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Crystal of 3,5-disubstituted phenylalkynyl compounds
专利权人:
TAIHO PHARMACEUTICAL CO., LTD.;大鹏药品工业株式会社;大鵬藥品工業株式會社
发明人:
江上浩介,江上浩介
申请号:
MOJ004218
公开号:
MOJ004218B
申请日:
2020.06.11
申请国别(地区):
MO
年份:
2020
代理人:
摘要:
The purpose of the present invention is to provide a stable crystal of (s)} 1  ̄ (3  ̄ (4  ̄ amino  ̄ 3  ̄ o ((3,5  ̄ dimethoxyphenyl) ethynyl)} 1H  ̄ pyrazolo [3,4  ̄ D] pyrimidine  ̄ 1  ̄ YL)  ̄ 1  ̄ pyrrolidone  ̄ 2  ̄ propylene  ̄ 1  ̄ one, which can be used as an antitumor agent, has excellent oral absorption and high chemical purity, and is suitable for mass production.The invention provides a crystal crystal crystal of (s) s ponmatter-1 ponone (3 process (4-amino-acid-3-one) (3-step-5-step-dimethoxyphenyl) 3-step-1h-pyrazo [3,4-d-d] pyrimidi [3,4-d] pyrimidi [3,4-d] pyrimidi [3,4-d] pyrimidi [1-1-yl] pyrimidi [3-4-4-d] pyrimidi [1-1-yl] 1-one, the crystal of the crystal of (s) 1-1-one of (3-step-1-1-step-1-1-one, the invention provides the crystal of the crystal of the (s) of the X-ray powder powder diffraction spectrum of the X-ray powder powder diffraction spectrum, the diffraction angle (2 θ ± 0.2 ° there were at least three characteristic peaks of 8 °, 21.9 ° and 25.2 °.The invention also provides (s)  ̄ 1  ̄ (3  ̄ (4  ̄ amino  ̄ 3  ̄ (3,5  ̄ dimethoxyphenyl) ethynyl)} 1H  ̄ pyrazolo [3], The crystal of 4  ̄ D] pyrimidine  ̄ 1  ̄ YL)  ̄ 1  ̄ pyrrolidine  ̄ 2  ̄ propylene  ̄ 1  ̄ one is a crystal exhibiting at least seven characteristic peaks (2 θ ± 0.2 ° selected from 13.5 °, 17.9 °, 19.5?, 20.6?, 22.0?, 22.6?, 23.3?, 23.7?, and 24.2?, respectively.本發明的目的是提供(S)‑1‑(3‑(4‑氨基‑3‑((3,5‑二甲氧基苯基)乙炔基)‑1H‑吡唑并[3,4‑d]嘧啶‑1‑基)‑1‑吡咯烷基)‑2‑丙烯‑1‑酮的穩定晶體,其可用作抗腫瘤藥劑,具有優異的口服吸收性和高化學純度,該晶體適合於大量製造。本發明提供(S)‑1‑(3‑(4‑氨基‑3‑((3,5‑二甲氧基苯基)乙炔基)‑1H‑吡唑并[3,4‑d]嘧啶‑1‑基)‑1‑吡咯烷基)‑2‑丙烯‑1‑酮的晶體,其表現出在X‑射線粉末衍射光譜中衍射角(2θ±0.2°)選自9.5°、14.3°、16.7°、19.1°、20.8°、21.9°和25.2°的至少3個特徵峰。本發明還提供(S)‑1‑(3‑(4‑氨基‑3‑((3,5‑二甲氧基苯基)乙炔基)‑1H‑吡唑并[3,4‑d]嘧啶‑1‑基)‑1‑吡咯烷基)‑2‑丙烯‑1‑酮的晶體,其是表現出在X‑射線粉末衍射光譜中衍射角(2θ±0.2°)選自13.5°、17.9°、19.5°、20.6°、22.0°、22.6°、23.3°、23.7°和24.2°的至少7個特徵峰的晶體。
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中国工程科技知识中心
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