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一種酪胺酸激酶抑制劑的二馬來酸鹽的第I型結晶及製備方法
专利权人:
JIANGSU HENGRUI MEDICINE CO.; LTD.
发明人:
SUN, PIAOYANG,孙飘扬,孫飄揚,WU, GUAILI,武乖利,YUAN, BO,袁博,CHEN, YONGJIANG,陈永江,陳永江
申请号:
TW102121870
公开号:
TWI597277B
申请日:
2013.06.20
申请国别(地区):
TW
年份:
2017
代理人:
摘要:
The present invention relates to the form I crystal of dimaleate salt, a kind of tyrosine kinase inhibitors, as well as a process for its preparation. Specifically, the invention relates to the preparation method and use of the form I crystal of (R,E)-N-(4-(3-chloro-4-((pyridin-2-yl)methoxy)-phenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-3-(1-methylpyr rolidin-2-yl)acrylamide dimaleate (hereinafter referred to as SHR1258 dimaleate). The method claimed for the preparation of form I crystal of SHR1258 dimaleate include crystallization of arbitrary crystal or amorphous SHR1258 dimaleate in single organic solvent or their mixed organic solvent. The form I crystal of SHR1258 dimaleate claimed herein can be better used in clinical treatment for its good crystal structure stability and chemical stability in addition to the low toxicity and residue of the crystallization solvents.本發明涉及一種酪胺酸激酶抑制劑的二馬來酸鹽的第I型結晶及製備方法。具體地,本發明涉及(R,E)-N-(4-(3-氯-4-(吡啶-2-基)甲氧基)-苯基胺基)-3-氰基-7-乙氧基喹啉-6-基)-3-(1-甲基吡咯啶-2-基)丙烯醯胺二馬來酸鹽(簡稱SHR1258二馬來酸鹽)第I型結晶及其製備方法和用途。所述製備方法包括將任意晶形或無定形的SHR1258二馬來酸鹽固體在單一的有機溶劑或者其混合有機溶劑中結晶得到SHR1258二馬來酸鹽第I型結晶。本發明所得到SHR1258二馬來酸鹽第I型結晶具備良好的晶形穩定性和化學穩定性,並且所用結晶溶劑低毒低殘留,可更好地用於臨床治療。
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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