Original document(53 pages)  中文版
    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 R<1> is 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 ; R<2> is hydrogen, hydroxy, thio, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula (Ic);< >R<3> is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; R<4> is hydrogen, alkyl or benzyl; R<5> is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl ; or two vicinal R<5> radicals 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 ; R<6> is hydrogen, alkyl, Ar or Het R<7> is hydrogen or alkyl; R<8> is oxo ; or R<7> and R<8> taken together form the radical - CH=CH-N=; Z is CH2 or C(=O). The claimed compounds are useful for the treatment of mycobacterial 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.
Application Number
申请号
200580002679 Application Date
申请日
2005.01.21
Title 名称 Substituted quinolines and their use as mycobacterial inhibitors
Publication Number
公开号
1910177 Publication Date
公开日
2007.02.07
Approval Pub. Date Granted Pub. Date
International Classification 分类号 C07D413/06;C07D413/14;A61K31/5355;A61P31/10
Applicant(s) Name
申请人
Janssen Pharmaceutica NV
Address 地址
Inventor(s) Name 发明人 Guillemont Jerome E. G.;Pasquier Elisabeth T. J.
Attorney & Agent 代理人 li bingai
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