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:

公开(公告)号：US20170107213A1

公开(公告)日：2017-04-20

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： C07D417/14 ,  C07D401/12 ,  C07D409/14 ,  C07D413/14 ,  C07D405/14 ,  C07D401/14

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

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：US20170022250A1

公开(公告)日：2017-01-26

申请号：US15301081

申请日：2015-03-11

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

发明人： Yongzhou HU ,  Jia LI ,  Tao LIU ,  Jiankang ZHANG ,  Yubo ZHOU ,  Bo YANG ,  Qiaojun HE ,  Lei XU ,  Xiaobei HU

IPC分类号： C07K5/087 ,  C07K5/083

CPC分类号： C07K5/0812 ,  A61K38/00 ,  C07K5/06043 ,  C07K5/06121 ,  C07K5/0808 ,  Y02P20/55

摘要： Disclosed are a tripeptide epoxyketone compound, a preparation method thereof, and a use thereof in the preparation of anti-tumor drugs.

摘要翻译： 公开了三肽环氧酮化合物及其制备方法及其在制备抗肿瘤药物中的用途。

公开(公告)号：US20200165229A1

公开(公告)日：2020-05-28

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： C07D403/12 ,  C07D401/12 ,  A61P35/04

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