公开(公告)号：EP0990654A4

公开(公告)日：2004-09-15

申请号：EP98921863

申请日：1998-05-28

申请人： DAIICHI SEIYAKU CO

发明人： TAKEMURA MAKOTO ,  TAKAHASHI HISAHI ,  SUGITA KAZUYUKI ,  MIYAUCHI RIE

IPC分类号： A61K31/4709 ,  A61P31/04 ,  C07D401/04 ,  C07D498/06

CPC分类号： C07D401/04

摘要： Substituted cyclobutylamine derivatives with novel structures represented by general formula (I), wherein R1 to R4 and Q represent each a specific substituent and, in particular, Q represents a quinolone derivative of a specific structure. These derivatives are useful as antibacterial compounds which have excellent antibacterial actions over a wide scope of bacteria including gram-negative and gram-positive ones, exert potent antibacterial activities particularly on methicillin-resistant Staphylococcus aureus (MRSA), penicillin-resistant Streptococcus pneumoniae and quinolone-resistant bacteria and are excellent in the in vivo dynamics and safety.

摘要翻译： 具有由通式（I）表示的新结构的取代的环丁基胺衍生物，其中R 1至R 4和Q各自表示特定取代基，并且特别地，Q表示具体结构的喹诺酮衍生物。 这些衍生物作为抗菌化合物是有用的，其在广泛的细菌（包括革兰氏阴性和革兰氏阳性细菌）上具有优异的抗菌作用，对甲氧西林抗性金黄色葡萄球菌（MRSA），耐青霉素肺炎链球菌和喹诺酮 并且在体内动力学和安全性方面非常出色。