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    • 4. 发明授权
    • Quinoline derivatives as antibacterial agents
    • 喹啉衍生物作为抗菌剂
    • US08802671B2
    • 2014-08-12
    • US11997173
    • 2006-07-31
    • Jérôme Emile Georges GuillemontElisabeth Thérèse Jeanne PasquierDavid Francis Alain LançoisKoenraad Jozef Lodewijk Marcel AndriesAnil KoulLeo Jacobus Jozef BackxLieven Meerpoel
    • Jérôme Emile Georges GuillemontElisabeth Thérèse Jeanne PasquierDavid Francis Alain LançoisKoenraad Jozef Lodewijk Marcel AndriesAnil KoulLeo Jacobus Jozef BackxLieven Meerpoel
    • A61K31/535
    • C07D215/227A61K31/47
    • 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 0 to 4; R2 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 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 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 then s is 1 to 4.
    • 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(I)化合物,其药学上可接受的酸或碱加成盐,季铵盐 胺,立体化学异构形式,互变异构形式或其N-氧化物形式,其中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, (Ar)烷基; p为1〜3; s为0〜4; R2是氢; 光环; 烷基; 羟基; 巯基 任选取代的烷氧基; 烷氧基烷氧基; 烷硫基; 单或二(烷基)氨基,其中烷基可任选被取代; Ar; Het或式R3的基团是烷基,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基团可以与它们所连接的苯环一起形成萘基; r为1〜5; R7是氢,烷​​基,Ar或Het; R8是氢,烷基,羟基,氨基羰基,单或二(烷基)氨基羰基,Ar,Het,被一个或两个Het取代的烷基,被一个或两个Ar,Het-C(= O) - 或Ar- C(= O) - ; 条件是当将带有R3的自由基置于喹啉部分的位置3时; R7位于4位,R2位于2位,代表氢,羟基,巯基,烷氧基,烷氧基烷氧基,烷硫基,单或二(烷基)氨基或式基团,其中s为1至4。