| abstract |
Quinoline derivs. of formula (I), their pharmaceutically acceptable hydrates, acid addition salts and salts with alkali metal, alkaline earth metals and guanidine are new. In formula (I), X1 and X2 = H or halo, esp. Cl or F; R1, R2 and R3 = H, Me, Cl or F but not all 3 can be the same; R4 and R5 complete a 5-6 membered heterocyclic ring which may additionally include O, S, SO, SO2, NR6 or CON-R6, and opt. C-substd., 1-3 times, by 1-4C alkyl, phenyl (opt. substd. by 1-3 Cl, F, Br, Me, phenyl, OH, MeO, benzyloxy, NO2 or piperidino); cyclohexyl; 2-thienyl; OH; 1-3C alkoxy; NH2; MeNH or EtNH; R6 = H, 1-6C alkyl, alkenyl or alkynyl (opt. substd. by 1 or 2 OH, 1-3C alkoxy, 1-3C mono- or di-alkylamino; CN or 1-4C alkoxycarbonyl); phenyl(1-4C)alkyl (opt. ring substd.); phenacyl (opt. substd. by 1 or 2 OH, OMe, Cl or F); up to 6C oxoalkyl; COR7; CN or SO2R8; R7 = H, 1-4C alkyl (opt. substd. by 1 or 2 NH2; 1-3C alkoxycarnonyl, COOH, 1-3C alkoxy or halo); 1-4C alkoxy or NH2 (opt. substd. by 1 or 2 1-5C alkyl); R8 = 1-3C alkyl. Also new are the intermediates of formula (A) (where Ra = Rb = F or Cl). |