Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor
    8.
    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

    CPC classification number: C07D401/06 C07D211/60 C07D409/14 Y02P20/55

    Abstract: 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.

    Abstract translation: 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。

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