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专利概况
专利名称 Stable, not included in the solvate crystal form II [...], and manufacturing method thereof
申请号 JP2017553290 申请日
公开(公告)号 JP6457658B2 公开(公告)日 2015-08-05
申请(专利权)人 发明人 羅軍芝; 年静; 高思原
专利来源 国家知识产权局 转化方式
摘要

A stable apremilast (represented by formula I) crystal form II free of solvates, a preparation method therefor, a pharmaceutical composition and pharmaceutical uses thereof, as well as a mixed crystal of the crystal form II and a crystal form B and a preparation method therefor. The 2副0.2 of an X-ray powder diffraction (XRPD) pattern of the apremilast crystal form II has five characteristic absorption peaks : 11.2, 13.2, 13.5, 13.8, and 14.7; and a Differential Scanning Calorimetry (DSC) thermogram shows a single absorption peak at 150? 癈. The activity of the crystal form II is not lower than that of the crystal form B, and the thermodynamic stability of the crystal form II is superior to that of the crystal form B. The preparation methods are simple to operate, and a used crystal solvent is safe and is easy to be removed.

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