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Title:
CRYSTAL POLYMORPHISM OF KCNQ 2-5 CHANNEL ACTIVATOR
Document Type and Number:
WIPO Patent Application WO/2017/183725
Kind Code:
A1
Abstract:
Crystal polymorphism may be present in a crystalline compound. In cases where there is crystal polymorphism, depending on the crystal form, solubility, dissolution rate, or stability against heat, light, humidity and the like are different. Accordingly, in the manufacturing of medicaments, selecting a crystal form of the drug substance most suitable for the indicated disease and dosage form is a very important task. The present invention is related to a novel crystal form (A crystal, W crystal, and hydrate crystal (H crystal)) of compound I having a strong opening action with respect to KCNQ 2-5 channels.

Inventors:
YASHIRO KENTARO (JP)
KIJIMA HIDEOMI (JP)
WAKAMATSU DAISUKE (JP)
SAITO TETSUJI (JP)
Application Number:
PCT/JP2017/016109
Publication Date:
October 26, 2017
Filing Date:
April 21, 2017
Export Citation:
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Assignee:
ONO PHARMACEUTICAL CO (JP)
International Classes:
C07D213/61; A61K31/44; A61P13/10; A61P43/00
Domestic Patent References:
WO2016063990A12016-04-28
Foreign References:
JP2016508960A2016-03-24
JP2015514728A2015-05-21
JP2010535244A2010-11-18
Other References:
YUSAKU SHIOJI, MANUFACTURE TECHNOLOGY OF SOLID TABLET, vol. 9, 27 January 2003 (2003-01-27), Tokyo, pages 12 - 13, XP009507058
BYRN,S. ET AL.: "Pharmaceutical Solids: A Strategic Approach to Regulatory Considerations", PHARMACEUTICAL RESEARCH, vol. 12, no. 7, 1995, pages 945 - 954, XP055399407
AKIRA OGATA: "Passage, KAGAKU JIKKEN SOSAHO", KAGAKU JIKKEN SOSAHO, 20 November 1963 (1963-11-20), pages 366 - 399, XP009510132
CHEMICAL SOCIETY OF JAPAN: "Passages, Jikken kagaku kōza zoku dai 2 (bunri to seisei) [Experimental Chemistry Course Sequel 2 (Separation and Purification)]", JIKKEN KAGAKU KŌZA ZOKU DAI 2 (BUNRI TO SEISEI) , 25 January 1967 (1967-01-25), pages 159-162,184 - 193, XP009510623, DOI: 10.11501/1369199
"Jikken Kagaku Guidebook", THE CHEMICAL SOCIETY OF JAPAN, 30 April 1992 (1992-04-30), JP, pages 130 - 131, XP009510266, ISBN: 4-621-02830-8
See also references of EP 3447047A4
Attorney, Agent or Firm:
AOKI, Atsushi et al. (JP)
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