Chinese Academy of Sciences

Zhejiang University

Guangzhou Lixin Pharmaceutical Co., Ltd.

Wenhu Zhan

Bo Yang

Tao Liu

Yongzhou Hu

Qiaojun He

Xiaowu Dong

Qinjie Weng

Jia Tao Li

Lei Xu

Yubo Zhou

A polyfluoro-substituted aromatic heterocyclic derivative having the structure as represented by formula I or formula I', wherein at least one of Rand Ris a fluorine atom, and at least two substituents of Rc, Rd, Re, and Rf are fluorine atoms; and an optical isomer of the derivative, or a pharmaceutically acceptable salt or solvate of the same, or a pharmaceutically acceptable salt or solvate of the optical isomer of the same. A composition containing the polyfluoro-substituted aromatic heterocyclic derivative and an application of the composition in preparing an anti-tumour medicament. The compound provides significant inhibitory effects with respect to Akt1 and demonstrates strong proliferation inhibitory activity with respect to tumour cell lines such as an ovarian cancer cell line, a colon cancer cell line, and a prostate cancer cell line. Therefore, the compound may be used as an Akt inhibitor in the medicament for treating a cell proliferation-related solid tumour or blood cancer in the human or animal body.

Polyfluoro-substituted aromatic heterocyclic derivative, pharmaceutical composition containing same, and applications thereof

Disclosed are new substituted nitrogen-containing heterocyclic derivatives represented by formula (I) as AKT inhibitors, optical isomers, pharmaceutically acceptable salts or solvates thereof, wherein the definition of R1, R2, R3, R4, R5, R6, ring A, ring C, B, Q, Y, Z and m is shown in the description for details. In addition, medicaments comprising the derivatives as active components are also disclosed, which can be useful for treating proliferative diseases, such as cancer and inflammation, especially diseases relating to AKT kinase.

Substituted nitrogen-containing heterocyclic derivatives, pharmaceutical compositions comprising the same and applications of antitumor thereof

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New York, NY, United States of America

Wenhu Zhan