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    Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor
    5.
    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。

    Use of 2-aminothiazoline derivatives as inhibitors of inducible no-synthase
    6.
    发明授权
    Use of 2-aminothiazoline 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：US06451821B1

    公开(公告)日：2002-09-17

    申请号：US09878814

    申请日：2001-06-08

    申请人： Jean-Christophe Carry ,  Dominique Damour ,  Claude Guyon ,  Serge Mignani ,  Antony Bigot ,  Eric Bacque ,  Michel Tabart

    发明人： Jean-Christophe Carry ,  Dominique Damour ,  Claude Guyon ,  Serge Mignani ,  Antony Bigot ,  Eric Bacque ,  Michel Tabart

    IPC分类号： A61K3144

    CPC分类号： C07D417/06 ,  A61K31/426 ,  A61K31/4439 ,  C07D277/18

    摘要： The present invention relates to the use of 2-aminothiazoline derivatives of formula: in which either R1 is a hydrogen atom or an alkyl radical and R2 is an alkyl, -alk—NH2, —CH2—R3, —CH2—S—R4 or phenyl radical substituted with a nitro or —NH— C (═NH) CH3 radical, or R1 is an alkyl radical and R2 is a hydrogen atom, R3 is a (3-6C) cycloalkyl, pyridyl, pyridyl N-oxide, thienyl, thiazolyl, imidazolyl, pyrazinyl, triazolyl or phenyl radical or a phenyl radical substituted with a nitro, hydroxy or carboxyl radical, R4 represents a pyridyl or pyridyl N-oxide radical, alk represents an alkylene radical, or pharmaceutically acceptable salts thereof, as inhibitors of inducible NO-synthase.

    摘要翻译： 本发明涉及下式的2-氨基噻唑啉衍生物的用途：其中R1是氢原子或烷基，R2是烷基，-alk-NH2，-CH2-R3，-CH2-S-R4或 被硝基或-NH- C（= NH）CH 3基取代的苯基，或R 1是烷基，R 2是氢原子，R 3是（3-6C）环烷基，吡啶基，吡啶基N-氧化物，噻吩基， 噻唑基，咪唑基，吡嗪基，三唑基或苯基或被硝基，羟基或羧基取代的苯基，R4表示吡啶基或吡啶基N-氧化物基，alk表示亚烷基或其药学上可接受的盐，作为 诱导型NO合成酶。

    4-Substituted quinoline derivatives, method and intermediates for their preparation and pharmaceutical compositions containing them
    9.
    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。

    Method for preparing enantiomerically enriched N-carboxyanhydride
    10.
    发明授权
    Method for preparing enantiomerically enriched N-carboxyanhydride 有权
    制备对映体富集的N-羧酸酐的方法

    公开(公告)号：US08119813B2

    公开(公告)日：2012-02-21

    申请号：US12617398

    申请日：2009-11-12

    申请人： Antony Bigot ,  Maxime Lampilas

    发明人： Antony Bigot ,  Maxime Lampilas

    IPC分类号： C07D263/04 ,  C07C271/18

    CPC分类号： C07D263/44

    摘要： This disclosure relates to methods for preparing an enantiomerically enriched N-carboxyanhydride of an amino alpha acid of the formula (IIIa) or (IIIb): from a compound of the formula (IIa) or (IIb), respectively: wherein R1, R2, and R3 are as defined in the disclosure.

    摘要翻译： 本公开涉及分别由式（IIa）或（IIb）的化合物制备分子式（IIIa）或（IIIb）的氨基酸的对映体富集的N-羧酸酐的方法：其中R1，R2， 和R3如本公开中所定义。