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1. 发明授权

US06841562B2 Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor 失效
标题翻译：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。

2. 发明授权

US07232834B2 Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor 失效
标题翻译：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

3. 发明授权

US07232833B2 4-substituted quinoline derivatives, method and intermediates for their preparation and pharmaceutical compositions containing them 失效
标题翻译： 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：US07232833B2
公开(公告)日：2007-06-19
申请号：US10810711
申请日：2004-03-26
申请人： Antony Bigot , Youssef El-Ahmad , Jean-Luc Malleron , Jean-Paul Martin , Serge Mignani , Guy Pantel , Baptiste Ronan , Michel Tabart , Michel Cheve , Fabrice Viviani
发明人： Antony Bigot , Youssef El-Ahmad , Jean-Luc Malleron , Jean-Paul Martin , Serge Mignani , Guy Pantel , Baptiste Ronan , Michel Tabart , Michel Cheve , Fabrice Viviani
IPC分类号： A61K31/47 , A61K31/517 , A61K31/44 , A61K31/50 , A61K31/54
CPC分类号： C07D401/06 , C07D409/14 , C07D413/06
摘要： The invention relates to 4-substituted quinoline compounds of general formula: which are active as antimicrobials, in which: X1, X2, X3, X4 and X5 is C—R′1, to C—R′5 respectively, or alternatively at most one represents N, Y represents CHR, CO, CROH, CRNH2, CRF or CF2, R being a hydrogen or alkyl, m is 1, 2 or 3 and n is 0, 1 or 2, Z is CH2 or Z is O, S, SO, SO2 and, in this case, n is equal to 2, R2 is —CO2R, —CH2CO2R, —CH2—CH2CO2R, —CH2OH or —CH2—CH2OH, wherein R is 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-取代喹啉化合物：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分别为C-R'1，C-R'5，或者至多一个表示N，Y表示CHR，CO，CROH，CRNH 2，CRF或CF 2，R为氢或烷基，m为1,2 或3，n为0,1或2，Z为CH 2或Z为O，S，SO，SO 2，在这种情况下，n等于 2，R 2是-CO 2 R，-CH 2 CO 2 R，-CH 2， 2个-CH 2 CO 2 R 2，-CH 2 OH或-CH 2 -CH（CH 2） R 2 OH，其中R如上所定义，R 3表示苯基，杂芳基或烷基-SO 3 - ， - 其中烷基是烷基，R 3 O 3表示各种基团，其中适当地含有它们的对映体或非对映异构形式或其混合物中的氧，硫或胺， d /或适当时以合成或反式形式或其混合物及其盐。

4. 发明授权

US06903217B2 Heterocyclylalkylpiperidine derivatives, their preparation and compositions containing them 失效
标题翻译：杂环基烷基哌啶衍生物，它们的制备方法和含有它们的组合物
公开(公告)号：US06903217B2
公开(公告)日：2005-06-07
申请号：US10607220
申请日：2003-06-27
申请人： Eric Bacqué , Jean-Christophe Carry , Youssef El-Ahmad , Michel Evers , Philippe Hubert , Jean-Luc Malleron , Serge Mignani , Guy Pantel , Michel Tabart , Fabrice Viviani
发明人： Eric Bacqué , Jean-Christophe Carry , Youssef El-Ahmad , Michel Evers , Philippe Hubert , Jean-Luc Malleron , Serge Mignani , Guy Pantel , Michel Tabart , Fabrice Viviani
IPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D417/14 , C07D471/02 , C07D215/18 , C07D237/26
CPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D417/14
摘要： Heterocyclylalkylpiperidine derivatives of general formula (I) in their enantiomeric or diastereoisomeric forms or mixtures of these forms, and/or, where appropriate, in their syn or anti form or a mixture thereof, as well as any salt thereof.
摘要翻译：通式（I）的杂环基烷基哌啶衍生物在它们的对映体或非对映异构体形式或这些形式的混合物中，和/或在适当的情况下以其顺式或反式或其混合物以及其任何盐。

5. 发明授权

US06602884B2 Quinolylpropylpiperidine derivatives, their preparation, and compositions containing them 失效
公开(公告)号：US06602884B2
公开(公告)日：2003-08-05
申请号：US10096482
申请日：2002-03-13
申请人： Eric Bacqué , Serge Mignani , Jean-Luc Malleron , Michel Tabart , Michel Evers , Fabrice Viviani , Youssef El Ahmad , Stéphane Mutti , Christophe Daubié
发明人： Eric Bacqué , Serge Mignani , Jean-Luc Malleron , Michel Tabart , Michel Evers , Fabrice Viviani , Youssef El Ahmad , Stéphane Mutti , Christophe Daubié
IPC分类号： A01N4342
CPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D417/14
摘要： Quinolylpropylpiperidine derivatives of general formula (I) are described, and are useful as antimicrobial agents. Their preparation is also described.

6. 发明授权

US06603005B2 Heterocyclylalkylpiperidine derivatives, their preparation and compositions containing them 失效
标题翻译：杂环基烷基哌啶衍生物，它们的制备方法和含有它们的组合物
公开(公告)号：US06603005B2
公开(公告)日：2003-08-05
申请号：US09987386
申请日：2001-11-14
申请人： Eric Baque , Jean-Christophe Carry , Youssef El-Ahmad , Michel Evers , Philippe Hubert , Jean-Luc Malleron , Serge Mignani , Guy Pantel , Michel Tabart , Fabrice Viviani
发明人： Eric Baque , Jean-Christophe Carry , Youssef El-Ahmad , Michel Evers , Philippe Hubert , Jean-Luc Malleron , Serge Mignani , Guy Pantel , Michel Tabart , Fabrice Viviani
IPC分类号： C07D47102
CPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D417/14
摘要： Heterocyclylalkylpiperidine derivatives of general formula (I) in their enantiomeric or diastereoisomeric forms or mixtures of these forms, and/or, where appropriate, in their syn or anti form or a mixture thereof, as well as any salt thereof.
摘要翻译：通式（I）的杂环基烷基哌啶衍生物在它们的对映异构体或非对映异构体形式或这些形式的混合物中，和/或在适当时以其顺式或反式或其混合物以及其任何盐。

7. 发明授权

US06403610B1 Quinolylpropylpiperidine derivatives, their preparation and the compositions which comprise them 失效
标题翻译：醌基丙基哌啶衍生物，它们的制备方法和包含它们的组合物
公开(公告)号：US06403610B1
公开(公告)日：2002-06-11
申请号：US09664959
申请日：2000-09-18
申请人： Jean-Luc Malleron , Michel Tabart , Jean-Christophe Carry , Michel Evers , Youssef El Ahmad , Serge Mignani , Fabrice Viviani , Michel Cheve
发明人： Jean-Luc Malleron , Michel Tabart , Jean-Christophe Carry , Michel Evers , Youssef El Ahmad , Serge Mignani , Fabrice Viviani , Michel Cheve
IPC分类号： A61K3147
CPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D417/14
摘要： Quinolylpropylpiperidine derivatives of formula (I) which are particularly advantageous antimicrobial agents, their compositions, and their use.
摘要翻译：式（I）的喹啉基丙基哌啶衍生物，其是特别有利的抗微生物剂，它们的组成及其用途。

8. 发明授权

US06815547B2 Quinolylpropylpiperidine derivatives, their preparation, and compositions containing them 失效
标题翻译：醌基丙基哌啶衍生物，它们的制备和含有它们的组合物
公开(公告)号：US06815547B2
公开(公告)日：2004-11-09
申请号：US10387479
申请日：2003-03-14
申请人： Eric Bacque , Serge Mignani , Jean-Luc Malleron , Michel Tabart , Michel Evers , Fabrice Viviani , Youssef El Ahmad , Stéphane Mutti , Christophe Daubié
发明人： Eric Bacque , Serge Mignani , Jean-Luc Malleron , Michel Tabart , Michel Evers , Fabrice Viviani , Youssef El Ahmad , Stéphane Mutti , Christophe Daubié
IPC分类号： C07D21512
CPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D417/14
摘要： Quinolylpropylpiperidine derivatives of general formula (I) are described, and are useful as antimicrobial agents. Their preparation is also described.
摘要翻译：描述了通式（I）的喹啉基丙基哌啶衍生物，并且可用作抗微生物剂。还描述了它们的制备方法。

9. 发明授权

US06806277B2 Quinolylpropylpiperidine derivatives, preparation process and intermediates, and compositions including them 失效
标题翻译：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。

10. 发明授权

US07524838B2 Pyrazolyl derivatives, preparation process and intermediates of this process as medicinal products and pharmaceutical compositions containing them 失效
标题翻译：吡唑基衍生物，该方法的制备方法和中间体作为药物产品和含有它们的药物组合物
公开(公告)号：US07524838B2
公开(公告)日：2009-04-28
申请号：US10997736
申请日：2004-11-24
申请人： Arielle Genevois-Borella , Jean-Luc Malleron , Jean Bouquerel , Gilles Doerflinger , Andrees Bohme , Gaetan Touyer , Jean-Francois Sabuco , Corrine Terrier , Serge Mignani , Michel Evers , Youssef El-Ahmad
发明人： Arielle Genevois-Borella , Jean-Luc Malleron , Jean Bouquerel , Gilles Doerflinger , Andrees Bohme , Gaetan Touyer , Jean-Francois Sabuco , Corrine Terrier , Serge Mignani , Michel Evers , Youssef El-Ahmad
IPC分类号： A61K31/55 , A61K31/5377 , A61K31/454 , A61K31/4152 , A61K31/4155 , C07D403/06 , C07D231/18 , C07D401/06 , C07D453/02
CPC分类号： C07D231/12 , C07D231/14 , C07D231/20 , C07D401/04 , C07D401/06 , C07D403/06 , C07D409/04 , C07D453/02 , C07D453/06 , C07D487/08
摘要： The present invention relates to the novel derivatives of formula (I) in which A is, if it is present, a (C1-C6) alkyl, a (C3-C6) alkenyl, a (C3-C6) alkynyl, a (C3-C7) cycloalkyl or a (C5-C7) cycloalkenyl, R1 is an NR6R7, (C4-C7) azacycloalkyl, (C5-C7) azacycloalkenyl, (C5-C9) azabicycloalkyl or (C5-C9) azabicycloalkenyl group; A-R1 is such that the nitrogen of R1 and the nitrogen in the 1-position of the pyrazole are necessarily separated by at least two carbon atoms, R3 is an H, halogen, OH, SH, NH2, ORc, SRc, SORa, SO2Ra, NHCHO, NRaRb, NHC(O)Ra, NHC(S)Ra or NHSO2Ra, R4 is an aryl or heteroaryl; and R5 is an H, halogen, CF3, CHF2, CH2F, linear or branched (C1-C6) alkyl or (C3-C7) cycloalkyl, to their racemates, enantiomers and diastereoisomers and to their mixtures, their tautomers and to their pharmaceutically acceptable salts.
摘要翻译：本发明涉及式（I）的新衍生物，其中A是（C 1 -C 6）烷基，（C 3 -C 6）烯基，（C 3 -C 6）炔基，（C 3 （C 5 -C 7）氮杂双环烷基或（C 5 -C 9）氮杂双环链烯基;（C 1 -C 7）氮杂环烷基，（C 5 -C 9） A-R1使得R 1的氮和吡唑1位的氮必须分开至少两个碳原子，R3是H，卤素，OH，SH，NH2，ORc，SRc，SORa， SO 2 R a，NHCHO，NR a R b，NHC（O）R a，NHC（S）R a或NHSO 2 R a，R 4是芳基或杂芳基; 其中R 5为H，卤素，CF 3，CHF 2，CH 2 F，直链或支链（C 1 -C 6）烷基或（C 3 -C 7）环烷基，与其外消旋体，对映异构体和非对映异构体及其混合物，其互变异构体及其药学上可接受的盐。

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