Claims
- 1. A compound of the formula:
- 2. A compound of claim 1 selected from the group of:
1-Cyclopentyl-7-(4-diethylamino-butylamino)-3-(2,6-difluoro-3-hydroxy-5-methoxy phenyl)-3,4-dihydro -1H -pyrimido[4,5-d]pyrimidin-2-one; 1-Cyclopentyl-7-(4-diethylamino-butylamino)-3-(2,6-difluoro-3,5-dimethoxy-phenyl)-3,4-dihydro-1H-pyrimido [4,5-d]pyrimidin-2-one; (S,S)-1-Cyclopentyl-3-(2,6-difluoro-3,5-dimethoxy-phenyl)-7-[(5-hydroxymethyl-2-phenyl-[1,3]dioxolan-4-ylmethyl)-amino]-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; (S,S)-1-Cyclopentyl-3-(2,6-difluoro-3,5-dimethoxy-phenyl)-7-(2,3,4-trihydroxy-butylamino)-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; or 1-Cyclopentyl-3-(2,6-difluoro-3,5-dimethoxy-phenyl)-7-(4-hydroxy-cyclohexylamino)-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; 1-Cyclopentyl-3-(2,6-difluoro-3,5-dimethoxy-phenyl)-7-(2-hydroxy-1-hydroxymethyl-ethylamino)-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; 7-(3-Amino-2-hydroxy-propylamino)-1-cyclopentyl-3-(2,6-difluoro-3,5-dimethoxy-phenyl)-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; 1-Cyclopentyl-3-(2,6-difluoro-3,5-dimethoxy-phenyl)-7-[2-(2-hydroxy-ethoxy)-ethylamino]-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; 1-Cyclopropyl-7-(4-diethylamino-butylamino)-3-(2,6-difluoro-3,5-dimethoxy-phenyl)-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; or 7-(4-Diethylamino-butylamino)-3-(2,6-difluoro-3,5-dimethoxy-phenyl)-1-ethyl-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; or a pharmaceutically acceptable salt or ester form thereof.
- 3. A compound of claim 1 selected from the group of:
3-(2,6-Difluoro-3,5-dimethoxy-phenyl)-1-ethyl-7-(2-hydroxy-1-hydroxymethyl-ethylamino)-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; 3-(2,6-Difluoro-3,5-dimethoxy-phenyl)-1-ethyl-7-(4-hydroxy-cyclohexylamino)-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; 1-Cyclopentyl-3-(2,6-difluoro-3,5-dimethoxy-phenyl)-7-(2,3-dihydroxy-butylamino)-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one 1-Cyclopentyl-3-(2,6-difluoro-3,5-dimethoxy-phenyl)-7-(2,3-dihydroxy-propylamino)-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; or 7-(4-Amino-2,3-dihydroxy-butylamino)-1-cyclopentyl-3-(2,6-difluoro-3,5-dimethoxy-phenyl)-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; 1-Cyclopentyl-3-(2-fluoro-3,5-dimethoxy-phenyl)-7-([S,S]-2,3,4-trihydroxy-butylamino)-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; 3-(2,6-Difluoro-3,5-dimethoxy-phenyl)-1-ethyl-7-[2-(2-hydroxy-ethoxy)-ethylamino]-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; 7-(4-Amino-2,3-dihydroxy-butylamino)-3-(2,6-difluoro-3,5-dimethoxy-phenyl)-1-ethyl-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; 7-{3-[Bis-(2-hydroxy-ethyl)-amino]-propylamino}-3-(2,6-difluoro-3,5-dimethoxy-phenyl)-1-ethyl-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; or 1-Cyclopentyl-3-(2,6-difluoro-3,5-dimethoxy-phenyl)-7-(2,3-dihydroxy-propylamino)-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; or a pharmaceutically acceptable salt or ester form thereof.
- 4. A compound of claim 1 selected from the group of:
3-(2,6-Difluoro-3,5-dimethoxy-phenyl)-7-(2,3-dihydroxy-butylamino)-1-ethyl-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; Ethyl-4-[3-(2,6-difluoro-3,5-dimethoxy-phenyl)-7-methylamino-2-oxo-3,4-dihydro-2H-pyrimido[4,5-d]pyrimidin-1-yl]-cyclohexanecarboxylate; 4-[3-(2,6-Difluoro-3,5-dimethoxy-phenyl)-7-methylamino-2-oxo-3,4-dihydro-2H-pyrimido[4,5-d]pyrimidin-1-yl]-cyclohexanecarboxylic acid; 7-Amino-3-(2,6-difluoro-3,5-dimethoxy-phenyl)-1-piperidin-4-yl-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; compound with trifluoroacetic acid; or 1-Cyclopentyl-3-(2-fluoro-3,5-dimethoxy-phenyl)-7-(2-hydroxy-1-hydroxymethyl-ethylamino)-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; 1-Ethyl-3-(2-fluoro-3,5-dimethoxy-phenyl)-7-(4-hydroxy-butylamino)-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; (S)-1-Cyclopentyl-7-(2,3-dihydroxy-propylamino)-3-(2-fluoro-3,5-dimethoxy-phenyl)-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; 1-Ethyl-3-(2-fluoro-3,5-dimethoxy-phenyl)-7-(4-hydroxy-cyclohexylamino)-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; 4-[3-(2,6-Difluoro-3,5-dimethoxy-phenyl)-7-methylamino-2-oxo-3,4-dihydro-2H-pyrimido[4,5-d]pyrimidin-1-yl]-piperidine-1-carboxylic acid; or 3-(2,6-Difluoro-3,5-dimethoxy-phenyl)-7-methylamino-1-piperidin-4-yl-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; 3-(2,6-Difluoro-3,5-dimethoxy-phenyl)-7-(2,3-dihydroxy-propylamino)-1-ethyl-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; 1-Cyclopentyl-7-(4-diethylamino-butylamino)-3-(3-ethoxy-2,6-difluoro-phenyl)-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; (R)-1-Cyclopentyl-7-(2,3-dihydroxy-propylamino)-3-(2-fluoro-3,5-dimethoxy-phenyl)-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; 1-Ethyl-3-(2-fluoro-3,5-dimethoxy-phenyl)-7-[2-(2-hydroxy-ethoxy)-ethylamino]-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; or 1-Cyclopentyl-3-(2-fluoro-3,5-dimethoxy-phenyl)-7-(trans-4-hydroxy-cyclohexylamino)-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one; or a pharmaceutically acceptable salt or ester form thereof.
- 5. A pharmaceutical composition comprising a pharmaceutically effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier.
- 6. A compound of the formula:
- 7. A compound of claim 9 wherein of R2 and R3 are fluorine, and R4, R5, Ra, and R are as defined in claim 10.
- 8. A compound of claim 9 wherein of R2 and R3 are fluorine, R4 is —OCH3, R5 is —OCH3 or —OCH2CH3, Ra is NH2, I, CN, —CH2CN, —C(O)CN, —CH2OH, —C(O)H, —C(O)OR, —CH2C(O)OR, or —C(O)C(O)OR; and R is H or C1-C6 alkyl.
- 9. A compounds of the formulae:
Parent Case Info
[0001] This application is a Non-Provisional Utility Application, which claims priority to U.S. provisional application Serial No. 60/398,638, filed Jul. 25, 2002.
Provisional Applications (1)
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Number |
Date |
Country |
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60398638 |
Jul 2002 |
US |