DERIVATIVES OF SUBSTITUTED TETRACYCLIC AZEPINE, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION, INTERMEDIATE SUBSTANCE AND METHOD OF ITS SYNTHESIS Russian patent published in 2001 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes compounds of the general formula (I) , their pharmaceutically acceptable acid additive salts, their stereochemical isomeric forms, their N-oxides where R¹ means hydrogen atom, C_1-6-alkyl; R² means hydrogen atom, C_1-6-alkyl, trihaloidmethylcarbonyl, C_1-6-alkyl substituted with hydroxyl, carboxyl, C_1-6-alkyl- carbonyloxy-group; R¹ and R² taken in common with nitrogen atom to which they are bound form morpholinyl ring or heterocycle; R¹⁵, R¹⁶, R¹⁷, R¹⁸, R²⁰ where each means hydrogen atom; R²¹ and R²² in common form bivalent radical C_4-5-alkanediyl; R²³ means hydrogen atom, C_1-6-alkyl, trihaloidmethylcarbonyl, aryl, di-(aryl)-methyl and aryl means unsubstituted phenyl or phenyl monosubstituted with halogen atom; R³ and R⁵ where each means hydrogen, halogen atom, C_1-6-alkyl; R⁴ and R⁶ each means hydrogen atom, C_1-6-alkyl, halogen atom, C_1-6-alkoxy- group; R⁷, R⁸, R¹³, R¹⁴ where each means hydrogen atom, C_1-6-alkyl or R⁷ and R⁸ taken in common form mono-(cyano)-methylene or methylene; R⁹ means hydrogen, halogen atom, C_1-6-alkyl or trifluoromethyl; R¹⁰ means hydrogen, C_1-6/ -alkyl, halogen atom, trifluoromethyl, di-(C_1-6-alkyl)-amino-group; R¹¹ means hydrogen atom, C_1-6-alkyl, halogen atom, C_1-6-alkyloxy-group, trifluoromethyl; R¹² means hydrogen atom, C_1-6-alkyl, trifluoromethyl. These compounds are tested as мХФП-antagonists in rats. Compounds of the formula (I) are used as therapeutic agents for prophylaxis or treatment of patients with central nervous system disorders, cardiovascular or gastroenteric disorders. Invention describes also method of synthesis of compounds of the formula (I), pharmaceutical composition based on their, intermediate substance and method of its synthesis. EFFECT: improved method of synthesis, valuable medicinal properties. 11 cl, 6 tbl, 24 ex