Substituted piperidin derivative, and pharmaceutical composition containing substituted piperidin derivative and application thereof in antitumor

By developing substituted piperidine derivatives that bind to Akt protein kinase B and inhibit its activity, the problems of high toxicity and drug resistance of existing anti-tumor drugs have been solved, providing a highly effective anti-tumor treatment option.

CN104926788AInactive Publication Date: 2015-09-23ZHEJIANG UNIV +1
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Patent Information

Application Number
CN201510101220.8
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Priority Date
2014-03-22
Filing Date
2015-03-08
Publication Date
2015-09-23
Estimated Expiration
Not applicable · inactive patent

AI Technical Summary

Technical Problem

Existing anti-tumor drugs have problems such as significant toxic side effects and easy development of drug resistance. There is a need to develop new, highly effective, and low-toxicity anti-tumor drugs, especially inhibitors of Akt, to improve the effectiveness of tumor treatment.

Method used

A series of substituted piperidine derivatives and their optical isomers or pharmaceutically acceptable salts or solvates were developed to inhibit cell proliferation by binding to Akt protein kinase B and inhibiting its activity.

Benefits of technology

These compounds exhibit significant Akt inhibition and potent anti-proliferative effects against human ovarian cancer cells and colon cancer cell lines, providing a novel anti-tumor treatment strategy.

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Abstract

The invention discloses a novel substituted piperidin derivative used as an Akt inhibitor. The derivative is a compound as shown in a formula I, and an optical isomer thereof or pharmaceutically-acceptable salt or a polymer solvent thereof, wherein ring A and R1, R2, R3, R4 and R5 are defined in the specification. Moreover, the invention also discloses a drug with the substituted piperidin derivative in the invention as an active ingredient, and the drug can be applied in treating hyperplasia diseases like cancer and inflammatory diseases, and specifically diseases associated with Akt kinase.
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