公开(公告)号：US5547962A

公开(公告)日：1996-08-20

申请号：US261446

申请日：1994-06-17

申请人： Yasuo Ito ,  Hideo Kato ,  Singo Yasuda ,  Noriyuki Kado ,  Toshihiko Yoshida ,  Yoichi Yamamoto

发明人： Yasuo Ito ,  Hideo Kato ,  Singo Yasuda ,  Noriyuki Kado ,  Toshihiko Yoshida ,  Yoichi Yamamoto

IPC分类号： C07D401/04 ,  A61K31/47 ,  A61K31/4725 ,  A61P31/04 ,  C07D215/56 ,  C07D215/233

CPC分类号： C07D215/56 ,  C07D401/04

摘要： A 5-amino-8-methyl-7-pyrrolidinylquinoline-3-carboxylic acid derivative represented by the general formula: ##STR1## wherein R.sup.1 is a hydrogen atom or a lower alkyl group; R.sup.2 is a hydrogen atom, a lower alkyl group, a lower alkanoyl group, a halogenated lower alkanoyl group or a residue of carboxylic acid ester; R.sup.3 is a hydrogen atom or a lower alkyl group; R.sup.4, R.sup.5 or R.sup.6 are each independently a hydrogen atom or a lower alkyl group; or two of R.sup.4, R.sup.5 and R.sup.6 may be taken together to form a --(CH.sub.2).sub.n -group wherein n is 1 or 2, a stereoisomer thereof, or a pharmacologically acceptable salt thereof, the process for preparing these compounds, a pharmaceutical composition comprising an effective amount of these compounds and methods for the treatment of infectious diseases through the administration to patients of an effective amount of these compounds, and intermediates of these compounds are disclosed. These compounds are effective as antibacterial agents.

摘要翻译： 由以下通式表示的5-氨基-8-甲基-7-吡咯烷基喹啉-3-羧酸衍生物：其中R1是氢原子或低级烷基; R2是氢原子，低级烷基，低级烷酰基，卤代低级烷酰基或羧酸酯的残基; R3是氢原子或低级烷基; R4，R5或R6各自独立地为氢原子或低级烷基; 或R 2，R 5和R 6中的两个可以一起形成其中n为1或2的 - （CH 2）n - 基团，其立体异构体或其药理学上可接受的盐，制备这些化合物的方法，药物组合物 包括有效量的这些化合物和通过向患者施用有效量的这些化合物来治疗感染性疾病的方法，以及这些化合物的中间体。 这些化合物作为抗菌剂是有效的。