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(11)    Patent No :    AP 2383    (73) Applicant(s)       
(21)    Application No :    AP/P/2007/004264    JANSSEN PHARMACEUTICA N.V., Turnhoutseweg 30,       
            B-2340 Beerse,       
(22)    Filing Date :    06.06.2006    Belgium       
(24)    Date of Grant &    16.03.2012           
(45)    Publication :

(30)  Priority Data    (72) Inventors

    (33) Country    (31) Number    (32) Date    ANDRIES Koenraad Jozef Lodewijk Marcel, Belgium   
    EP            05105023.5    08.06.2005    KOUL Anil, Belgium   
    US            11/296,918        08.12.2005       
                            GUILLEMONT Jérôme Emile Georges, France   
                                et al       
                                (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)    A61P 31/04 (2006.01)   
                            A61K 31/4709 (2006.01)    C07D 215/22 (2006.01)   
                            C07D 215/36 (2006.01)    C07D 401/04 (2006.01)   
                            C07D 405/04 (2006.01)    C07D 401/06 (2006.01)
(54)    Title

Quinoline derivatives as antibacterial agents

(57)    Abstract

The present invention relates to the use of a compound for the manufacture of a medicament for the treatment of a bacterial infection, said compound being a compound of formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof or a N-oxide form thereof, wherein R1 is hydrogen, halo, polyhaloC1 -6alkyl, C1-6alkyl, hydroxyC1 -6alkyl, C1-6alkyloxy, Ar or Het; p is an integer equal to 1 or 2; R is C1-6alkyloxy, C1-6alkyloxyC1 -6alkyloxy or C1-6alkylt hio : R3 is C1-6alkyl, Ar, Het or Hetl; R4 and R5 each independently are hydrogen, C1 -6alkyl or benzyl;

or R4 and R5 together and including the N to which they are attached may form a radical selected from the group of pyrrolidinyl, 2 -pyrrolinyl,

3-pyrrolinyl, pyrrolyl, imidazolidinyl, pyrazolidinyl, 2-imidazolinyl,


imidazolyl, pyrazolyl, triazolyl, piperidinyl, pyridinyl, piperazinyl, pyridazinyl, pyrimidinyl, pyrazinyl, triazinyl, morpholinyl and thiomorpholinyl, each of said rings may optionally be substituted with Cl-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, hydroxyC1 -6alkyl, C1-6alkyloxy, amino, mono - or di(C1-6alkyl)amino, C1-6alkylt hio, C1 -6alkyloxyC1-6alkyl, C1-6alkylt hioC1-6alkyl or pyrimidinyl; R6 is hydrogen, halo, polyhaloC1 -6alkyl,

C1-6alkyl, C1 -6alkylo xy, C1-6alkylt hio ; or two vicinal R6 radicals may be taken together to form a bivalent radical of formula -CH=CH-CH=CH- ; r is an

(56)    Documents Cited :    WO 2004/011436 A    J. SCIENCE, VOL. 307    WO 1995/06047 A    WO 2005/117875 A


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