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(11)    Patent No :    AP 2188   
(21)    Application No :    AP/P/2006/003693   
(22)    Filing Date :    21.01.2005   
(24)    Date of Grant &    14.12.2010   
           
(45)    Publication :

(30)  Priority Data       
(33) Country    (31) Number    (32) Date
US    60/538,768    23.01.2004

(84)    Designated State

BW    GM    GH    KE    LS    MW  MZ   NA   SL
SD    SZ    T Z    UG    ZM    ZW
 
(73) Applicant(s)

JANSSEN PHARMACEUTICA N.V., Turnhoutseweg 30,

B-2340 Beerse,
Belgium

(72) Inventors

GUILLEMONT Jerome Emile Georges, France

PASQUIER Elisabeth Thérèse Jeanne, France

(74) Representative

HONEY & BLANCKENBERG
 

(51)  International  Classification   C07D413/06 (2006.01)    C07D413/14 (2006.01)


(54)    Title

Substituted quinolines and their use as mycobacterial inhibitors

(57)    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 R1 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 ; R2 is hydrogen, hydroxy, thio, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula (Ic);

R3 is alkyl, Ar, Ar-alkyl, Het or Het -alkyl; R4 is hydrogen, alkyl or benzyl; R5 is

hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R5 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 ; R6 is hydrogen, alkyl, Ar or Het R7 is hydrogen or alkyl; R8 is oxo ; or R7 and R8 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

(56)    Documents Cited :    WO 00/34265 A   US 5 965 572 A

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