]1,4]DIAZEPINO[6,7,1-IJ]QUINOLINE DERIVATIVES USED AS ANTI-PSYCHOTIC AGENTS AND AGENTS AGAINST OBESITY Russian patent published in 2007 - IPC C07D471/06 C07D243/00 A61K31/5513 A61P25/00 A61P3/00 A61P1/04 

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of [1,4]diazepino[6,7,1-IJ]-quinoline of the general formula (I): wherein R¹ represents hydrogen atom, (C₁-C₆)-alkyl, (C₂-C₆)-alkanoyl or (C₇-C₁₁)-carboarylalkoxy-group; each R² and R³ represents independently hydrogen atom, hydroxy-group, (C₁-C₆)-alkyl, (C₁-C₆)-alkoxy-group, halogen atom, (C₂-C₆)-carboalkyloxy-group, (C₁-C₆)-perfluoroalkyl, (C₂-C₆)-alkanoyloxy-group, (C₂-C₆)-alkanoyl, (C₆-C₈)-aroyl, (C₅-C₇)-aryl, (C₆-C₁₃)-alkylaryl having 5-7 carbon atoms in aryl moiety; R⁴ and R⁵ represents independently hydrogen atom or (C₁-C₆)-alkyl, or R⁴ and R⁵ taken in common with carbon atoms with which they are bound form cyclic group chosen from (C₄-C₈)-cycloalkane, (C₄-C₈)-cycloalkene; each R⁶ and R⁷ represents independently hydrogen atom or (C₁-C₆)-alkyl; n = 1 or 2; a dotted line means a double bond optionally. Also, invention describes using compounds of the formula (I) in preparing a drug used in treatment of different psychotic disorders. Also, invention relates to a pharmaceutical composition possessing activity as 5-HT_2C antagonist based on proposed compounds, and a method for synthesis of compounds of the formula (I). Invention provides synthesis of novel compounds, preparing a pharmaceutical composition and a drug based on thereof.

EFFECT: improved method of synthesis, valuable medicinal properties of compounds and pharmaceutical composition.

53 cl, 1 tbl, 34 ex