Macrocyclic indole derivatives useful as hepatitis C virus inhibitors
View Patent ↗Inhibitors of HCV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein Y, R 1 , R 2 , R 4 and n have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.
1. A compound of formula (I),
or a stereochemically isomeric form, or a pharmaceutically acceptable salts, thereof, wherein:
R 1 is selected from hydrogen, halo and C 1-4 alkoxy;
R 2 is selected from C 1-4 alkyl and C 3-6 cycloalkyl;
R 4 is C 3-7 cycloalkyl optionally substituted with halo;
n is 1 or 2;
Y is selected from
a is 2,3,4 or 5;
each b is independently 1 or 2;
R 3 and R 3 ′ are independently selected from hydrogen, C 1-6 alkyl and C 3-6 cycloalkyl.
2. A compound according to claim 1 wherein Y is selected from —N(CH 3 )—(CH 2 ) 4 —N(CH 3 )—,
3. A compound according to claim 1 wherein R 1 is hydrogen or methoxy or fluoro.
4. A compound according to claim 1 wherein R 2 is selected from methyl, ethyl, iso-propyl and cyclopropyl.
5. A compound according to claim 1 wherein R 4 is selected from cyclohexyl and 2-fluorocyclohexyl.
6. A compound according to claim 1 wherein n is 1.
7. A compound according to claim 1 selected from
or a stereochemically isomeric form, or a pharmaceutically acceptable salt, thereof.
8. A pharmaceutical composition comprising a carrier, and as active ingredient an anti-virally effective amount of a compound as claimed in claim 1 .
9. A pharmaceutical composition according to claim 8 , further comprising at least one other anti-HCV compound.
10. A pharmaceutical composition according to claim 8 , further comprising at least one anti HIV compound.