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    • 4. 发明授权
    • Quinolylpropylpiperidine derivatives, preparation process and intermediates, and compositions including them
    • 醌基丙基哌啶衍生物,制备方法和中间体,以及包括它们的组合物
    • US06806277B2
    • 2004-10-19
    • US10622655
    • 2003-07-18
    • Eric BacquéJean-Luc MalleronSerge MignaniMichel Tabart
    • Eric BacquéJean-Luc MalleronSerge MignaniMichel Tabart
    • A61K3147
    • C07D401/06C07D409/12
    • Quinolylpropylpiperidine derivatives of general formula (I) in which: R1 is NH2, alkylamino, dialkylamino, hydroxyamino, alkyl(alkyloxy)amino or alkyloxyamino, R2 is a carboxyl, carboxymethyl or hydroxymethyl radical, R3 is alkyl (1 to 6C) substituted by phenylthio which can itself carry 1 to 3 substituents selected from halogen, OH, alkyl, alkyloxy, CF3, OCF3, COOH, alkyloxycarbonyl, CN and NH2, by cycloalkylthio (3 to 7 members) or by heteroarylthio (5 to 6 members) comprising 1 to 4 heteroatoms selected from N, S and O and optionally itself substituted [by halogen, OH, alkyl, alkyloxy, CF3, OCF3, ═O, COOH, alkyloxycarbonyl, CN or NH2] or R3 is propargyl substituted by phenyl which can itself carry 1 to 3 substituents selected from halogen, OH, alkyl, alkyloxy, CF3, OCF3, COOH, alkyloxycarbonyl, CN and NH2 or substituted by cycloalkyl comprising 3 to 7 members or substituted by 5- to 6-membered heteroaryl comprising 1 to 4 heteroatoms chosen from N, O or S and optionally itself substituted by halogen, OH, alkyl, alkyloxy, CF3, OCF3, ═O, COOH, alkyloxycarbonyl, CN or NH2, and R4 is alkyl (1 to 6C), alkenyl-CH2—, alkynyl-CH2— (3 to 7C), cycloalkyl or (cycloalkyl)alkyl, in their diastereoisomeric forms or their mixtures, and their pharmaceutically acceptable salts. These novel derivatives are particularly advantageous antimicrobial agents.
    • 通式(I)的喹啉基丙基哌啶衍生物,其中:R1是NH2,烷基氨基,二烷基氨基,羟基氨基,烷基(烷氧基)氨基或烷氧基氨基,R2是羧基,羧甲基或羟甲基,R3是被苯硫基取代的(1-6) 其可以自身携带1至3个选自卤素,OH,烷基,烷氧基,CF 3,OCF 3,COOH,烷氧基羰基,CN和NH 2的取代基,被环烷硫基(3至7个成员)或通过杂芳硫基(5至6个成员)包含1至 4个选自N,S和O的杂原子,并且任选地本身被[由卤素,OH,烷基,烷氧基,CF 3,OCF 3,= O,COOH,烷氧基羰基,CN或NH 2]取代的R 3或被苯基取代的苯基, 被选自卤素,OH,烷基,烷氧基,CF 3,OCF 3,COOH,烷氧基羰基,CN和NH 2的3个取代基,或被包含3至7个成员的环烷基或被包含1至4个选自 N,O或S,以及任选的其自身取代基 CN,NH 2,R 4是烷基(1-6),链烯基-CH 2 - ,炔基-CH 2 - (3至7C),环烷基(C 1 -C 6)烷基,烷氧基羰基, 或(环烷基)烷基,其非对映异构体形式或其混合物及其药学上可接受的盐。这些新型衍生物是特别有利的抗微生物剂。