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。

公开(公告)号：US5541175A

公开(公告)日：1996-07-30

申请号：US301619

申请日：1994-09-07

申请人： Jae H. Yeo ,  Chan S. Bang ,  Jong C. Lim ,  Young M. Woo ,  Deog H. Yang ,  Se H. Kim ,  Jae H. Jeon ,  Mu Y. Kim ,  Sam S. Kim ,  Tae H. Lee ,  Yong Z. Kim ,  Hun S. Oh

发明人： Jae H. Yeo ,  Chan S. Bang ,  Jong C. Lim ,  Young M. Woo ,  Deog H. Yang ,  Se H. Kim ,  Jae H. Jeon ,  Mu Y. Kim ,  Sam S. Kim ,  Tae H. Lee ,  Yong Z. Kim ,  Hun S. Oh

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  C07D501/04 ,  C07D501/24 ,  C07D501/60 ,  A01K31/545

CPC分类号： C07D501/00 ,  Y02P20/55

摘要： The present invention relates to a cephalosporin compound represented by the following general formula (I): ##STR1## its pharmaceutically acceptable non-toxic salt, physiologically hydrolyzable ester, hydrate or solvate, or isomers thereof, in whichR.sup.1 represents hydrogen or an amino-protecting group,R.sup.2 and R.sup.3 can be identical or different and independently of one another represent hydrogen or a hydroxy-protecting group, orR.sup.2 and R.sup.3 together can form a cyclic diol-protecting group,R.sup.4 represents hydrogen or a carboxyl-protecting group,R.sup.5, R.sup.6 and R.sup.7 independently of one another represent hydrogen, amino or substituted amino, hydroxy, alkoxy, C.sub.1-4 alkyl, carboxyl or alkoxycarbonyl, orR.sup.5 and R.sup.6 together with the carbon atoms to which they are attached can form a C.sub.3-7 cycle, andQ represents CH or N,and to a process for preparation thereof and a pharmaceutical composition containing the compound (I) as an active ingredient.

摘要翻译： 本发明涉及由以下通式（I）表示的头孢菌素化合物：其药学上可接受的无毒盐，生理上可水解的酯，水合物或溶剂合物或其异构体，其中R 1 表示氢或氨基保护基，R2和R3可以相同或不同，彼此独立地表示氢或羟基保护基，或者R2和R3一起可以形成环状二醇保护基，R4表示氢或 羧基保护基，R 5，R 6和R 7彼此独立地表示氢，氨基或取代的氨基，羟基，烷氧基，C 1-4烷基，羧基或烷氧基羰基，或者R 5和R 6与它们所连接的碳原子一起可以 形成C3-7周期，Q表示CH或N，以及其制备方法和含有化合物（I）作为活性成分的药物组合物。