Invention Grant
US09328089B2 7-{(3S,4S)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidine-1-YL}-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid crystal
有权
7 - {(3S,4S)-3 - [(环丙基氨基)甲基] -4-氟吡咯烷-1-基} -6-氟-1-(2-氟乙基)-8-甲氧基-4-氧代-1,4- - 二氢喹啉-3-羧酸晶体
- Patent Title: 7-{(3S,4S)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidine-1-YL}-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid crystal
- Patent Title (中): 7 - {(3S,4S)-3 - [(环丙基氨基)甲基] -4-氟吡咯烷-1-基} -6-氟-1-(2-氟乙基)-8-甲氧基-4-氧代-1,4- - 二氢喹啉-3-羧酸晶体
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Application No.: US14741713Application Date: 2015-06-17
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Publication No.: US09328089B2Publication Date: 2016-05-03
- Inventor: Ichiro Araya , Akinori Goto , Wataru Minagawa , Keiko Funada , Muneki Nagao
- Applicant: KYORIN PHARMACEUTICAL CO., LTD.
- Applicant Address: JP Tokyo
- Assignee: KYORIN PHARMACEUTICAL CO., LTD.
- Current Assignee: KYORIN PHARMACEUTICAL CO., LTD.
- Current Assignee Address: JP Tokyo
- Agency: Wenderoth, Lind & Ponack, L.L.P.
- Priority: JP2011-246209 20111110; JP2012-071739 20120327
- Main IPC: C07D401/04
- IPC: C07D401/04 ; A61K31/4709
![7-{(3S,4S)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidine-1-YL}-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid crystal](/abs-image/US/2016/05/03/US09328089B2/abs.jpg.150x150.jpg)
Abstract:
Disclosed is a technique for improving the water solubility and storage stability of 7-{(3S,4S)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidine-1-yl}-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (compound (1)) that is safe and not only has a strong antibacterial action but also is effective for resistant bacteria for which conventional antibacterial agent are less effective. Crystals of the hydrochloride salt of the compound (1), crystals of the hydrochloride salt hydrate of the compound (1), and crystals of the methanesulfonate salt of the compound (1) are provided. In these crystals, decomposition due to influences of light is suppressed as compared to that in crystals of the compound (1) in free, and their storage stability is high. These crystals have higher solubility in water than the crystals of the compound (1) in free.
Public/Granted literature
- US20150284361A1 7--6-FLUORO-1-(2-FLUOROETHYL)-8-METHOXY-4-OXO-1,4-DIHYDROQUINOLINE-3-CARBOXYLIC ACID CRYSTAL Public/Granted day:2015-10-08
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