| 摘要 |
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-HT2C 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 |
