公开(公告)号：EP3530656A1

公开(公告)日：2019-08-28

申请号：EP17869906.2

申请日：2017-11-08

申请人： Zhejiang University ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： LIU, Tao ,  LI, Jia ,  HU, Yongzhou ,  ZHOU, Yubo ,  DONG, Xiaowu ,  GAO, Anhui ,  SONG, Pinrao ,  WANG, Peipei ,  TONG, Lexian ,  HU, Xiaobei ,  SU, Mingbo

IPC分类号： C07D401/14 ,  A61K31/506 ,  A61P35/00

摘要： A 2-substituted aromatic ring-pyrimidine derivative as shown in a general fomula I, and an optical isomer or a pharmaceutically acceptable salt or a solvate thereof are provided. The present invention designs and synthesizes a series of novel small molecular Chkl inhibitors by using N -substituted pyridin-2-aminopyrimidine obtained through structure-based virtual screening as a lead compound, and carries out Chkl kinase inhibitory activity test. The experiment confirmed that said compounds possess strong anti-cancer effect, Chkl kinase inhibitory activity and are promising Chkl inhibitors. The compounds can be used as new cancer therapeutic drugs, which can be applied to treat solid tumors or hematologic tumors related to proliferative disease of human or animal.

公开(公告)号：EP3530657A1

公开(公告)日：2019-08-28

申请号：EP17870509.1

申请日：2017-11-08

申请人： Zhejiang University ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： LIU, Tao ,  LI, Jia ,  HU, Yongzhou ,  ZHOU, Yubo ,  DONG, Xiaowu ,  GAO, Anhui ,  SONG, Pinrao ,  WANG, Peipei ,  TONG, Lexian ,  HU, Xiaobei ,  SU, Mingbo

IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D409/14 ,  C07D405/14 ,  A61K31/506 ,  A61P35/00

摘要： The present invention provides a 2-polysubstituted aromatic ring-pyrimidine derivative and an optical isomer thereof, or a pharmaceutically acceptable salt or solvate thereof, the compound, and an optical isomer thereof or a pharmaceutically thereof acceptable salts or solvates can be used in the preparation of anti-tumor drugs. The invention designs and synthesizes a series of novel small molecule Chkl inhibitors by using N-substituted pyridin-2-aminopyrimidine obtained by structure-based virtual screening as a lead compound, and carries out Chkl kinase inhibitory activity test. The experiment confirmed that said compounds possess potent anticancer activity, Chkl kinase inhibitory activity, and are promising Chkl inhibitors, and can be used as new cancer therapeutic drugs, which can be applied to treat solid tumors or hematologic tumors related to proliferative disease of human or animal. The 2-polysubstituted aromatic ring-pyrimidine derivatives provided by the present invention has the structure of the formula I: