发明名称 QUINOLINE DERIVATIVES AS ANTIBACTERIAL AGENTS
摘要 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 2 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 ; R 7 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 (III), then s is 1 to 4.
申请公布号 KR20080035666(A) 申请公布日期 2008.04.23
申请号 KR20087005071 申请日期 2006.07.31
申请人 JANSSEN PHARMACEUTICA N. V 发明人 GUILLEMONT JEROME EMILE GEORGES;PASQUIER ELISABETH THERESE JEANNE;LANCOIS DAVID FRANCIS ALAIN;ANDRIES KOENRAAD JOZEF LODEWIJK MARCEL;KOUL ANIL;BACKX LEO JACOBUS JOZEF;MEERPOEL LIEVEN
分类号 C07D215/22;A61K31/47;A61P31/04;C07D215/18 主分类号 C07D215/22
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