapeutic composition comprising a pharmaceutically acceptable carrier and an antivirally effective amount of one or more compounds of structure I

wherein B is a monoaza, monodeaza or monoaza-monodeaza analogue of guanine, adenine or hypoxanthine.

38. The composition of claim 37 wherein B is monoaza adenine.

39. The composition of claim 37 wherein B is 7-deaza-8-azaadenin-9-yl.

40. N-phosphonylmethoxyalkyl derivatives of heterocyclic bases of structure I

wherein B is a purin-9-yl base other than adenin-9-yl, guanin-9-yl, guanin-7-yl or 2,6-diaminopurin-9-yl.
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