4-substituted quinoline compounds and applications thereof

By designing and synthesizing new 4-substituted quinoline compounds, the problem of existing anti-tumor drugs' poor inhibitory effect on c-Met kinase has been solved, and effective inhibition of various cancers, especially lung cancer and colon cancer, has been achieved, providing new treatment strategies.

CN104086530AInactive Publication Date: 2014-10-08SHENYANG PHARMA UNIV
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Patent Information

Application Number
CN201410321292.9
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2014-07-07
Publication Date
2014-10-08
Estimated Expiration
Not applicable · inactive patent

AI Technical Summary

Technical Problem

Existing anti-tumor drugs are difficult to effectively inhibit the abnormal activation of c-Met kinase, which leads to tumor invasion and metastasis, and have limited therapeutic effects on various tumor types.

Method used

A series of new 4-substituted quinoline compounds were designed and synthesized. Through in vitro activity screening, it was found that these compounds have significant anti-tumor activity, especially strong inhibitory effects on c-Met kinase, and are used to prepare, treat and prevent various cancers. of drugs.

Benefits of technology

These quinoline compounds significantly inhibit the proliferation and survival of lung cancer, colon cancer and other cells, providing new targeted treatment strategies, especially showing strong effects in the treatment of lung cancer and colon cancer.

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Abstract

The invention relates to 4-substituted quinoline derivatives as shown in the general formula (I) as well as configurational isomers and pharmaceutically acceptable solvants or prodrugs of the 4-substituted quinoline derivatives. In the general formula (I), substituent groups A, R1 and R2 are defined as the specification. The invention also relates to an application of the compounds as shown in the general formula (I) in strong inhibition for c-Met kinase, an application of the compounds as well as pharmaceutically acceptable salts and hydrates of the compounds in preparation of drugs for treating diseases caused by abnormal high expression of c-Met kinase and particularly an application in preparation of drugs for treating and / or preventing cancer.
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