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Have the 7 (4 aminomethyl 3 oxime) pyro lysine substitution product the new quinoline carboxylic acid derivative and its production manner

机译:具有7(4氨基甲基3肟)吡啶赖氨酸取代产物的新喹啉羧酸衍生物及其生产方式

摘要

The present invention relates to a novel quinolone compound having an excellent antibacterial activity. More specifically, the present invention relates to a novel quinoline(naphthyridine)carboxylic acid derivative represented by the following formula (I), which has an 4-aminomethyl-3-oximepyrrolidine substituent on 7-position of the quinolone nucleus and shows a superior antibacterial activity in contrast to the known quinolone antibactrial agents having a weak activity against gram-positive bacterial strains and also has a broad antibacterial spectrum and a highly improved pharmacokinetic property : CHEM wherein R, R1, R2, R3, R4 and Q are defined as described in the specification.
机译:本发明涉及具有优异抗菌活性的新型喹诺酮化合物。更具体地,本发明涉及由下式(I)表示的新型喹啉(萘啶)羧酸衍生物,其在喹诺酮核的7位具有4-氨基甲基-3-肟基吡咯烷取代基,并且显示出优异的抗菌性。与已知的喹诺酮类抗细菌药相反,其对革兰氏阳性细菌菌株的活性较弱,并且具有广谱抗菌谱和高度改善的药代动力学性质:其中定义了R,R1,R2,R3,R4和Q如规范中所述。

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