| abstract |
FIELD: organic chemistry, chemical technology, pharmacy. SUBSTANCE: invention relates to derivatives of benzamide of the formula (I): wherein R 3 means (1-6C)-alkyl or halogen atom; R 1 is taken among substituents determined below in paragraph (A) and (B): (A): hydroxy-, halogen atom, trifluoromethyl, cyano-, nitro-, amino-, carboxy-, carbamoyl, (1-6C)-alkyl, (2-6C)-alkenyl, (2-6C)-alkynyl, (1-6C)-alkoxy-, (1-6C)-alkylamino, and so on; (B): halogen-(1-6C)- -alkyl, (1-6C)-alkoxy-(1-6C)-alkyl, carboxy-(1-6C)-alkyl, (1-6C)-alkoxycarbonyl-(1-6C)-alkyl, and so on; m = 1, 2 or 3; R 2 means hydroxy-, halogen atom, (1-6C)-alkyl, (2-6C)-alkenyl, (2-6C)-alkynyl or (1-6C)-alkoxy-; p = 0 or 1; q = 0, 1, 2, 3 or 4; and R 4 means aryl or cycloalkyl wherein R 4 is substituted with 1, 2 or 3 substituents taken among paragraph (C) and (D) below: (C): hydrogen atom, hydroxy-, halogen atom, trifluoromethyl, cyano-, mercapto- nitro-, amino-, carboxy-, carbamoyl, (1-6C)-alkyl, (2-6C)-alkenyl, (2-6C)-alkynyl, (1-6C)-alkoxy- , (1-6C)-alkylamino-, and so on; (D): halogen-(1-6C)- alkyl, (1-6C)-alkoxy-(1-6C)-alkyl, carboxy-(1-6C)- alkyl, (1-6C)-alkoxycarbonyl-(1-6C)-alkyl, and so on. Invention proposes methods for preparing derivative of benzamide. Invention proposes pharmaceutical composition eliciting inhibitory activity with respect to cytokines that contains an active component and pharmaceutically acceptable excipient or carrier. The composition contains effective dose of benzamide derivative of the formula (I) as an active component. Invention provides preparing derivatives of benzamide using as inhibitors of cytokine-mediated disease. EFFECT: improved preparing method, valuable medicinal properties. 10 cl, 4 tbl, 77 ex |