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    Quinoline derivatives as antibacterial agents
    7.
    发明授权
    Quinoline derivatives as antibacterial agents 有权
    喹啉衍生物作为抗菌剂

    公开(公告)号：US08802671B2

    公开(公告)日：2014-08-12

    申请号：US11997173

    申请日：2006-07-31

    申请人： Jérôme Emile Georges Guillemont ,  Elisabeth Thérèse Jeanne Pasquier ,  David Francis Alain Lançois ,  Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul ,  Leo Jacobus Jozef Backx ,  Lieven Meerpoel

    发明人： Jérôme Emile Georges Guillemont ,  Elisabeth Thérèse Jeanne Pasquier ,  David Francis Alain Lançois ,  Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul ,  Leo Jacobus Jozef Backx ,  Lieven Meerpoel

    IPC分类号： A61K31/535

    CPC分类号： C07D215/227 ,  A61K31/47

    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 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.

    摘要翻译： 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。

    Quinoline derivatives as antibacterial agents
    8.
    发明授权
    Quinoline derivatives as antibacterial agents 有权
    喹啉衍生物作为抗菌剂

    公开(公告)号：US08691800B2

    公开(公告)日：2014-04-08

    申请号：US11997015

    申请日：2006-07-31

    申请人： Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul ,  Jérôme Emile Georges Guillemont ,  Elisabeth Thérèse Jeanne Pasquier

    发明人： Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul ,  Jérôme Emile Georges Guillemont ,  Elisabeth Thérèse Jeanne Pasquier

    IPC分类号： A61K31/33

    CPC分类号： C07D413/06 ,  A61K31/4709 ,  C07D413/14 ,  Y02A50/473

    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 (Ia) or (Ib) a pharmaceutically acceptable acid or base addition salt thereof, a quaternary amine thereof, a stereochemically isomeric form thereof, a tautomeric form thereof 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, 2, 3 or 4; R2 is hydrogen, hydroxy, thio, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; R4 is hydrogen, alkyl or benzyl; R5 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R5 radicals may be taken together to form together with the phenyl ring to which they are attached a naphthyl; r is 1, 2, 3, 4 or 5; R6 is hydrogen, alkyl, Ar or Het; R7 is hydrogen or alkyl; R5 is oxo; or R7 and R5 together form the radical —CH═CH—N═; Z is CH2 or C(═O).

    摘要翻译： 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，其药学上可接受的酸或碱加成 其盐，其季胺，其立体化学异构形式，其互变异构形式或其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，芳烷基或二（Ar）烷基; p为1,2,3或4; R 2是氢，羟基，硫代，烷氧基，烷氧基烷氧基，烷硫基，一或二（烷基）氨基或式R3基团是烷基，Ar，Ar-烷基，Het或Het-烷基; R4是氢，烷基或苄基; R5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R5基团可以与它们所连接的苯环一起形成萘基; r为1,2,3,4或5; R6是氢，烷基，Ar或Het; R7是氢或烷基; R5是氧代; 或R7和R5一起形成基团-CH = CH-N =; Z是CH 2或C（= O）。