公开(公告)号：EP1336611A4

公开(公告)日：2004-07-21

申请号：EP01996540

申请日：2001-11-19

申请人： DAIICHI SEIYAKU CO

发明人： TAKAHASHI HISASHI ,  MIYAUCHI RIE ,  ITOH MASAO ,  TAKEMURA MAKOTO ,  HAYAKAWA ISAO

IPC分类号： C07D401/04 ,  C07D471/04 ,  C07D498/06 ,  A61K31/4709 ,  A61K31/4741 ,  A61P31/04

CPC分类号： C07D401/04 ,  C07D471/04

摘要： 3-(1-Aminocycloalkyl)pyrrolidinyl-substituted-6-dehalodeno(hydrogen-su bstituted)quinolon carboxylic acid derivatives having specific substitunets as represented by the following formula (I), its salts, and hydrates thereof exhibit a broad and potent antibacterial activity on gram-negative and gram-positive bacteria, in particular, resistant bacteria typified by gram-positive cocci, including MRSA, PRSP and VRE . Thus these compounds are usable as drugs.

摘要翻译： 具有下述通式（I）表示的特定取代基的3-（1-氨基环烷基）吡咯烷基 - 取代-6-脱卤（氢取代）喹诺酮羧酸衍生物，其盐和它们的水合物显示广泛且有效的抗菌活性 对革兰氏阴性和革兰氏阳性细菌，特别是以革兰氏阳性球菌为代表的耐药细菌，包括MRSA，PRSP和VRE。 因此，这些化合物可用作药物。

公开(公告)号：EP1298131A4

公开(公告)日：2004-09-08

申请号：EP01917706

申请日：2001-03-30

申请人： DAIICHI SEIYAKU CO

发明人： TAKEMURA MAKOTO ,  TAKAHASHI HISASHI ,  KAWAKAMI KATSUHIRO ,  ITOH MASAO ,  SUZUKI TETSUYA ,  OHTANI TSUYOSHI ,  SEKIGUCHI MASAYASU ,  MIYAUCHI RIE ,  HAYAKAWA ISAO

IPC分类号： A61K31/4709 ,  A61P31/04 ,  C07D401/04 ,  C07M7/00

CPC分类号： C07D401/04 ,  A61K31/4709

摘要： (-)-7-[(7S)-7-Amino-5-azaspiro[2.4]heptan-5-yl]-6-fluoro-1-[(1R,2S)-2-fluoro-1-cyclopropyl]-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid monohydrochloride monohydrate and antibacterial agents containing the same. This compound is excellent in antibacterial activity and safety and highly stable to light and humidity, which makes it useful as an antibacterial agent.