| abstract |
FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to novel bicyclic carboxamides of the formula (i) where: (1) X means N and (a) Z means =CR 1 -CR 2 and Y means N; (b) Z means =CR 1 and Y means O, S or NR 4 ,; or (c) Z means =CR 1 -N= and Y means CR 2 ; or (2) X means NR 4 ,; Z means -CR 1 = and Y means N; Q means O; R 1 and R 2 mean COR 6 , C(=NOR 6 )R 13 , alkyl-C-(=NOR 6 )R 13 , NR 8 R 9 , CF 3 or R 6 ; R 3 means C 1-6 -alkoxy-group; R 4 means H or alkyl; R 5 means heteroaryl optionally substituted with halogen atom, alkyl, CON-R 11 R 12 , CF 3 or CN, aryl substituted with halogen atom; R 6 means H, alkyl, cycloalkyl, aryl, heteroaryl, heterocycle, arylalkyl, hetero-arylalkyl or heterocycloalkyl; R 7 means alkyl, hydroxy-group, O-R 10 , N-R 8 R 9 , CN, CO 2 H, CO 2 R 10 , CONR 11 R 12 ; R 8 and R 9 means H or alkyl or NR 8 R 9 means heterocyclc ring optionally substituted with R 14 ; R 10 means alkyl, heterocycle; R 11 and R 12 means H or alkyl; R 13 ,R 14 ,R 15 mean alkyl; Y means O and n = 2-4, and their pharmaceutically acceptable salts. Compounds of the formula (i) show inhibitory effect on activity of phosphodiesterase and tumor necrosis factor and can be used in medicine as an agent for inhibition of phosphodiesterase and tumor necrosis factor. EFFECT: new compounds indicated above, valuable medicinal and biochemical properties. 13 cl, 2 tbl |