Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor
    9.
    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

    IPC分类号: A61K31/4545 C07D401/06

    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