公开(公告)号：US5677316A

公开(公告)日：1997-10-14

申请号：US473357

申请日：1995-06-07

申请人： Hideki Ao ,  Tsuyoshi Kuroda ,  Kazuyuki Kawasaki ,  Akihiko Moriguchi ,  Yoshifumi Ikeda ,  Shin-ichi Uesato

发明人： Hideki Ao ,  Tsuyoshi Kuroda ,  Kazuyuki Kawasaki ,  Akihiko Moriguchi ,  Yoshifumi Ikeda ,  Shin-ichi Uesato

IPC分类号： C07D401/04 ,  A01N43/42 ,  A61K31/47 ,  C07D215/16

CPC分类号： C07D401/04

摘要： 8-Methoxy-quinolonecarboxylic acid derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom, a lower alkyl, a phenylalkyl or an ester residue hydrolyzable in the living body, R.sub.2 is a hydrogen atom or methyl and n is an integer of 1, optical isomers thereof, pharmaceutically acceptable salts thereof and hydrates thereof. The 8-methoxy-quinolonecarboxylic acid derivatives of the present invention have enforced and a wide range of in vitro and in vivo antibacterial effects against Gram-positive bacteria, while retaining a strong antibacterial effect against Gram-negative bacteria, that the conventional quinolonecarboxylic acid antibacterial agents have. In addition, the compounds of the present invention scarcely show problematic side-effects and are low toxic. Therefore, they are expected to show superior clinical effects as antibacterial agents.

摘要翻译： 式（I）的8-甲氧基 - 喹啉酮羧酸衍生物，其中R1是氢原子，低级烷基，苯基烷基或可在生物体中水解的酯残基，R2是氢原子或甲基，n是 1的整数，其光学异构体，其药学上可接受的盐和其水合物。 本发明的8-甲氧基 - 喹诺酮羧酸衍生物对革兰氏阳性细菌的体外和体内抗菌作用具有广泛的应用范围，同时保留对革兰氏阴性细菌的强烈的抗菌作用，常规的喹诺酮羧酸抗菌剂 代理商有。 此外，本发明的化合物几乎不显示有问题的副作用，并且毒性低。 因此，作为抗菌剂，预期其具有优异的临床效果。