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(11)    Patent No :    AP 2327    (73) Applicant(s)       
(21)    Application No :    AP/P/2007/004054    JANSSEN PHARMACEUTICA N.V., Turnhoutseweg 30,       
            B-2340 Beerse,       
(22)    Filing Date :    08.12.2005    Belgium       
(24)    Date of Grant &    25.11.2011           
(45)    Publication :

(30)  Priority Data    (72) Inventors

    (33) Country    (31) Number    (32) Date    ANDRIES Koenraad Jozef Lodewijk Marcel, Belgium   
    EP            04078529.7    24.12.2004    KOUL Anil, Belgium   
    EP            05105008.6    08.06.2005       
                        (74) Representative   
(84)    Designated State                   
    BW    GM    GH    KE    LS    MW    MZ   NA   SL    HONEY & BLANCKENBERG   
    SD    SZ    T Z    UG    ZM    ZW               
(51)    International    Classification    A61K 31/47 (2006.01)    A61K 31/4704 (2006.01)   
                            A61P 31/06 (2006.01)       

(54)    Title

Quinoline derivatives for the treatment of latent tuberculosis

(57)    Abstract

Use of a compound of formula (Ia) or (Ib) for the manufacture of a medicament for the treatment of latent tuberculosis, wherein the compound of formula (Ia) or (Ib) is a pharmaceutically acceptable salt, a quaternary amine, a N-oxide, a tautomeric form or a stereochemically isomeric form 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, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula (II); R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is zero, 1, 2,3 or 4; R4 and R5 each independently

are hydrogen, alkyl or benzyl; or R4 and R5 may be taken together including the N to which they are attached; R6 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl ; or two vicinal R6 radicals may be taken together to form a bivalent radical -CH=CH-CH=CH-; r is 1, 2, 3, 4 or 5; R7 is hydrogen, alkyl, Ar or Het; R8 is hydrogen or alkyl; R9 is oxo; or R8 and R9 together form the radical

(56)    Documents Cited :    WO 03/0725553 A    WO 04/011436 A    NUERMBERGER ERIC ET AL Vol. 25 No.3,June 2004


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