公开(公告)号：US07713997B2

公开(公告)日：2010-05-11

申请号：US11719547

申请日：2005-11-17

申请人： Akira Yazaki ,  Yasuhiro Kuramoto ,  Kenji Itoh ,  Kazusa Yoshikai ,  Yuzo Hirao ,  Yoshihiro Ohshita ,  Norihiro Hayashi ,  Hirotaka Amano ,  Takayuki Amago ,  Hitomi Takenaka

发明人： Akira Yazaki ,  Yasuhiro Kuramoto ,  Kenji Itoh ,  Kazusa Yoshikai ,  Yuzo Hirao ,  Yoshihiro Ohshita ,  Norihiro Hayashi ,  Hirotaka Amano ,  Takayuki Amago ,  Hitomi Takenaka

IPC分类号： C07D215/38 ,  A61K38/02

CPC分类号： C07D401/14

摘要： The present invention provides an agent which exhibits excellent antibacterial activity, low toxicity, improved bioavailability, and low binding rate to serum proteins. The present invention is directed to a pyridonecarboxylic acid derivative represented by formula (1): or a salt thereof, wherein R1 represents a methyl group, a fluorine atom, or a chlorine atom; R2 represents a hydrogen atom or a lower alkyl group; R3 represents an isopropyl group or a tert-butyl group; R4 represents a methyl group or a halogen atom; and R5 represents a fluorine atom or a chlorine atom. The present invention is also directed to an antibacterial agent and a medicament containing the derivative or the salt thereof as an active ingredient.

摘要翻译： 本发明提供了具有优异的抗菌活性，低毒性，改善的生物利用度和与血清蛋白的低结合速率的试剂。 本发明涉及由式（1）表示的吡啶酮羧酸衍生物或其盐，其中R1表示甲基，氟原子或氯原子; R2表示氢原子或低级烷基; R3表示异丙基或叔丁基; R4表示甲基或卤原子; R 5表示氟原子或氯原子。 本发明还涉及一种抗菌剂和含有其衍生物或其盐作为活性成分的药物。

公开(公告)号：US20090149440A1

公开(公告)日：2009-06-11

申请号：US11719547

申请日：2005-11-17

申请人： Akira Yazaki ,  Yasuhiro Kuramoto ,  Kenji Itoh ,  Kazusa Yoshikai ,  Yuzo Hirao ,  Yoshihiro Ohshita ,  Norihiro Hayashi ,  Hirotaka Amano ,  Takayuki Amago ,  Hitomi Takenaka

发明人： Akira Yazaki ,  Yasuhiro Kuramoto ,  Kenji Itoh ,  Kazusa Yoshikai ,  Yuzo Hirao ,  Yoshihiro Ohshita ,  Norihiro Hayashi ,  Hirotaka Amano ,  Takayuki Amago ,  Hitomi Takenaka

IPC分类号： A61K31/4709 ,  C07D401/14 ,  A61P31/00

CPC分类号： C07D401/14

摘要： The present invention provides an agent which exhibits excellent antibacterial activity, low toxicity, improved bioavailability, and low binding rate to serum proteins. The present invention is directed to a pyridonecarboxylic acid derivative represented by formula (1): or a salt thereof, wherein R1 represents a methyl group, a fluorine atom, or a chlorine atom; R2 represents a hydrogen atom or a lower alkyl group; R3 represents an isopropyl group or a tert-butyl group; R4 represents a methyl group or a halogen atom; and R5 represents a fluorine atom or a chlorine atom. The present invention is also directed to an antibacterial agent and a medicament containing the derivative or the salt thereof as an active ingredient.

摘要翻译： 本发明提供了具有优异的抗菌活性，低毒性，改善的生物利用度和与血清蛋白的低结合速率的试剂。 本发明涉及由式（1）表示的吡啶酮羧酸衍生物或其盐，其中R1表示甲基，氟原子或氯原子; R2表示氢原子或低级烷基; R3表示异丙基或叔丁基; R4表示甲基或卤原子; R 5表示氟原子或氯原子。 本发明还涉及一种抗菌剂和含有其衍生物或其盐作为活性成分的药物。