PYRIMIDINE OR PYRIDINE COMPOUNDS, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USES THEREOF
申请人:Shanghai Shaletech Technology Co., Ltd.
公开号:EP3216786A1
公开(公告)日:2017-09-13
The present invention disclosed a class of pyrimidine or pyridine compounds, pharmaceutically acceptable salts, stereoisomers, prodrugs and solvates thereof, preparation method therefor and pharmaceutical compositions and pharmaceutical uses thereof. The compounds can inhibit the variants of EGFR (Epidermis Growth Factor Receptor) proteinases, and therefore can inhibit the growth of a variety of tumor cells effectively. The compounds can be used to prepare antitumor drugs, used for the treatment, combined therapy or prevention of various different cancers. The compounds can overcome the drug resistance induced by the existing first-generation EGFR inhibitors such as gefitinib, erlotinib and so on. Particularly, the compounds can be used to prepare drugs for treating or preventing diseases, disturbances, disorders or conditions mediated by epidermis growth factor receptor variants (such as L858R activated mutants, Exon19 deletion activated mutants and T790M resistant mutants).
本发明公开了一类嘧啶或吡啶化合物、其药学上可接受的盐、立体异构体、原药和溶液、其制备方法和药物组合物及其药物用途。这些化合物可以抑制表皮生长因子受体蛋白酶的变体,从而有效抑制多种肿瘤细胞的生长。这些化合物可用于制备抗肿瘤药物,用于治疗、联合治疗或预防各种不同的癌症。这些化合物可以克服现有的第一代表皮生长因子受体抑制剂(如吉非替尼、厄洛替尼等)引起的耐药性。特别是,这些化合物可用于制备治疗或预防由表皮生长因子受体变体(如 L858R 激活突变体、Exon19 缺失激活突变体和 T790M 耐药突变体)介导的疾病、紊乱、失调或病症的药物。