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    Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor
    1.
    发明授权
    Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor 失效
    醌基丙基哌啶衍生物，含有它们的中间体和组合物及其制备方法

    公开(公告)号：US06841562B2

    公开(公告)日：2005-01-11

    申请号：US10659095

    申请日：2003-09-10

    申请人： Eric Bacqué ,  Antony Bigot ,  Youssef El Ahmad ,  Jean-Luc Malleron ,  Serge Mignani ,  Baptiste Ronan ,  Michel Tabart ,  Fabrice Viviani

    发明人： Eric Bacqué ,  Antony Bigot ,  Youssef El Ahmad ,  Jean-Luc Malleron ,  Serge Mignani ,  Baptiste Ronan ,  Michel Tabart ,  Fabrice Viviani

    IPC分类号： A61P31/04 ,  C07D211/60 ,  C07D401/06 ,  C07D409/14 ,  A61K31/44 ,  C07D215/12 ,  C07D215/18

    CPC分类号： C07D401/06 ,  C07D211/60 ,  C07D409/14 ,  Y02P20/55

    摘要： Quinolylpropylpiperidine derivatives of general formula (I) in which R1a is hydrogen, halogen, hydroxyl, amino, alkylamino, dialkylamino, hydroxyamino, alkoxyamino or alkylalkoxyamino and R1b is hydrogen, or R1a and R1b form an oxo, R2 is carboxyl, carboxymethyl or hydroxymethyl, R3 is alkyl either substituted with phenylthio optionally substituted with halogen, hydroxyl, alkyl, alkoxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkoxycarbonyl, cyano or amino, or with cycloalkylthio (3 to 7 members) optionally substituted with halogen or trifluoromethyl, or with heteroarylthio (5 to 6 members and 1 to 4 heteroatoms chosen from N, O and S), optionally substituted with halogen, hydroxyl, alkyl, alkoxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkoxycarbonyl, cyano or amino or R3 is propargyl substituted with phenyl or heteroaryl as defined above, R4 is alkyl, alkenyl-CH2— or alkynyl-CH2—, cycloalkyl or cycloalkylalkyl, in their various isomeric forms, separate or as mixtures, and also their salts, their preparation process and intermediates and the compositions containing them. These novel derivatives are potent antibacterial agents.

    摘要翻译： 通式（I）的喹啉基丙基哌啶衍生物，其中R 1a是氢，卤素，羟基，氨基，烷基氨基，二烷基氨基，羟基氨基，烷氧基氨基或烷基烷氧基氨基，R 1b是氢，或者R 1a和R 1b形成氧代，R 2是羧基，羧甲基或羟甲基， 羟基，烷基，烷氧基，三氟甲基，三氟甲氧基，羧基，烷氧基羰基，氰基或氨基，或与任选被卤素或三氟甲基取代的环烷硫基（3至7个成员）或与杂芳硫基（ 羟基，烷基，烷氧基，三氟甲基，三氟甲氧基，羧基，烷氧基羰基，氰基或氨基或R3是被苯基或杂芳基取代的炔丙基，被苯基或杂芳基取代 R4是烷基，烯基-CH 2 - 或炔基-CH 2 - ，环烷基或环烷基烷基，其各种异构体形式，分别或混合物，和 它们的盐，它们的制备方法和中间体以及含有它们的组合物。 这些新型衍生物是有效的抗菌剂。

    Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor
    2.
    发明授权
    Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor 失效
    醌基丙基哌啶衍生物，含有它们的中间体和组合物及其制备方法

    公开(公告)号：US07232834B2

    公开(公告)日：2007-06-19

    申请号：US10659164

    申请日：2003-09-10

    申请人： Eric Bacque ,  Antony Bigot ,  Youssef El Ahmad ,  Jean-Luc Malleron ,  Serge Mignani ,  Baptiste Ronan ,  Michel Tabart ,  Fabrice Viviani

    发明人： Eric Bacque ,  Antony Bigot ,  Youssef El Ahmad ,  Jean-Luc Malleron ,  Serge Mignani ,  Baptiste Ronan ,  Michel Tabart ,  Fabrice Viviani

    IPC分类号： A61K31/4545 ,  C07D401/06

    CPC分类号： C07D401/06 ,  C07D211/34 ,  C07D409/14 ,  Y02P20/55

    摘要： Quinolylpropylpiperidine derivatives of general formula (I) in which R1 is hydrogen or fluorine, R2 is carboxyl, carboxymethyl or hydroxymethyl, R3 is alkyl substituted either with phenylthio optionally substituted with halogen, hydroxyl, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkyloxycarbonyl, cyano or amino, or with cycloalkylthio (3 to 7 members) optionally substituted with halogen or trifluoromethyl, or with heteroarylthio (5 to 6 members and 1 to 4 heteroatoms chosen from N, O and S), optionally substituted with halogen, hydroxyl, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkyloxycarbonyl, cyano or amino or R3 is propargyl substituted by phenyl or heteroaryl as defined above and R4 is alkyl, alkenyl-CH2— or alkynyl-CH2—, cycloalkyl or cycloalkylalkyl, in their various isomeric forms, separate or as mixtures, and also their salts, their preparation process and intermediates and the compositions containing them. These novel derivatives are potent antibacterial agents

    摘要翻译： R 1是氢或氟的通式（I）的喹啉基丙基哌啶衍生物，R 2是羧基，羧甲基或羟甲基，R 3是 被任选被卤素，羟基，烷基，烷氧基，三氟甲基，三氟甲氧基，羧基，烷氧基羰基，氰基或氨基取代的苯硫基取代或被任选被卤素或三氟甲基取代的环烷硫基（3至7成员）或与杂芳硫基 6个成员和1至4个选自N，O和S的杂原子），任选被卤素，羟基，烷基，烷氧基，三氟甲基，三氟甲氧基，羧基，烷氧基羰基，氰基或氨基取代的杂原子，或者R 3是炔丙基 被如上定义的苯基或杂芳基取代，并且R 4是烷基，链烯基-CH 2 - 或炔基-CH 2 - ，环烷基或环烷基烷基 以其各种异构体形式，分别或作为混合物，以及它们的盐，其制备方法和含量 ermediates和含有它们的组合物。 这些新型衍生物是有效的抗菌剂

    Quinolylpropylpiperidine derivatives, preparation process and intermediates, and compositions including them
    9.
    发明授权
    Quinolylpropylpiperidine derivatives, preparation process and intermediates, and compositions including them 失效
    醌基丙基哌啶衍生物，制备方法和中间体，以及包括它们的组合物

    公开(公告)号：US06806277B2

    公开(公告)日：2004-10-19

    申请号：US10622655

    申请日：2003-07-18

    申请人： Eric Bacqué ,  Jean-Luc Malleron ,  Serge Mignani ,  Michel Tabart

    发明人： Eric Bacqué ,  Jean-Luc Malleron ,  Serge Mignani ,  Michel Tabart

    IPC分类号： A61K3147

    CPC分类号： C07D401/06 ,  C07D409/12

    摘要： Quinolylpropylpiperidine derivatives of general formula (I) in which: R1 is NH2, alkylamino, dialkylamino, hydroxyamino, alkyl(alkyloxy)amino or alkyloxyamino, R2 is a carboxyl, carboxymethyl or hydroxymethyl radical, R3 is alkyl (1 to 6C) substituted by phenylthio which can itself carry 1 to 3 substituents selected from halogen, OH, alkyl, alkyloxy, CF3, OCF3, COOH, alkyloxycarbonyl, CN and NH2, by cycloalkylthio (3 to 7 members) or by heteroarylthio (5 to 6 members) comprising 1 to 4 heteroatoms selected from N, S and O and optionally itself substituted [by halogen, OH, alkyl, alkyloxy, CF3, OCF3, ═O, COOH, alkyloxycarbonyl, CN or NH2] or R3 is propargyl substituted by phenyl which can itself carry 1 to 3 substituents selected from halogen, OH, alkyl, alkyloxy, CF3, OCF3, COOH, alkyloxycarbonyl, CN and NH2 or substituted by cycloalkyl comprising 3 to 7 members or substituted by 5- to 6-membered heteroaryl comprising 1 to 4 heteroatoms chosen from N, O or S and optionally itself substituted by halogen, OH, alkyl, alkyloxy, CF3, OCF3, ═O, COOH, alkyloxycarbonyl, CN or NH2, and R4 is alkyl (1 to 6C), alkenyl-CH2—, alkynyl-CH2— (3 to 7C), cycloalkyl or (cycloalkyl)alkyl, in their diastereoisomeric forms or their mixtures, and their pharmaceutically acceptable salts. These novel derivatives are particularly advantageous antimicrobial agents.

    摘要翻译： 通式（I）的喹啉基丙基哌啶衍生物，其中：R1是NH2，烷基氨基，二烷基氨基，羟基氨基，烷基（烷氧基）氨基或烷氧基氨基，R2是羧基，羧甲基或羟甲基，R3是被苯硫基取代的（1-6） 其可以自身携带1至3个选自卤素，OH，烷基，烷氧基，CF 3，OCF 3，COOH，烷氧基羰基，CN和NH 2的取代基，被环烷硫基（3至7个成员）或通过杂芳硫基（5至6个成员）包含1至 4个选自N，S和O的杂原子，并且任选地本身被[由卤素，OH，烷基，烷氧基，CF 3，OCF 3，= O，COOH，烷氧基羰基，CN或NH 2]取代的R 3或被苯基取代的苯基， 被选自卤素，OH，烷基，烷氧基，CF 3，OCF 3，COOH，烷氧基羰基，CN和NH 2的3个取代基，或被包含3至7个成员的环烷基或被包含1至4个选自 N，O或S，以及任选的其自身取代基 CN，NH 2，R 4是烷基（1-6），链烯基-CH 2 - ，炔基-CH 2 - （3至7C），环烷基（C 1 -C 6）烷基，烷氧基羰基， 或（环烷基）烷基，其非对映异构体形式或其混合物及其药学上可接受的盐。这些新型衍生物是特别有利的抗微生物剂。