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    • 8. 发明申请
    • Quinoline Derivatives as Antibacterial Agents
    • 喹啉衍生物作为抗菌剂
    • US20100197727A1
    • 2010-08-05
    • US11917091
    • 2006-06-26
    • Koenraad Jozef Lodewijk Marcel AndriesAnil KoulDavid Francis Alain LancoisMagali Madeleine Simone MotteJérôme Emile Georges Guillemont
    • Koenraad Jozef Lodewijk Marcel AndriesAnil KoulDavid Francis Alain LancoisMagali Madeleine Simone MotteJérôme Emile Georges Guillemont
    • A61K31/47C07D215/227C07D409/06A61K31/4709C07D401/06C07D215/36A61P31/04
    • C07D409/06A61K31/47A61K31/4709C07D215/227C07D215/36C07D401/06
    • 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 (Ia) or (Ib) a N-oxide, a tautomeric form or a stereochemically isomeric form thereof wherein A− is a counter ion; R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1 to 4; R2 is hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or wherein Y is CH2, O, S, NH or N-alkyl; R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is 0 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 —CH═CH—CH═CH—; r is 1 to 5; R7 is hydrogen, alkyl, Ar or Het; R8 is hydrogen or alkyl; R9 is oxo; or R8 and R9 taken together form —CH═CH—N═; R10 is alkyl, alkylcarbonyl, Ar, Ar-alkyl, Ar-carbonyl, Het1-alkyl or Het1-carbonyl.
    • 使用化合物制造用于治疗细菌感染的药物,只要细菌感染不是分枝杆菌感染,所述化合物是式(Ia)或(Ib)的化合物,N-氧化物,互变异构体 形式或其立体化学异构体形式,其中A-是抗衡离子; R 1是氢,卤素,卤代烷基,氰基,羟基,Ar,Het,烷基,烷氧基,烷硫基,烷氧基烷基,烷硫基烷基,芳烷基或二(Ar) p为1〜4; R2是氢,羟基,巯基,烷氧基,烷氧基烷氧基,烷硫基,一或二(烷基)氨基或其中Y是CH2,O,S,NH或N-烷基; R3是烷基,Ar,Ar-烷基,Het或Het-烷基; q为0〜4; R4和R5各自独立地为氢,烷基或苄基; 或R4和R5可以一起包括它们所连接的N; R 6是氢,卤素,卤代烷基,羟基,Ar,烷基,烷氧基,烷硫基,烷氧基烷基,烷硫基烷基,芳烷基或二(Ar) 或两个连位的R6基团可以一起形成-CH = CH-CH = CH-; r为1〜5; R7是氢,烷​​基,Ar或Het; R8是氢或烷基; R9是氧代; 或R8和R9一起形成-CH = CH-N =; R10是烷基,烷基羰基,Ar,Ar-烷基,Ar-羰基,Het1-烷基或Het1-羰基。