| 摘要 |
The present invention relates to novel substituted quinoline derivatives according to the general formula (Iа) or the general formula (Ib) salts, quaternary amines, stereochemically isomeric forms, tautomeric forms and N-oxide forms thereof, wherein Ris hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2, 3 or 4; Ris hydrogen, hydroxy, thio, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula (Ic); Ris alkyl, Ar, Ar-alkyl, Het or Het-alkyl; Ris hydrogen, alkyl or benzyl; Ris hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal Rradicals may be taken together to form together with the phenyl ring to which they are attached a naphthyl; r is 1, 2, 3, 4 or 5; Ris hydrogen, alkyl, Ar or Het Ris hydrogen or alkyl; Ris oxo; or Rand Rtaken together form the radical - CH=CH-N=; Z is CH, or C(=O). The claimed compounds are useful for the treatment of mycobaclerial diseases, particularly those diseases caused by pathogenic mycobacteria such as M. tuberculosis, M. bovis, M. avium, M. smegmatis and M. marinum. Also claimed is a pharmaceutical composition containing a compound of the present invention, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of mycobacterial diseases and a process for preparing the claimed compounds., (Ia), (Ib) |
