Fused bicyclic sulfamoyl derivatives and the use thereof as medicaments for the treatment of hepatitis B

摘要

Inhibitors of HBV replication of Formula (I);
including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein A-E, R1, R2, R3 and R5, 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) a stereoisomer, tautomeric form thereof, a pharmaceutically acceptable salt, or a solvate thereof, wherein: A is N, C or O; B is C or N; D is C or N; E is C or N; wherein if A and E are either N or C, they are optionally substituted with R4; R1 is hydrogen or C1-C3alkyl; R2 is C1-C6alkyl, C1-C3alkyl-R6, benzyl, or a 3-7 membered saturated ring optionally containing one or more heteroatoms each independently selected from the group consisting of O, S and N, said C1-C6alkyl or a 3-7 membered saturated ring optionally being substituted with one or more substituents each independently selected from the group consisting of hydrogen, halo, C1-C3alkyloxy, C1-C4alkyl, OH, CN, CFH2, CF2H and CF3; or R1 and R2 together with the nitrogen to which they are attached form a 5-7 membered saturated ring optionally being substituted with one or more substituents each independently selected from the group consisting of hydrogen, halogen, C1-C4alkyloxy, C1-C3alkyl, OH, CN, CFH2, CF2H and CF3; each R3 is independently selected from the group consisting of hydrogen, halo, C1-C4alkyloxy, C1-C4alkyl, OH, CN, CFH2, CF2H, CF3 and a 3-5 membered saturated ring optionally containing one or more heteroatoms each independently selected from the group consisting of O and N; R4 is hydrogen, C1-C4alkyl, C3-C5cycloalkyl, —(C═O)C1-C4-alkyl, or —(C═O)—C1-C3alkyloxy; or if A or E is C, then R4 is hydrogen, halogen, C1-C4alkyl, C3-C5cycloalkyl, —(C═O)C1-C4-alkyl, —(C═O)—C1-C3alkyloxy; R5 is hydrogen or halogen; and R6 is a 3-7 membered saturated ring optionally containing one or more heteroatoms each independently selected from the group consisting of O, S and N, said 3-7 membered saturated ring optionally being substituted with one or more substituents each independently selected from the group consisting of hydrogen, halo, C1-C3alkyloxy, C1-C4alkyl, OH, CN, CFH2, CF2H, and CF3.