发明名称 |
7-{(3S,4S)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidine-1-yl}-6-fluoro-1-(2-fluorodethyl)-acid crystal |
摘要 |
Disclosed is a technique for improving the water solubility and storage stability of 7-{(3S,4S)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidine-1-y1}-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. |
申请公布号 |
US9090587(B2) |
申请公布日期 |
2015.07.28 |
申请号 |
US201214352141 |
申请日期 |
2012.11.09 |
申请人 |
KYORIN PHARMACEUTICAL CO., LTD. |
发明人 |
Araya Ichiro;Goto Akinori;Minagawa Wataru;Funada Keiko;Nagao Muneki |
分类号 |
C07D401/04;A61K31/4709 |
主分类号 |
C07D401/04 |
代理机构 |
Wenderoth, Lind & Ponack, L.L.P. |
代理人 |
Wenderoth, Lind & Ponack, L.L.P. |
主权项 |
1. A crystal 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 hydrochloride salt, having powder X-ray diffraction peaks at diffraction angles 2θ of 10.8°±0.2°, 12.9°±0.2°, and 24.7°±0.2°. |
地址 |
Tokyo JP |