DERIVATIVES OF NOR-SECO-CHIMBACINE, PHARMACEUTICAL COMPOSITION AND METHOD FOR INHIBITING BASED ON THEREOF Russian patent published in 2007 - IPC C07D405/06 C07D405/08 C07D405/14 C07D409/14 C07D413/14 C07D417/14 A61K31/365 A61K31/443 A61K31/4436 A61K31/4439 A61K31/444 A61K31/497 

FIELD: organic chemistry, medicine.

SUBSTANCE: invention relates to compound represented by the structural formula: or its pharmaceutically acceptable salt wherein Z represents -(CH₂)_n-; double dotted line represents a double bond; n = 0-2; R¹ and R² are chosen independently from the group comprising hydrogen atom (H), alkyl with 1-6 carbon atoms; R³ means H, hydroxy-, alkoxy-group with 1-6 carbon atoms, -C(O)OR¹⁷ or alkyl with 1-6 carbon atoms; Het means monocyclic heteroaromatic group consisting of 6 atoms and comprising 5 carbon atoms and one heteroatom chosen from nitrogen atom (N) and wherein Het is bound through ring carbon atom and wherein Het-group has one substitute W chosen independently from the group comprising bromine atom (Br), heterocycloalkyl representing group consisting of 4 carbon atoms and one heteroatom chosen from N; heterocycloalkyl representing group consisting of 4 carbon atoms and one heteroatom chosen from N substituted with OH-substituted alkyl with 1-6 carbon atoms or =O; R²¹ -aryl-NH-; -C(=NOR¹⁷)R¹⁸; R²¹-aryl; R⁴¹-heteroaryl representing group consisting of 5-6 atoms comprising 3-5 carbon atoms and 1-4 heteroatoms chosen independently from the group: N, S and O; R⁸ and R¹⁰ are chosen independently from group comprising R¹; R⁹ means H; R¹¹ is chosen from group comprising R¹ and -CH₂OBn wherein Bn means benzyl; B means -(CH₂)_n4CR¹²=CR^12a(CH₂)_n5; n₄ and n₅ mean independently 0; R¹² and R^12a are chosen independently from group comprising H, alkyl with 1-6 carbon atoms; X means -O-; Y means =O; R¹⁵ is absent as far as double dotted line mean a simple bond; R¹⁶ means lower alkyl with 1-6 carbon atoms; R¹⁷ and R¹⁸ are chosen independently from group comprising H, alkyl with 1-6 carbon atoms; R²¹ means 1-3 substituted chosen independently from group comprising hydrogen atom, -CN, -CF₃, halogen atom, alkyl with 1-6 carbon atoms and so on; R²² is chosen independently from group comprising hydrogen atom; R²⁴-alkyl with 1-10 carbon atoms; R²⁵-aryl and so on; R²³ is chosen independently from group comprising hydrogen atom, R²⁴-alkyl with 1-10 carbon atoms, R²⁵-aryl and -CH₂OBn; R²⁴ means 1-3 substitutes chosen independently from group comprising hydrogen atom, halogen atom, -OH, alkoxy-group with 1-6 carbon atoms; R²⁵ means hydrogen atom; R⁴¹ means 1-4 substitutes chosen independently from group comprising hydrogen atom, alkyl with 1-6 carbon atoms and so on. Also, invention relates to a pharmaceutical composition possessing the inhibitory activity with respect to receptors activated by protease and comprising the effective dose of derivative of nor-seco-chimbacine of the formula (I) and a pharmaceutically acceptable excipient. Also, invention relates to methods for inhibition of thrombin and cannabinoid receptors comprising administration in mammal derivative of nor-seco-chimbacine of the formula (I) in the effective dose as active substance. Invention provides derivatives of nor-seco-chimbacine as antagonists of thrombin receptors.

EFFECT: valuable medicinal and biological properties of compounds and pharmaceutical composition.

8 cl, 1 tbl, 18 ex