HEPATITIS C VIRUS MACROCYCLIC INHIBITORS Russian patent published in 2013 - IPC C07D487/04 C07D245/04 C07K5/06 C07K5/78 A61K38/05 A61P31/14 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula (I) a pharmaceutically acceptable salt thereof wherein each dash line (represented as ---) represents a double bond; X represents N or CH; R^1a and R^1b independently represent hydrogen or C_1-6-jalkyl; L represents -O-; R² represents hydrogen; R³ represents hydrogen or C_1-6-alkyl; R⁴ represents quinolinyl substituted by one, two or three substitutes specified in C_1-6-alkyl, C_1-6-alkyloxy, thiazolyl or pyrazolyl, wherein said thiazolyl or pyrazolyl are substituted on any carbon atom by C_1-6-alkyl; n is equal to 3, 4, 5 or 6; p is equal to 1 or 2. The invention refers to a pharmaceutical composition possessing the properties of KS3/4a-protease HCV inhibitors, containing a carrier, and an virally effective amount of the compound of formula (I) as an active ingredient. The method for preparing the compound of formula (I), wherein the above method involves forming an amide bond of an intermediate product (2a) and sulphonylamide (2b), as presented by the diagram, wherein G represents a group Also, the invention refers to alternative methods for preparing the compound of formula (I).

EFFECT: there are presented macrocyclic compounds possessing inhibitory activity on hepatitis C virus (HCV) replication.

13 cl, 1 tbl, 17 ex