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US 2010/0075988 A1Published application
Tetrahydroquinazoline compounds and their use in preparing medicaments for treating and preventing virosis
AssigneeBeijing Molecule Science and Technology Co., Ltd.
InventorsSong Li, Xuejun Zhu, Guoming Zhao, Lili Wang, Wu Zhong, Zhibing Zheng, Junhai Xiao
Life of this patent
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Abstract
The present invention relates to a compound of formula (I) or isomers thereof, or pharmaceutically acceptable salts or hydrates thereof. The present invention further relates to processes for the preparation of the compounds of formula (I) and optical isomers, and to the use of the compounds of formula (I), or isomers thereof, or pharmaceutically acceptable salts or hydrates thereof as medicaments, in particular as medicaments for the treatment and prevention of Hepatitis B.
Claims9
A compound of formula (I)
- or an isomer thereof, or a pharmaceutically acceptable salt or hydrate thereof,
- wherein
- R1 represents hydrogen, (C1-C4)-alkyl, (C2-C4)-alkenyl, (C2-C6)-acyl, sulfonyl or benzoyl,
- R2 represents a 5- or 6-membered aryl or heteroaryl mono-substituted or multiple-substituted with the same or different substituents selected from:
- hydrogen, halogen, hydroxyl, cyano, trifluoromethyl, nitro, benzyl, (C1-C6)-alkyl, (C1-C6)-alkoxyl, (C1-C6)-alkylthio, (C1-C6)-alkoxylcarbonyl, (C1-C6)-acyloxy, amino, (C1-C6)-alkylamino, (C1-C6)-dialkylamino, and (C1-C6)-acylamino,
- R3 represents an aryl or heteroaryl mono-substituted or multiple-substituted with the same or different substituents selected from:
- hydrogen, halogen, trifluoromethyl, trifluoromethoxyl, trifluoromethanesulfonyl, nitro, cyano, carboxyl, hydroxyl, (C1-C6)-alkoxyl, (C1-C6)-alkoxycarbonyl and (C1-C6)-alkyl, wherein the alkyl can be substituted with an aryl having 6-10 carbon atoms, halogen, or a group represented by —S—R5, NR6R7, CO—NR8R9 or -A-CH2—R10,
- wherein
- R5 represents phenyl which can be optionally substituted with halogen,
- R6, R7, R8 and R9 are the same or different, and independently represents hydrogen, phenyl, hydroxyl-substituted phenyl, hydroxyl, (C1-C6)-acyl or (C1-C6)-alkyl, wherein the alkyl can be substituted with hydroxyl, halogen, (C1-C6)-alkoxycarbonyl, phenyl or hydroxyl-substituted phenyl,
- A represents O, S, SO or SO2,
- R10 represents phenyl optionally mono- or multiple-substituted with same or different substituents selected from:
- halogen, nitro, trifluoromethyl, (C1-C6)-alkyl and (C1-C6)-alkoxy, and
- R4 represents an optionally mono- or multiple-substituted, the same or different substituent selected from:
- hydrogen, halogen, nitro, cyano, hydroxyl, (C1-C6)-alkyl, (C1-C6)-alkoxyl, (C1-C6)-alkoxylcarbonyl, aryl and heteroaryl having 6-10 carbon atoms, wherein the aryl or heteroaryl can be substituted with halogen or (C1-C6)-alkyl.
12 more elements
Dependencies are inferred from the claim text.