Title:
CRYSTAL OF 3,5-DISUBSTITUTED BENZENE ALKYNYL COMPOUND
Document Type and Number:
WIPO Patent Application WO/2016/159327
Kind Code:
A1
Abstract:
The purpose of the present invention is to provide stable crystals of (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidine-1-yl)-1-pyrrolidinyl)-2-propene-1-one, which is useful as an antitumor agent, having excellent oral absorbability and high chemical purity, the crystals being suitable for mass production. The present invention provides crystals of (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidine-1-yl)-1-pyrrolidinyl)-2-propene-1-one exhibiting at least three characteristic peaks for which the diffraction angle (2θ±0.2°) in the X-ray powder diffraction spectrum is selected from 9.5°, 14.3°, 16.7°, 19.1°, 20.8°, 21.9°, and 25.2°. The present invention also provides crystals of (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidine-1-yl)-1-pyrrolidinyl)-2-propene-1-one which are crystals exhibiting at least seven characteristic peaks for which the diffraction angle (2θ±0.2°) in the X-ray powder diffraction spectrum is selected from 13.5°, 17.9°, 19.5°, 20.6°, 22.0°, 22.6°, 23.3°, 23.7°, and 24.2°.
Inventors:
EGAMI KOSUKE (JP)
Application Number:
PCT/JP2016/060844
Publication Date:
October 06, 2016
Filing Date:
March 31, 2016
Export Citation:
Assignee:
TAIHO PHARMACEUTICAL CO LTD (JP)
International Classes:
C07D487/04; A61K31/519; A61P35/00; A61P43/00; C30B29/58
Domestic Patent References:
| WO2015008839A1 | 2015-01-22 | |||
| WO2013108809A1 | 2013-07-25 | |||
| WO2015008844A1 | 2015-01-22 |
Other References:
MITSURU HASHIDA: "Keiko Toyo Seizai no Sekkei to Hyoka", KABUSHIKI KAISHA YAKUGYO JIHOSHA, 10 February 1995 (1995-02-10), pages 76 - 79 , 171 to 172, XP009506428
YUKI KAGOBUTSU KESSHO SAKUSEI HANDBOOK -GENRI TO KNOW-HOW, 25 July 2008 (2008-07-25), pages 57 - 84, XP008183996
BYRN,STEPHEN ET AL.: "Pharmaceutical Solids: A Strategic Approach to Regulatory Considerations", PHARMACEUTICAL RESEARCH, vol. 12, no. 7, 1995, pages 945 - 954, XP000996386
BAVIN,MIKE: "Polymorphism in Process Development", CHEMISTRY & INDUSTRY, 1989, pages 527 - 529, XP001180136
YUKI KAGOBUTSU KESSHO SAKUSEI HANDBOOK -GENRI TO KNOW-HOW, 25 July 2008 (2008-07-25), pages 57 - 84, XP008183996
BYRN,STEPHEN ET AL.: "Pharmaceutical Solids: A Strategic Approach to Regulatory Considerations", PHARMACEUTICAL RESEARCH, vol. 12, no. 7, 1995, pages 945 - 954, XP000996386
BAVIN,MIKE: "Polymorphism in Process Development", CHEMISTRY & INDUSTRY, 1989, pages 527 - 529, XP001180136
Attorney, Agent or Firm:
SAEGUSA & PARTNERS (JP)
Patent business corporation 3 Edakuni [Hajime] patent firm (JP)
Patent business corporation 3 Edakuni [Hajime] patent firm (JP)
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