Pyrrolo [2, 3-d] pyrimidine derivative targeting EGFR mutation as well as preparation method and application of pyrrolo [2, 3-d] pyrimidine derivative

A use and drug technology, applied in the field of pyrrolo[2,3-d]pyrimidine derivatives and their preparation, can solve problems such as the occurrence of osimertinib resistance, achieve good application prospects, significant inhibitory effect, and good inhibitory effect Active and Selective Effects
CN111848631AActive Publication Date: 2020-10-30WEST CHINA HOSPITAL SICHUAN UNIV +1
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
WEST CHINA HOSPITAL SICHUAN UNIV
Publication Date
2020-10-30

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Abstract

The invention provides a pyrrolo [2, 3-d] pyrimidine derivative targeting EGFR mutation as well as a preparation method and application thereof, and belongs to the field of chemical medicines. The derivative is a compound shown as a formula I, or a salt thereof, or a stereoisomer thereof. The compound disclosed by the invention is low in toxicity to normal cells, has an obvious inhibition effect on a lung cancer cell line, particularly has good selectivity on EGFR mutant cells HCC827, and has an obvious inhibition effect; meanwhile, the compound provided by the invention can effectively inhibit phosphorylation of EGFR. In addition, the compound provided by the invention has good inhibitory activity and selectivity on mutant EGFR. The compound disclosed by the invention can be used for treating lung cancer, particularly non-small cell lung cancer, has a relatively strong inhibition effect on EGFR mutant lung cancer, and is relatively low in toxicity; the compound can also be used for preparing tyrosine kinase inhibitors, especially EGFR phosphorylation inhibitors, and has good application prospects.
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Description

technical field

[0001] The invention belongs to the field of chemical medicine, and specifically relates to a pyrrolo[2,3-d]pyrimidine derivative targeting EGFR mutation, a preparation method and application thereof. Background technique

[0002] Lung cancer is the malignant tumor with the highest morbidity and mortality worldwide, and the number of deaths due to lung cancer reaches 1.6 million each year. It is the main cause of cancer-related deaths in men (22% of cancer deaths) and women (13.8% of cancer deaths) reason. In the United States, about 14 percent of new cancers are lung cancers. The American Cancer Society estimates there were approximately 234,000 lung cancer cases and 154,000 deaths in the United States in 2018. The situation in my country is equally serious. According to the latest cancer data in China released by the National Cancer Center in January 2019, lung cancer is the malignant tumor with the highest morbidity and mortality in my country. Come unde...

Claims

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