公开(公告)号：US10233180B2

公开(公告)日：2019-03-19

申请号：US15128298

申请日：2015-03-21

申请人： ZHEJIANG UNIVERSITY ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Xiaowu Dong ,  Jia Li ,  Bo Yang ,  Yongzhou Hu ,  Yubo Zhou ,  Qinjie Weng ,  Wenhu Zhan ,  Lei Xu ,  Tao Liu ,  Qiaojun He

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： 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.

公开(公告)号：US11319300B2

公开(公告)日：2022-05-03

申请号：US16480599

申请日：2018-01-19

申请人： ZHEJIANG UNIVERSITY

发明人： Xiaowu Dong ,  Bo Yang ,  Yongzhou Hu ,  Qiaojun He ,  Qinjie Weng ,  Wenhu Zhan ,  Tao Liu

IPC分类号： A61P35/00 ,  A61P35/04 ,  C07D401/12 ,  C07D403/12

摘要： A polyfluoro-substituted aromatic heterocyclic derivative having the structure as represented by formula I or formula I′, wherein at least one of R1 and R2 is 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.