公开(公告)号：US5633262A

公开(公告)日：1997-05-27

申请号：US490978

申请日：1995-06-15

申请人： Chang Y. Hong ,  Young K. Kim ,  Jay H. Chang ,  Se H. Kim ,  Hoon Choi ,  Do H. Nam ,  Jin H. Kwak ,  Yi N. Jeong ,  Jeong I. Oh ,  Mu Y. Kim

发明人： Chang Y. Hong ,  Young K. Kim ,  Jay H. Chang ,  Se H. Kim ,  Hoon Choi ,  Do H. Nam ,  Jin H. Kwak ,  Yi N. Jeong ,  Jeong I. Oh ,  Mu Y. Kim

IPC分类号： A61K31/435 ,  A61K31/47 ,  A61P31/04 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  A61K31/44 ,  C07D471/02

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04

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 antibacterial agents having a weak activity against gram-positive bacterial strains and also has a broad antibacterial spectrum and a highly improved pharmacokinetic property: ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and Q are defined as described in the specification.

摘要翻译： 本发明涉及具有优异抗菌活性的新型喹诺酮化合物。 更具体地说，本发明涉及下述式（I）所示的喹啉（萘啶）羧酸衍生物，其在喹诺酮核的7-位具有4-氨基甲基-3-氧代吡咯烷酮取代基，显示出优异的抗菌性 与具有对革兰氏阳性菌菌株的弱活性的已知喹诺酮类抗菌剂相比，具有广泛的抗菌谱和高度改善的药代动力学性质：其中R，R1，R2，R3，R4和 Q如说明书所述定义。