2-aminopyrimidine compound and pharmaceutical composition and use thereof

US10059694B2 · kind B2 · utility

Assignees

• SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES · CN
• Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences · CN

Inventors

• Ke Ding · 流花街道, CN
• Jian Ding · Shanghai, CN
• Shingpan CHAN · 流花街道, CN
• Meiyu Geng · Shanghai, CN
• Xiaomei REN · Tangxia, CN
• Hua Xie · Shanghai, CN
• Zhengchao Tu · 流花街道, CN
• Yi Chen · Shanghai, CN

Key dates

• Filing date: Nov 18, 2015
• Grant date: Aug 28, 2018
• Expiry date: Nov 18, 2035

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D401/12
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Disclosed are a 2-aminopyrimidine compound and pharmaceutical composition and use thereof. The structure of the 2-aminopyrimidine compound is as represented by formula I, in the formula, R1, R2, R3, R4, R5, X, Y, Z, W, (i) being as defined in the specification and the claims. Such compounds effectively inhibit the growth of a variety of tumor cells and have inhibitory effects on EGFR and IGF1R protease, and can be used for preparing antineoplastic drugs and overcome the tolerance induced by the existing drugs such as gefitinib, erlotinib and the like. The compound has selectivity for tumors, in particular the wild-type non-small cell lung cancer and have good pharmacokinetic characteristics.