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(11)    Patent No :    AP 2654   
(21)    Application No :    AP/P/2008/004316   
(22)    Filing Date :    31.07.2006   
(24)    Date of Grant &    25.04.2013   
           
(45)    Publication :

(30)  Priority Data       
(33) Country    (31) Number    (32) Date
EP    05107164.5    03.08.2005
(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 Jérôme Emile Georges, France

PASQUIER Elisabeth Thérèse Jeanne, France

LANÇOIS David Francis Alain, France

et al

(74) Representative

HONEY & BLANCKENBERG
 

(51)  International  Classification   A61K 31/47 (2006.01)    A61P 31/04 (2006.01)
C07D 215/18 (2006.01)   


(54)    Title

Quinoline derivatives as antibacterial agents

(57)    Abstract
Use of a compound for the manufacture of a medicament for the treatment of

a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (I), a pharmaceutically acceptable acid or base addition salt, a quaternary amine, a stereochemically isomeric form, a tautomeric form or a N-oxide 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 to 3; s is O to 4; R is hydrogen; halo; alkyl; hydroxy; mercapto; optionally substituted alkyloxy; alkyloxyalkyloxy; alkylthio; mono or di(alkyl)amino wherein alkyl may optionally be substituted; Ar; Het or a radical of formula (II), R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is O to 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 together with the phenyl ring to which they are attached a naphthyl; r is 1 to 5 ; R7 is hydrogen, alkyl, Ar or Het ; R8 is hydrogen, alkyl, hydroxyl, aminocarbonyl, mono-or di(alkyl)aminocarbonyl, Ar, Het, alkyl substituted with one or two Het, alkyl substituted with one or two Ar, Het -C(=O)- or Ar-C(=O)-; provided that when the R3 bearing radical is placed in position 3 of the quinoline moiety; R7 is placed in position 4 and R2 is placed in position 2 and represents hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula (111), then s is 1 to

(56)    Documents Cited :    WO 2004/011436 A    ANDRIES K et al:    WO 95/06047 A    WO 2005/075428 A    GB 807

750

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