Claims
- 1. A compound of formula:
- 2. The compound of claim 1 wherein R1 is —COR4.
- 3. The compound of claim 2 wherein R2 is H.
- 4. The compound of claim 3 wherein R3 is H.
- 5. The compound of claim 4 which is selected from the group:
N-[3-(4-Methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]-N-phenylacetamide (Ex. 2); N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]-N-phenylpropanamide (Ex. 3); 2-Amino-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]-N-phenylacetamide acetic acid salt (Ex. 6b); 2-Amino-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]-N-phenylacetamide hydrochloric acid salt (Ex. 6c); (2S)-2-Amino-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]-4-phenyl-N-phenylbutanamide (Ex. 7b); (2S)-2-amino-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]-4-methylthio-N-phenylbutanamide acetic acid salt (Ex. 7c); (2S)-2-Amino-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]-4-methylthio-N-phenylbutanamide hydrochloric acid salt (Ex. 7d); (2S)-2-Amino-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimid[4,5-d]pyrimidin-7-yl)]-3-phenyl-N-phenylpropanamide (Ex. 8b); (2S)-2-Amino-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]-3-methylthio-N-phenylpropanamide hydrochloric acid salt (Ex. 8c); (2S)-2-Amino-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimid[4,5-d]pyrimidin-7-yl)]-4-methyl-N-phenylpentanamide acetic acid salt (Ex. 9b); (2S)-2-Amino-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]-4-methylthio-N-phenylpentanamide hydrochloric acid salt (Ex. 9c); (2S)-2-Amino-3-(4-hydroxyphenyl)-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]-N-phenylpropanamide hydrochloric acid salt (Ex. 10b); (2S)-2,6-Diamino-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]-N-phenylhexanamide di-hydrochloric acid salt (Ex. 11b); (2S)-2-Amino-3-indol-3-yl-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]-N-phenylpropanamide hydrochloric acid salt (Ex. 12b); (2S)-2-Amino-3-hydroxy-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]-N-phenylpropa (Ex. 13b); (2R)-2-Amino-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]-4-methylthio-N-phenylbutanamide hydrochloric acid saltn (Ex. 14b); N-[3-(4-Methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]-N-phenylpentanamide (Ex. 16); and N-[3-(4-Methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]-N-phenylbutanamide (Ex. 17).
- 6. The compound of claim 2 which is selected from the group:
N-(4-Hydroxyphenyl)-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]acetamide (Ex. 19e); and N-(4-methoxyphenyl)-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]acetamide (Ex. 21).
- 7. The compound of claim 1 wherein R1 is —COOCHR5OCOR4.
- 8. The compound of claim 7 wherein R2 is H.
- 9. The compound of claim 8 wherein R3 is H.
- 10. The compound of claim 9 which is selected from the group:
{N-[3-(4-Methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]-N-phenylcarbamoyloxy}methyl acetate (Ex. 4b); {N-[3-(4-Methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]-N-phenylcarbamoyloxy}methyl 2-(dimethylamino)acetate (Ex. 5a); {N-[3-(4-Methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]-N-phenylcarbamoyloxy}methyl 2-(dimethylamino)acetate hydrochloric acid salt (Ex. 5b); and {N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]-N-phenylcarbamoyloxy}methyl piperidine-4-carboxylate trifluoroacetic acid salt (Ex. 15).
- 11. The compound of claim 1 wherein R1 is H.
- 12. The compound of claim 11 wherein R1 is H.
- 13. The compound of claim 12 which is selected from the group:
3-(4-Methoxyphenyl)-1-phenyl-7-(phenylamino)-1,3,4-trihydropyrimidino[4,5-d]pyrimidin-2-one (Ex. 1g); 3-(4-Methoxyphenyl)-1-phenyl-7-(phenylamino)-1,3,4-trihydropyrimidino[4,5-d]pyrimidin-2-one methanesulfonate salt (Ex. 1h); 7-[(4-Hydroxyphenyl)amino]-3-(4-methoxyphenyl)-1-phenyl-1,3,4-trihydropyrimidino[4,5-d]pyrimidin-2-one (Ex. 18); and 3-(4-Methoxyphenyl)-7-[(4-methoxyphenyl)amino]-1-phenyl-1,3,4-trihydropyrimidino[4,5-d]pyrimidin-2-one.
- 14. A compound selected from the group:
3-(4-Methoxyphenyl)-1-phenyl-7-(phenylamino)-1,3,4-trihydropyrimidino[4,5-d]pyrimidin-2-one, 3-(4-Methoxyphenyl)-1-phenyl-7-(phenylamino)-1,3,4-trihydropyrimidino[4,5-d]pyrimidin-2-one methanesulfonate salt, 7-[(4-Hydroxyphenyl)amino]-3-(4-methoxyphenyl)-1-phenyl-1,3,4-trihydropyrimidino[4,5-d]pyrimidin-2-one, and 3-(4-Methoxyphenyl)-7-[(4-methoxyphenyl)amino]-1-phenyl-1,3,4-trihydropyrimid[4,5-d]pyrimidin-2-one.
- 15. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 1 and pharmaceutically acceptable carrier or excipient.
- 16. A method for treating cancer comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound of claim 1.
- 17. A method of controling cancer comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound of claim 1.
- 18. The method of claim 16 wherein the cancer is lung, colon or prostate cancer.
- 19. The method of claim 17 wherein the cancer is lung, colon or prostate cancer.
- 20. A compound selected from the group:
(Chloromethoxy)-N-[3-(4-methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]-N-benzamide [Example 4a]3-(4-Methoxyphenyl)-1-phenyl-7-{[4-(1,1,2,2-tetramethyl-1-silapropoxy) phenyl]amino}-1,3,4-trihydropyrimidino[4,5-d]pyrimidin-2-one [Example 19c], and N-[3-(4-Methoxyphenyl)-2-oxo-1-phenyl(1,3,4-trihydropyrimidino[4,5-d]pyrimidin-7-yl)]-N-[4-(1,1,2,2-tetramethyl-1-silapropoxy)phenyl]acetamide [Example 19d].
CONTINUITY INFORMATION
[0001] This application claims priority of Provisional application Serial No. 60/403,519, filed Aug. 14, 2002.
Provisional Applications (1)
|
Number |
Date |
Country |
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60403519 |
Aug 2002 |
US |