公开(公告)号：US20220017505A1

公开(公告)日：2022-01-20

申请号：US17358002

申请日：2021-06-25

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

发明人： Rong SHENG ,  Jia LI ,  Dongyan GU ,  Yubo ZHOU ,  Jun WEI ,  Mengmeng ZHANG ,  Yongzhou HU ,  Kaixiang ZHANG ,  Jieyu LIU ,  Weijuan KAN

IPC分类号： C07D413/14 ,  C07D403/12 ,  C07D471/04 ,  C07D239/95 ,  C07D417/12 ,  C07D473/00 ,  C07D401/14 ,  C07D491/107 ,  C07D491/056

摘要： Provided by the present disclosure are an amino quinazolinone and amino isoquinolone derivatives. It is verified by numerous experiments that the compounds provided by the present disclosure have good inhibiting effects on PI3Kα and PI3Kγ, most of the compounds have prominent inhibiting effect on PI3Kα, and show strong growth inhibiting effect on PIK3CA mutant tumor cells such as human breast cancer cell strain (MCF7). Therefore, the amino quinazolinone and amino isoquinolone derivatives according to the present disclosure can be applied in the preparation of anti-tumor and anti-inflammatory medicines, and can be used as PI3Kα inhibitors in the preparation of medicines for treatment of human or animal cell proliferation related tumors, the medicines comprising the derivatives any one or more of pharmaceutically acceptable salts and solvates thereof as well as pharmaceutically acceptable carriers. Formulas a and b are shown as below: