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Pharmaceutically acceptable salt of EGFR inhibitor, crystal form thereof, preparation method therefor and application thereof

机译:EGFR抑制剂的药学上可接受的盐,其晶型,其制备方法和应用

摘要

Provided in the present invention are a pharmaceutically acceptable salt of an epidermal growth factor receptor (EGFR) inhibitor, a crystal form thereof, a preparation method therefor and an application thereof. The structural formula of the EGFR inhibitor is as shown in formula I, and the pharmaceutically acceptable salt is a mesylate, p-toluenesulfonate, phosphate, hydrochloride or citrate salt of the EGFR inhibitor. The pharmaceutically acceptable salt of the EGFR inhibitor of the present invention has a specific crystal form, is more soluble and stable than a corresponding free base, is more suitable for preparing medicine for use in treating cancer (especially non-small cell lung cancer), and satisfies the requirements for bioavailability and efficacy.
机译:本发明提供了表皮生长因子受体(EGFR)抑制剂的药学上可接受的盐,其晶形,其制备方法及其应用。 EGFR抑制剂的结构式如式I所示,并且药学上可接受的盐是EGFR抑制剂的甲磺酸盐,对甲苯磺酸盐,磷酸盐,盐酸盐或柠檬酸盐。本发明的EGFR抑制剂的药学上可接受的盐具有特定的晶型,比相应的游离碱更易溶和稳定,更适合于制备用于治疗癌症(特别是非小细胞肺癌)的药物,并满足生物利用度和功效的要求。

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