Mycobacterial inhibitors

Details Mycobacterial inhibitors Mycobacterial inhibitors

2005-01-21

2008-03-04

Habte, Kahsay (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C514S233500, C514S233800, C544S096000

Reexamination Certificate

active

07338949

ABSTRACT:
The present invention relates to novel substituted quinoline derivatives according to the general formula (Ia) or the general formula (Ib)salts, quaternary amines, stereochemically isomeric forms, tautomeric forms and N-oxide forms thereof, wherein R1is 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; R2is hydrogen, hydroxy, thio, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formulaR3is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; R4is hydrogen, alkyl or benzyl; R5is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R5radicals 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; R6is hydrogen, alkyl, Ar or Het; R7is hydrogen or alkyl; R8is oxo; or R7and R8taken together form the radical —CH═CH—N═; Z is CH2or C(═O). The claimed compounds are useful for the treatment of mycobacterial diseases, particularly those diseases caused by pathogenic mycobacteria such asM. tuberculosis, M. bovis, M. avium, M. smegmatisandM. 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.

REFERENCES:
patent: 5965572 (1999-10-01), Ellis et al.
patent: WO 00/34265 (2000-06-01), None
patent: WO 04/011436 (2004-02-01), None
Hackh's Chemical Dictionary, 4th Edition, edited by J. Grant (1972), McGraw Hill, New York (p. 27).

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