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CRISTAL DEL COMPUESTO ALQUINIL BENCENO 3,5-DISUSTITUIDO.
专利权人:
TAIHO PHARMACEUTICAL CO.; LTD.
发明人:
EGAMI, Kosuke
申请号:
MX2017012568
公开号:
MX2017012568A
申请日:
2016.03.31
申请国别(地区):
MX
年份:
2018
代理人:
摘要:
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 (2?±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 (2?±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°.Un objetivo de la presente invención es proveer un cristal de (S)-1-(3-(4-amino-3-((3,5-dimetoxifenil)etinil)-1H-pirazolo[3,4-d ]pirimidin-1-il)-1-pirrolidinil)-2-propen-1-ona, el cual es útil como un agente antitumor, el cristal es estable, excelente en capacidad de absorción oral, muy puro químicamente, y adecuado para la producción en masa; la presente invención provee un cristal de (S)-1-(3-(4-amino-3-((3,5-dimetoxifenil)etinil)-1H-pira zolo[3,4-d]pirimidin-1-il)-1-pirrolidinil)-2-propen-1-ona que exhibe un espectro de difracción de rayos X de polvo que contiene al menos tres picos característicos a los ángulos de difracción (2?±0.2°) seleccionados de 9.5°, 14.3°, 16.7°, 19.1°, 20.8°, 21.9°, y 25.2°; la presente invención también provee un cristal de (S)-1-(3-(4-amino-3-((3,5-dimetoxifenil)etinil)-1H-pirazolo[3,4 -d]pirimidin-1-il)-1-pirrolidinil)-2-propen-1-ona que exhibe un espectr
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