Title:
PHENYL PYRROLE DERIVATIVE CRYSTAL
Document Type and Number:
WIPO Patent Application WO/2012/147832
Kind Code:
A1
Abstract:
Provided is a phenyl pyrrole derivative monomethanesulfonate having: excellent glucokinase activation action; markedly improved solubility, hygroscopicity, and stability; and excellent oral absorption. Also provided is a monomethanesulfonate crystal. The present invention provides a (2S)-2-(3-{5-[(5S)-5-methyl-4,5-dihydro-1,3-oxazol-2-yl]-1H-pyrrole-2-yl}-5-{[5-(methylsulfonyl) pyrazin-2-yl]oxy} phenoxy)propane-1-ol monomethanesulfonate having excellent glucokinase activation activity, and also provides a crystal thereof, and a drug containing the monomethanesulfonate or crystal, and an agent for preventing and/or treating diabetes or the like containing the same.
Inventors:
ONO MAKOTO
Application Number:
PCT/JP2012/061175
Publication Date:
November 01, 2012
Filing Date:
April 26, 2012
Export Citation:
Assignee:
DAIICHI SANKYO CO LTD (JP)
ONO MAKOTO
ONO MAKOTO
International Classes:
C07D413/14; A61K31/497; A61P3/10
Domestic Patent References:
| WO2009099080A1 | 2009-08-13 | |||
| WO2009099080A1 | 2009-08-13 |
Foreign References:
| JP2011051978A | 2011-03-17 |
Other References:
HIROSHI NAGASE, MEDICINAL CHEMISTRY LAST VOLUME, 1999, pages 347 - 348, 359 TO 362, XP008160781
GRUNENBERG, A. ET AL.: "Theoretical derivation and practical application of energy/temperature diagrams as an instrument in performulation studies of polymorphic drug substances", INTERNATIONAL JOURNAL OF PHARMACEUTICS, vol. 129, 1996, pages 147 - 158, XP000909867
See also references of EP 2703400A4
GRUNENBERG, A. ET AL.: "Theoretical derivation and practical application of energy/temperature diagrams as an instrument in performulation studies of polymorphic drug substances", INTERNATIONAL JOURNAL OF PHARMACEUTICS, vol. 129, 1996, pages 147 - 158, XP000909867
See also references of EP 2703400A4
Attorney, Agent or Firm:
ISHIBASHI Koki et al. (JP)
Kimiki Ishibashi (JP)
Kimiki Ishibashi (JP)
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Claims: