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发明授权
US07232833B2 4-substituted quinoline derivatives, method and intermediates for their preparation and pharmaceutical compositions containing them 失效
4-取代喹啉衍生物，其制备方法和中间体以及含有它们的药物组合物

4-substituted quinoline derivatives, method and intermediates for their preparation and pharmaceutical compositions containing them
摘要：
The invention relates to 4-substituted quinoline compounds of general formula: which are active as antimicrobials, in which: X1, X2, X3, X4 and X5 is C—R′1, to C—R′5 respectively, or alternatively at most one represents N, Y represents CHR, CO, CROH, CRNH2, CRF or CF2, R being a hydrogen or alkyl, m is 1, 2 or 3 and n is 0, 1 or 2, Z is CH2 or Z is O, S, SO, SO2 and, in this case, n is equal to 2, R2 is —CO2R, —CH2CO2R, —CH2—CH2CO2R, —CH2OH or —CH2—CH2OH, wherein R is as defined above, R3 represents phenyl, heteroaryl or alk-Ro3, where alk is alkyl and Ro3 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（中）：

本发明涉及以下通式的4-取代喹啉化合物：其作为抗微生物剂是有活性的，其中：X 1，X 2，X 3， >，X 4和X 5分别为C-R'1，C-R'5， 或者至多一个表示N，Y表示CHR，CO，CROH，CRNH 2，CRF或CF 2，R为氢或烷基，m为1,2 或3，n为0,1或2，Z为CH 2或Z为O，S，SO，SO 2，在这种情况下，n等于 2，R 2是-CO 2 R，-CH 2 CO 2 R，-CH 2， 2个-CH 2 CO 2 R 2，-CH 2 OH或-CH 2 -CH（CH 2） R 2 OH，其中R如上所定义，R 3表示苯基，杂芳基或烷基-SO 3 - ， - 其中烷基是烷基，R 3 O 3表示各种基团，其中适当地含有它们的对映体或非对映异构形式或其混合物中的氧，硫或胺， d /或适当时以合成或反式形式或其混合物及其盐。

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