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    4-substituted quinoline derivatives, method and intermediates for their preparation and pharmaceutical compositions containing them
    3.
    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。

    Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor
    4.
    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

    Use of 2-amino-thiazoline derivatives as inhibitors of inducible no-synthase
    5.
    发明授权
    Use of 2-amino-thiazoline derivatives as inhibitors of inducible no-synthase 失效
    使用2-氨基 - 噻唑啉衍生物作为诱导型无合成酶的抑制剂

    公开(公告)号：US07227022B2

    公开(公告)日：2007-06-05

    申请号：US11200713

    申请日：2005-08-10

    申请人： Antony Bigot ,  Jean-Christophe Carry ,  Serge Mignani

    发明人： Antony Bigot ,  Jean-Christophe Carry ,  Serge Mignani

    IPC分类号： C07D241/04

    CPC分类号： C07D295/13 ,  C07D241/04 ,  C07D277/18 ,  C07D295/15 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

    摘要： The present invention relates to a process for preparing 2-amino-thiazoline derivatives of formula (II): in which either Y is a methylene (CH2) and X is chosen from the following groups: O, NH, (C1–C4) N-Alkyl, N-Bn, N-Ph, N-(2-Py), N-(3-Py), N-(4-Py), N-2-pyrimidyl, N-5-pyrimidyl, S, SO, SO2, CH2 or CHPh; or Y is a carbonyl (C═O) and X is chosen from the following groups: NH, N-Ph, N-(2-Py), N-(3-Py), N-(4-Py), N-2-pyrimidyl or N-5-pyrimidyl.

    摘要翻译： 本发明涉及制备式（II）的2-氨基 - 噻唑啉衍生物的方法：其中Y是亚甲基（CH 2 CH 2），X选自下列基团：O， NH，（C 1 -C 4）N-烷基，N-Bn，N-Ph，N-（2-Py），N-（3-Py），N-（4-Py），N-2-嘧啶基，N -5-嘧啶基，S，SO，SO 2，CH 2或CHPh; 或者Y是羰基（CO），X选自下列基团：NH，N-Ph，N-（2-Py），N-（3-Py），N-（4-Py），N-2 - 嘧啶基或N-5-嘧啶基。

    Novel process for preparing 3-fluoroquinolines
    7.
    发明申请
    Novel process for preparing 3-fluoroquinolines 失效
    制备3-氟喹啉的新方法

    公开(公告)号：US20050182259A1

    公开(公告)日：2005-08-18

    申请号：US10985533

    申请日：2004-11-10

    申请人： Youssef El-Ahmad ,  Jean-Pierre Leconte ,  Joel Malpart ,  Serge Mignani ,  Stephane Mutti ,  Michel Tabart

    发明人： Youssef El-Ahmad ,  Jean-Pierre Leconte ,  Joel Malpart ,  Serge Mignani ,  Stephane Mutti ,  Michel Tabart

    IPC分类号： C07D215/18 ,  C07D215/38 ,  C07D215/12

    CPC分类号： C07D215/38 ,  C07D215/18 ,  Y02P20/55

    摘要： The invention relates to a novel preparation of 3-fluoroquinolines of formula (I) in which R1, R2, R3 and R4 represent: a) a fluorine; b) an alkyl optionally substituted with one to three fluorines, with OR5 in which R5 is an alkyl, a hydrogen or a hydroxyl-protecting group, or with NR′R″ in which R′ and R″ represent an alkyl, a hydrogen or an amino-protecting group; c) OR6 in which R6 represents a hydrogen, a phenol-protecting group or an alkyl, optionally substituted with a fluorine, with OR5 or with NR′R″ as defined above; d) NR′1R″1 in which R′1 and R″1 have the values of R′ et R″ or represent an alkyl substituted with a fluorine, with OR5 or NR′R″ as defined above; e) CO2Ra, in which Ra represents hydrogen, alkyl or a carboxyl-protecting group, and also novel intermediate compounds. The quinolines of formula (I) are intermediates useful in the preparation of compounds having antibacterial activity, described in particular in applications WO 02/40474 or WO 02/72572.

    摘要翻译： 本发明涉及式（I）的3-氟喹啉的新型制备方法，其中R 1，R 2，R 3和R 3， 代表：a）氟; b）任选被一至三个氟取代的烷基，其中R 5是烷基，氢或羟基保护基或NR' 其中R'和R“表示烷基，氢或氨基保护基的”R“ c）OR 6其中R 6表示氢，苯酚保护基或任选被氟取代的烷基，OR 5或N >或如上定义的NR'R“ d）NR'1 R“1其中R'1和R”1 <1的数值为 或者代表被氟取代的烷基，其具有如上定义的OR 5或NR'R“; e）其中R aa代表氢，烷基或羧基保护基，以及新的中间体化合物的CO 2 CO 2。 式（I）的喹啉是可用于制备具有抗菌活性的化合物的中间体，特别在申请WO 02/40474或WO 02/72572中有所描述。