发明名称 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
摘要 Disclosed is a technique for improving the water solubility and storage stability of 7-{(3S,4S)-3-[(cyclopropylamino)methyl]-4-fluoropyyrolidine-1-yl}-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquin oline-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 EP2778159(A1) 申请公布日期 2014.09.17
申请号 EP20120846895 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;A61P31/04 主分类号 C07D401/04
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