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：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.

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：US20220062316A1

公开(公告)日：2022-03-03

申请号：US16976765

申请日：2019-11-04

申请人： ZHEJIANG UNIVERSITY

发明人： Bo YANG ,  Qiaojun HE ,  Ling DING

IPC分类号： A61K31/7042 ,  A61P35/00

摘要： The present invention provides a use of canagliflozin in preparation of an antitumor drug, especially in preparation of a drug for treating solid tumors. It has been proven through researches that canagliflozin has a significant down-regulation effect on immune checkpoint protein PD-L1 in various tumor cells and can effectively enhance the killing effect of T cells on tumor cells in a co-incubation model of T cells and tumor cells, thereby broadening a clinical application scope of the chemical drug canagliflozin in tumor immunotherapy. The present invention provides a new medical use of canagliflozin, and also provides new approaches and potential targets for the development of small molecular drugs based on PD-L1.

公开(公告)号：US20210330659A1

公开(公告)日：2021-10-28

申请号：US16612770

申请日：2018-10-31

申请人： ZHEJIANG UNIVERSITY

发明人： Qiaojun HE ,  Bo YANG ,  Peihua LUO

IPC分类号： A61K31/455 ,  A61K31/44 ,  A61P17/00

摘要： The present disclosure provides a use of a nicotinamide composition in preparation of a drug for treating hand-foot skin reaction (HFSR) induced by sorafenib, the composition being consisted of nicotinamide and sorafenib in a dosage ratio of 2:3. The composition provided by the present disclosure can alleviate the HFSR caused by excessive keratinization induced by sorafenib. This protective effect is achieved by inhibiting HB-EGF/SIRT1 pathway. The present disclosure provides a mechanism of sorafenib-induced HFSR, i.e., the excessive activation of the HB-EGF/SIRT1 pathway, thereby providing a theoretical foundation for clinical research of sorafenib-induced HFSR. The present disclosure also provides a drug that can effectively treat sorafenib-induced HFSR, thereby greatly broadening the clinical application of sorafenib. Nicotinamide is highly clinically feasible due to its moderate price, and thus can be prepared in any suitable formulation according to the requirements.