Wuxi Shuangliang Biotechnology Co., Ltd.

Shenshuang Jin

Jiaquan Wu

Li Li

Huanyan Cao

Ping Zhou

Shuai Zhang

Jian Dong

Chengchen Wang

Zhenghua Lu

Qiu Tan

Haijun Zhang

Provided in the present disclosure 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 EGFR inhibitor of the present disclosure has a specific crystal form, has a higher solubility and stability than a corresponding free base, is more suitable for preparing drugs for use in treating cancer (especially non-small cell lung cancer), and satisfies the requirements for bioavailability and drug efficacy. 

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

The present disclosure relates to 2-arylamino pyridine, pyrimidine, or triazine derivatives, and the preparation method and use thereof. The 2-arylamino pyridine, pyrimidine, or triazine derivatives may act on certain mutated forms of epidermal growth factor receptor, for example the L858R activating mutant, the delE746_A750 mutant, the Exonl9 deletion activating mutant, and the T790M resistance mutant, so as to be used for treatment and prevention of diseases and medical conditions. The 2-arylamino pyridine, pyrimidine, or triazine derivatives may be used for treatment and prevention of cancer. The present disclosure also relates to a pharmaceutical composition comprising 2-arylamino pyridine, pyrimidine, or triazine derivatives, intermediates useful in the manufacture of 2-arylamino pyridine, pyrimidine, or triazine derivatives, and to methods of treatment of diseases mediated by various different forms of EGFR using 2-arylamino pyridine, pyrimidine, or triazine derivatives.

2-arylamino pyridine, pyrimidine or triazine derivatives, preparation method and use thereof

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Jiangsu, China

Shenshuang Jin