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    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：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
    3.
    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

    4-substituted quinoline derivatives, method and intermediates for their preparation and pharmaceutical compositions containing them
    4.
    发明授权
    4-substituted quinoline derivatives, method and intermediates for their preparation and pharmaceutical compositions containing them 失效
    4-取代喹啉衍生物，其制备方法和中间体以及含有它们的药物组合物

    公开(公告)号：US07348434B2

    公开(公告)日：2008-03-25

    申请号：US10913222

    申请日：2004-08-06

    申请人： Antony Bigot ,  Serge Mignani ,  Baptiste Ronan ,  Michel Tabart ,  Fabrice Viviani

    发明人： Antony Bigot ,  Serge Mignani ,  Baptiste Ronan ,  Michel Tabart ,  Fabrice Viviani

    IPC分类号： C07D215/38

    CPC分类号： C04B35/632 ,  C07D401/12

    摘要： The invention relates to 4-substituted quinoline derivatives of general formula: which are active as antimicrobials, in which: X1, X2, X3, X4 and X5 represent >C—R′1 to >C—R′5 respectively, or alternatively at most one represents nitrogen, Y represents CHR, CO, CROH, CRNH2, CRF or CF2, R being a hydrogen or alkyl, m is 0, 1 or 2 and n is 0 or 1, R2 represents a radical R, —CO2R, —CH2CO2R, —CH2—CH2CO2R, —CONH2, —CH2—CONH2, —CH2—CH2—CONH2, —CH2OH, —CH2—CH2OH, —CH2—NH2—CH2—CH2—NH2 or —CH2—CH2—CH2—NH2, R being as defined above, R3 represents phenyl, heteroaryl or alk-Ro3, where alk is alkyl and Ro3 represents various groups, where appropriate containing oxygen, sulfur or amine, in their enantiomeric or diastereoisomeric forms or their mixtures, and/or where appropriate in the syn or anti form or their mixtures, and their salts.

    摘要翻译： 本发明涉及以下通式的4-取代喹啉衍生物：其作为抗微生物剂是有活性的，其中：X 1，X 2，X 3 ，X 4和X 5分别表示C-R 1至C-R'5 R 2如上所定义，R 3表示苯基，杂芳基或烷基-R（R 2） 其中烷基是烷基 和R 3表示各种基团，其中适当地含有它们的对映异构体或非对映异构形式或其混合物中的氧，硫或胺，和/或在合适的情况下在顺式或顺式 抗体形式或它们的混合物及其盐。

    4-Substituted quinoline derivatives, method and intermediates for their preparation and pharmaceutical compositions containing them
    5.
    发明申请
    4-Substituted quinoline derivatives, method and intermediates for their preparation and pharmaceutical compositions containing them 失效
    4-取代的喹啉衍生物，其制备方法和中间体以及含有它们的药物组合物

    公开(公告)号：US20050032800A1

    公开(公告)日：2005-02-10

    申请号：US10913222

    申请日：2004-08-06

    申请人： Antony Bigot ,  Serge Mignani ,  Baptiste Ronan ,  Michel Tabart ,  Fabrice Viviani

    发明人： Antony Bigot ,  Serge Mignani ,  Baptiste Ronan ,  Michel Tabart ,  Fabrice Viviani

    IPC分类号： C07D401/12 ,  C07D487/02 ,  C07D41/02

    CPC分类号： C04B35/632 ,  C07D401/12

    摘要： The invention relates to 4-substituted quinoline derivatives of general formula: which are active as antimicrobials, in which: X1, X2, X3, X4 and X5 represent >C—R′1 to >C—R′5 respectively, or alternatively at most one represents nitrogen, Y represents CHR, CO, CROH, CRNH2, CRF or CF2, R being a hydrogen or alkyl, m is 0, 1 or 2 and n is 0 or 1, R2 represents a radical R, —CO2R, —CH2CO2R, —CH2—CH2CO2R, —CONH2, —CH2—CONH2, —CH2—CH2—CONH2, —CH2OH, —CH2—CH2OH, —CH2—NH2—CH2—CH2—NH2 or —CH2—CH2—CH2—NH2, R being as defined above, R3 represents phenyl, heteroaryl or alk-R°3, where alk is alkyl and R°3 represents various groups, where appropriate containing oxygen, sulfur or amine, in their enantiomeric or diastereoisomeric forms or their mixtures, and/or where appropriate in the syn or anti form or their mixtures, and their salts.

    摘要翻译： 本发明涉及以下通式的4-取代喹啉衍生物：其作为抗微生物剂具有活性，其中：X 1，X 2，X 3，X 4和X 5分别表示> C-R'1至> C-R'5，或者替代地 大多数代表氮，Y代表CHR，CO，CROH，CRNH2，CRF或CF2，R是氢或烷基，m是0,1或2，n是0或1，R2代表基团R，-CO 2 R， CH2CO2R，-CH2-CH2CO2R，-CONH2，-CH2-CONH2，-CH2-CH2-CONH2，-CH2OH，-CH2-CH2OH，-CH2-NH2-CH2-CH2-NH2或-CH2-CH2-CH2-NH2， R如上定义，R 3表示苯基，杂芳基或烷基-R 3，其中alk是烷基，R 3表示各种基团，其中适当地含有其对映体或非对映异构体形式的氧，硫或胺，或其混合物，以及 /或适当时以合成或反式形式或其混合物及其盐。