FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to derivatives of amide of the formula (I): wherein R3 represents (1-6C)-alkyl or halogen atom; m = 0, 1, 2 or 3; R1 represents hydroxy- -group, halogen atom, trifluoromethyl group, nitro-group, amino-group, (1-6C)-alkyl, (2-6C)-alkenyl, (2-6C)-alkynyl, (1-6C)-alkoxy-group, (1-6C)-alkylamino-group, di-[(1-6C)-alkyl] amino-group, amino-(2-6C)-alkylamino-group, (1-6C)-alkylamino-(2-6C)-alkylamino-group and so on; or R1 represents aryl, aryl-(1-6C)-alkyl, heteroaryl, heteroaryl-(1-6C)-alkyl, heteroaryloxy-group, heterozry-(1-6C)-alkoxy-group, heterocyclyl, heterocyclyl-(1-6C)-alkyl or heterocyclyloxy-group; p = 0, 1 or 2; R2 represents hydroxy-group, halogen atom, trifluoromethyl group, (1-6C)-alkyl or (1-6C)-alkoxy-group; R4 represents aminogroup, (1-6C)- alkylamino-group, di-[(1-6C)-alkyl]-amino-group, amino-(1-6C)-alkyl, (1-6C)-alkylamino-(1-6C)-alkyl and so on; or R4 represents heteroaryl, heteroaryl-(1-6C)-alkyl, heteroaryloxy, heteroaryl-(1-6C)-alkoxy-group, heterocyclyl and so on; q = 0, 1, 2, 3 or 4; Q2 represents heteroaryl, heteroaryloxy or heteroaryl-(1-6C)-alkoxy- group and Q2 is substituted optionally with 1, 2 or 3 substituents taken among hydroxy-group, halogen atom, trifluoromethyl, (1-6C)-alkyl, (2-6C)-alkenyl, (2-6C)-alkynyl, (1-6C)-alkoxy-group, amino-(1-6C)-alkyl and so on; or its pharmaceutically acceptable salt or ester cleaving in vivo. Invention proposes methods for preparing derivatives of amide. Also, invention proposes pharmaceutical composition eliciting cytokine-inhibitory effect and containing active component and pharmaceutically acceptable excipient or carrier. Composition comprises effective amount of amide derivative of the formula (I) or its pharmaceutically acceptable salt of ester cleaving in vivo as an active component. Invention provides preparing amide derivatives of the formula (I) using as inhibitors of cytokine-mediated diseases. EFFECT: improved preparing method, valuable medicinal properties of compounds. 14 cl, 6 tbl
Authors
Dates
2003-12-20—Published
1999-09-21—Filed