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EGFR抑制劑游離堿或其酸式鹽的多晶型、其製備方法和應用
专利权人:
JIANGSU HANSOH PHARMACEUTICAL GROUP CO., LTD.;SHANGHAI HANSOH BIOMEDICAL CO., LTD.
发明人:
CHEN, ZHONGKE,陈中科,陳中科,LIU, FUPING,刘福平,劉福平,LIU, LEI,刘磊,劉磊,BAO, RUDI,包如迪
申请号:
TW105144164
公开号:
TW201734006A
申请日:
2016.12.30
申请国别(地区):
TW
年份:
2017
代理人:
摘要:
The present invention discloses crystalline free bases of EGFR inhibitor or crystalline acid salts thereof, and preparation methods and uses thereof. In particular, the invention relates to the crystalline free bases of N-(5-((4-(1-cyclopropyl-1H-benzazole-3-yl)pyrimidine-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl) propylene acyl amides or crystalline acid salt thereof, and their preparation methods, and the use in the preparation of medicaments for inhibiting the activity of L858R EGFR mutant, T790M EGFR mutant and exon 19 deletion mutant activation to treat diseases which is mediated by EGFR mutant. It can be widely used in the prevention and treatment of cancer, especially non-small cell lung cancer and other related diseases, and it is expected to develop into a new generation of EGFR inhibitors.本發明公開了EGFR抑制劑游離堿或其酸式鹽的多晶型、其製備方法和應用。具體涉及N-(5-((4-(1-環丙基-1H-吲哚-3-基)嘧啶-2-基)氨基)-2-((2-(二甲氨基)乙基)(甲基)氨基)-4-甲氧苯基)丙烯醯基醯胺游離堿或其酸式鹽的多晶型和其製備方法,以及所述的多晶型在製備治療EGFR突變體活性介導疾病藥物中的應用,用於抑制L858R EGFR突變體、T790M EGFR突變體和外顯子19缺失啟動突變體等的活性,可廣泛應用於預防與治療癌症尤其是非小細胞肺癌等相關疾病,有望開發成新一代EGFR抑制劑。
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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