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    Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor
    41.
    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。

    Fluoroquinoline derivative
    47.
    发明授权
    Fluoroquinoline derivative 失效
    氟喹啉衍生物

    公开(公告)号：US5776948A

    公开(公告)日：1998-07-07

    申请号：US728431

    申请日：1996-10-09

    申请人： Takeshi Yokota ,  Masayuki Haramura ,  Akira Okamachi ,  Toshihiko Makino

    发明人： Takeshi Yokota ,  Masayuki Haramura ,  Akira Okamachi ,  Toshihiko Makino

    IPC分类号： C07D215/56 ,  C07D401/04 ,  C07D405/04 ,  A61K31/47 ,  C07D215/18 ,  C07D215/233

    CPC分类号： C07D215/56 ,  C07D401/04 ,  C07D405/04

    摘要： Antibacterial fluoroquinoline derivatives and salts thereof of the following formula are stable and have low toxicity and high photostability and low cytotoxicity under light irradiation: ##STR1## wherein R.sub.1 is hydrogen or lower alkyl; R.sub.2 is hydrogen, optionally protected amino, optionally protected aminocarbonyl or optionally protected carboxyl; R.sub.5 is halogen, lower alkyl or optionally protected hydroxyl or is the same as R.sub.2 ; R.sub.6 is lower alkyl; A is CH.sub.2, optionally protected nitrogen or oxygen; and n and m are each an integer of from 0 to 4, provided that n +m is an integer of from 1 to 4.

    摘要翻译： 下式的抗菌氟喹啉衍生物及其盐是稳定的，并且在光照射下具有低毒性和高光稳定性和低细胞毒性：其中R1是氢或低级烷基; R2是氢，任选保护的氨基，任选保护的氨基羰基或任选被保护的羧基; R5是卤素，低级烷基或任意保护的羟基或与R2相同; R6是低级烷基; A是CH 2，任选地保护的氮或氧; n和m各自为0〜4的整数，条件是n + m为1〜4的整数。

    6-aryl-(methyl - or methylidone)-quinoline derivatives as voltage-gated potassium channel blockers
    49.
    发明授权
    6-aryl-(methyl - or methylidone)-quinoline derivatives as voltage-gated potassium channel blockers 失效
    6-甲基 - 或甲基吡啶酮 - 喹啉衍生物作为电压门控钾通道阻断剂

    公开(公告)号：US5753676A

    公开(公告)日：1998-05-19

    申请号：US448467

    申请日：1995-09-29

    申请人： Roger Crossley ,  Albert Opalko ,  Peter Jonathan Meade ,  Anderson Decourtney Ifill ,  Brian John Bushell

    发明人： Roger Crossley ,  Albert Opalko ,  Peter Jonathan Meade ,  Anderson Decourtney Ifill ,  Brian John Bushell

    IPC分类号： C07C217/74 ,  C07C229/46 ,  C07D215/12 ,  C07D215/14 ,  C07D215/18 ,  C07D215/20 ,  C07D215/32 ,  C07D215/38 ,  C07D215/54 ,  A61K31/47

    CPC分类号： C07D215/54 ,  C07C217/74 ,  C07C229/46 ,  C07D215/12 ,  C07D215/14 ,  C07D215/18 ,  C07D215/20 ,  C07D215/32 ,  C07D215/38 ,  C07C2101/14

    摘要： This invention concerns a compound of generic formula: ##STR1## or a pharmaceutically acceptable salt thereof, where the dotted lines represent optional bonds, R.sup.3 is an optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl group; optionally substituted by one or more substituents the same or different, R' represents one or more optional substituents the same or different, selected from the following: halogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkoxycarbonyl, C.sub.1 -C.sub.6 hydroxyalkyl, CN, aminocarbonyl, C.sub.2 -C.sub.7 alkanoyloxy(C.sub.1 -C.sub.6 )alkyl, carboxy, C.sub.2 -C.sub.7 alkanoxylamino, optionally substituted C.sub.6 -C.sub.10 or heteroaryl or an optionally substituted (C.sub.6 -C.sub.10 aryl)alkyl or a heteroaryl alkyl radical; and R" represents one or more optional mono- or di- valent substituents in the 5, 7 or 8 positions the same or different: monovalent substituents being selected from the following: C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkanoyloxy, hydroxy, amino, C.sub.2 -C.sub.7 alkanoylamino, C.sub.1 -C.sub.6 alkylamino, C.sub.1 -C.sub.6 hydroxalkyl, C.sub.7 -C.sub.17 aralkyloxyamino, R" can also represent hydroxy in the 6 position (when the optional bond is absent); the di-valent substituents being selected from oxo (i.e .dbd.O) and methylene (i.e .dbd.CH.sub.2); and the N-oxides thereof, which compounds have pharmaceutical uses conferred by their ability to block voltage gated potassium channels.

    摘要翻译： PCT No.PCT / GB95 / 00277 Sec。 371 1995年9月29日第 102（e）1995年9月29日PCT PCT 1995年2月10日PCT公布。 公开号WO95 / 21825 日期：1995年8月17日本发明涉及以下通式的化合物：其中虚线代表任选的键，R 3为任选取代的C 6 -C 10芳基或杂芳基; 任选地被一个或多个相同或不同的取代基取代，R'表示一个或多个选自以下的相同或不同的任选取代基：卤素，C 1 -C 6烷基，C 2 -C 7烷氧基羰基，C 1 -C 6羟基烷基，CN，氨基羰基 ，C 2 -C 7烷酰氧基（C 1 -C 6）烷基，羧基，C 2 -C 7链烷氧基氨基，任选取代的C 6 -C 10或杂芳基或任选取代的（C 6 -C 10芳基）烷基或杂芳基烷基; 并且R“表示相同或不同的5,7或8位中的一个或多个任选的一价或二价取代基：一价取代基选自如下：C 1 -C 6烷基，C 2 -C 7链烷酰氧基，羟基，氨基 ，C 2 -C 7烷酰基氨基，C 1 -C 6烷基氨基，C 1 -C 6羟烷基，C 7 -C 17芳烷氧基氨基，R“也可以表示6位羟基（当不存在任选键时）。 二价取代基选自氧代（即= O）和亚甲基（即= CH 2）; 其N-氧化物，其化合物具有通过其阻断电压门控钾通道的能力而赋予的药学用途。