7-AMINO-1-(SUBST.CYCLOPROPYL)-1,4-DIHYDRO-4-OXO-3-CHINOLINCARBONSAEUREN, VERFAHREN ZU IHRER HERSTELLUNG SOWIE DIESE ENTHALTENDE ANTIBAKTERIELLE MITTEL.

摘要

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).