| abstract |
FIELD: organic chemistry, biochemistry, virology. n SUBSTANCE: invention relates to inhibitors of hepatitis C virus of the general formula (I): wherein R 1 means (C 1 -C 8 )-alkyl, (C 3 -C 7 )-cycloalkyl; m means 2; n means 1; R 2 means hydrogen atom (H), (C 1 -C 6 )-alkyl, (C 2 -C 6 )-alkenyl wherein each of them is optionally substituted with halogen atom; R 3 means (C 1 -C 8 )-alkyl optionally having the following substitute: (C 6 -C 10 )-aryl, (C 7 -C 14 )-alkylaryl, (C 1 -C 6 )-alkoxy-, carboxy-, hydroxy-, (C 7 -C 14 )-alkylaryloxy-group, (C 2 -C 6 )-alkyl ester, (C 8 -C 15 )-alkylaryl ester, (C 3 -C 7 )-alkenyl, (C 3 -C 7 )-cycloalkyl or (C 4 -C 10 )-alkylcycloalkyl wherein cycloalkyl or alkylcycloalkyl have optionally (C 1 -C 6 )-alkyl as a substitute; Y means H or (C 1 -C 6 )-alkyl under condition that if R 4 and R 5 means H then Y means H; B means H, R 4 -(C=O)-, R 4 O(C=O)-, R 4 -N(R 5 )-C(=O)- wherein R 4 means: (i) (C 1 -C 10 )-alkyl optionally having the following substitute: phenyl, 1-3 halogen atoms, hydroxy-group, -OC(O)-(C 1 -C 6 )-alkyl, (C 1 -C 6 )-alkoxy-group; (ii) (C 3 -C 7 )-cycloalkyl, (C 3 -C 7 )-cycloalkoxy-group or (C 4 -C 10 )-alkylcycloalkyl; (iii) (C 6 -C 10 )-aryl or (C 7 -C 16 )-arylalkyl wherein each of them is optionally substituted with halogen atom; (iv) Het; (v) bicyclo[1.1.1]pentane, or (vi) -C(O)O-(C 1 -C 6 )-alkyl; R 5 means H, (C 1 -C 6 )-alkyl optionally substituted with (C 1 -C 6 )-alkoxy-group under condition that R 4 means (C 1 -C 10 )-alkyl; X means oxygen atom (O), sulfur atom (S), -SO 2 , -CH 2 O or -NH; R' means Het or (C 6 -C 10 )-aryl optionally substituted with R a wherein R a means (C 1 -C 6 )-alkyl, (C 1 -C 6 )-alkoxy-group, (C 3 -C 7 )-cycloalkyl, halogen atom, (C 1 -C 6 )-alkyl, -CF 3 , dihalogen-(C 1 -C 6 )-alkoxy-, cyano-group, halogen atom, thioalkyl, hydroxy-group, di-(C 1 -C 6 )-alkyl-(alkoxy)-amine, (C 6 -C 10 )-aryl, (C 7 -C 14 )-alkylaryl or 5-7-membered monocyclic heterocycle under condition that X-R' doesn't mean compound of the formula: Also, invention relates to a method for treatment of hepatitis C virus (HCV) infection and inhibition of activity of HCV NS3-protease, and to a composition containing these compounds and using these compositions. Invention provides synthesis of novel compounds possessing valuable biological properties. n EFFECT: valuable medicinal properties of inhibitors and compositions. n 48 cl, 2 tbl, 472 ex |