公开(公告)号：US06525066B2

公开(公告)日：2003-02-25

申请号：US10124485

申请日：2002-04-18

申请人： Ryoichi Fukumoto ,  Hiroyuki Kusakabe ,  Chong Chu ,  Hiroaki Kimura ,  Satoshi Yanagihara ,  Masatoshi Kato ,  Chisato Hirosawa ,  Seiji Ishiduka ,  Fusae Shizume

发明人： Ryoichi Fukumoto ,  Hiroyuki Kusakabe ,  Chong Chu ,  Hiroaki Kimura ,  Satoshi Yanagihara ,  Masatoshi Kato ,  Chisato Hirosawa ,  Seiji Ishiduka ,  Fusae Shizume

IPC分类号： A61K31435

CPC分类号： C07D455/02 ,  A61K31/4375 ,  Y02A50/473 ,  Y02P20/55

摘要： A compound represented by the following Formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 represents a hydrogen atom or a carboxyl-protecting group, R2 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or a hydroxyl group, R3 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a nitro group, a cyano group, a hydroxyl group or an amino group; R4 represents a hydrogen atom, an amino-protecting group, an alkyl group or a cycloalkyl group, and R5 represents a hydrogen atom, a halogen atom, an alkyl group, an alkenyl group, a cycloalkyl group, an aryl group, an alkoxy group, an alkylthio group, a hydroxyl group, an imino group or an amino group.

摘要翻译： 由下式（I）表示的化合物或其药学上可接受的盐：其中R1表示氢原子或羧基保护基，R2表示氢原子，卤素原子，低级烷基，低级烷氧基或 羟基，R3表示氢原子，卤素原子，低级烷基，低级烷氧基，低级烷硫基，硝基，氰基，羟基或氨基; R4表示氢原子， 氨基保护基，烷基或环烷基，R 5表示氢原子，卤素原子，烷基，烯基，环烷基，芳基，烷氧基，烷硫基，羟基 基团，亚氨基或氨基。

公开(公告)号：US07223773B2

公开(公告)日：2007-05-29

申请号：US10809874

申请日：2004-03-26

申请人： Ryoichi Fukumoto ,  Yoshimi Niwano ,  Hiroyuki Kusakabe ,  Chong Chu ,  Hiroaki Kimura ,  Koh Nagasawa ,  Satoshi Yanagihara ,  Chisato Hirosawa ,  Seiji Ishiduka

发明人： Ryoichi Fukumoto ,  Yoshimi Niwano ,  Hiroyuki Kusakabe ,  Chong Chu ,  Hiroaki Kimura ,  Koh Nagasawa ,  Satoshi Yanagihara ,  Chisato Hirosawa ,  Seiji Ishiduka

IPC分类号： A61K31/44 ,  C07D455/02

CPC分类号： A61K31/4375 ,  C07D455/02 ,  Y02A50/473 ,  Y02P20/55

摘要： The present invention provides a 4-oxoquinolizine antibacterial agent having a 2-pyridone skeleton as a partial structure and also having a strong antibacterial effect on gram-positive bacteria, gram-negative bacteria or anaerobic bacteria. The compound having the following formula (I) or a pharmaceutically acceptable salt thereof: wherein: R1 represents hydrogen atom or a carboxyl-protecting group, R2 represents hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxyl group or hydroxyl group, R3 represents phenyl group or an aromatic substituent selected from the group consisting of 5-membered and 6-membered heterocyclic groups and R3 has a substituent selected from the group consisting of a hydrogen atom, a lower alkyl group, a lower alkoxyl group, a nitro group, a cyano group, an amino group, an acyl group, a carbamoyl group and a ureido group, and R4 represents a hydrogen atom or a halogen atom.

摘要翻译： 本发明提供了具有2-吡啶酮骨架作为部分结构并且对革兰氏阳性细菌，革兰氏阴性细菌或厌氧细菌具有强抗菌作用的4-氧喹诺酮抗菌剂。 具有下式（I）的化合物或其药学上可接受的盐：其中R 1表示氢原子或羧基保护基，R 2表示氢原子， 卤素原子，低级烷基，低级烷氧基或羟基，R 3表示苯基或选自5元和6元杂环基的芳香族取代基，R 3 3 <3>具有选自氢原子，低级烷基，低级烷氧基，硝基，氰基，氨基，酰基，氨基甲酰基的取代基 和脲基，R 4代表氢原子或卤素原子。