| 摘要 |
Inhibitors of HBV replication of formula (I);;including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein X and R1 to R8 have the meaning as defined herein.;The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy. |
| 主权项 |
1. A compound of Formula (I) or a stereoisomer or tautomeric form thereof, wherein: X is S or CR4, wherein one X is S and the other two X are each CR4; R2 is fluoro or hydrogen; R1 and R3 are each independently selected from the group consisting of hydrogen, fluoro, chloro, bromo, CHF2, CH2F, CF3, CN and methyl, wherein at least one of R1 and R3 is not hydrogen, and R1 and R3 are not ortho methyl or ortho chloro; R4 is selected from the group consisting of hydrogen, halogen, C1-C3alkyl, cyclopropyl, CHF2, CH2F and CF3, wherein at least one R4 is hydrogen; R5 is hydrogen; R6 is selected from the group consisting of C1-C6alkyl, C1-C3alkyl-R7, and a 3-7 membered saturated ring optionally containing one or more heteroatoms, each heteroatom independently selected from the group consisting of O, S and N, wherein each of said 3-7 membered saturated ring and C1-C6alkyl is independently optionally substituted with one or more substituents, each substituent independently selected from the group consisting of hydrogen, fluoro, OH, CF3 and C1-C4alkyl; R7 is a 3-7 membered saturated ring optionally containing one or more heteroatoms, each heteroatom independently selected from the group consisting of O, S and N, and wherein said 3-7 membered saturated ring is optionally substituted with C(═O)—R8; R8 is selected from the group consisting of C1-C3alkoxy and —NH2; wherein
if R1 is methyl, R2 is fluoro, and R3 is hydrogen, then R6 is not methyl; or a pharmaceutically acceptable salt or a solvate thereof. |
