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公开(公告)号:EP3683214A1
公开(公告)日:2020-07-22
申请号:EP18855304.4
申请日:2018-09-14
发明人: FAN, Lei , XU, Kexin , CHEN, Ke , WANG, Fei , WU, Xiaoquan , LUO, Tongchuan , ZHANG, Shaohua , LI, Xinghai , CHEN, Yuanwei
IPC分类号: C07D401/14 , C07D239/91 , A61K31/517 , A61K31/553 , A61K31/555 , A61P35/00 , A61P29/00
摘要: Disclosed is a BRD4 inhibitor as shown in formula I, belonging to the field of compound drugs. The compound provided has a good inhibitory effect on prostate cancer cell proliferation, and can be used for preparing a drug combatting tumors, autoimmune or inflammatory diseases and viral infection, and in particular an anti-prostate cancer drug.
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公开(公告)号:EP4043458A1
公开(公告)日:2022-08-17
申请号:EP20868375.5
申请日:2020-09-25
发明人: FAN, Lei , WANG, Fei , WU, Xiaoquan , XU, Kexin , LUO, Tongchuan , ZHANG, Shaohua , HUO, Yongxu , LI, Xinghai , CHEN, Yuanwei
IPC分类号: C07D413/14 , C07D471/04 , A61K31/422 , A61P35/00
摘要: An EP300/CBP inhibitor; specifically provided is a compound as shown in formula I, or a deuterated product thereof, or a salt thereof, or a conformational isomer thereof, or a crystal form thereof, or a solvate thereof. The compound is highly selective for EP300/CBP, and can effectively inhibit the activity of EP300/CBP; in addition, the compound has an excellent inhibitory effect on various tumor cells including prostate cancer cells, leukemia cells, breast cancer cells and multiple myeloma cells. The compound has broad application prospects in the preparation of an EP300/CBP inhibitor, and drugs for preventing and/or treating tumors, myeloid hematopoietic stem/progenitor cells malignant disease, and regulating regulatory T cells.
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公开(公告)号:EP3889138A1
公开(公告)日:2021-10-06
申请号:EP19888999.0
申请日:2019-11-27
发明人: FAN, Lei , WANG, Fei , WU, Xiaoquan , XU, Kexin , CHEN, Ke , LUO, Tongchuan , ZHANG, Shaohua , DU, Wu , ZHANG, Chengzhi , HUO, Yongxu , TU, Zhilin , LI, Xinghai , CHEN, Yuanwei
IPC分类号: C07D235/02 , C07D263/52 , C07D269/02 , C07D277/60 , C07D283/02 , A61P35/00 , A61K31/381 , A61K31/4184 , A61K31/428
摘要: Provided are a histone acetylase p300 inhibitor and a use thereof, belonging to the filed of medicinal chemistry technology. A compound represented by formula (I), or a stereochemical isomer thereof, or a solvate thereof, or a pharmaceutically acceptable salt thereof, can inhibit the activity of histone acetylase p300 and inhibit the proliferation activity of a variety of tumor cells.
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公开(公告)号:EP4368614A1
公开(公告)日:2024-05-15
申请号:EP22836982.3
申请日:2022-07-06
发明人: FAN, Lei , YU, Hua , WANG, Fei , AI, Chaowu , XU, Kexin , LIU, Xingtai , DU, Jing , PENG, Ying , LUO, Tongchuan , PENG, Shiming , TAN, Bin , XIAO, Daibiao , HUO, Yongxu , LIU, Chengcheng , LI, Xinghai , CHEN, Yuanwei
IPC分类号: C07D239/48 , C07D241/26 , C07D249/14 , A61P35/00
CPC分类号: A61K31/497 , A61K31/501 , A61K31/506 , A61K31/517 , A61K31/55 , A61K38/05 , A61P35/00 , A61P35/02 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/107 , C07D519/00 , C07K5/06017 , C07D249/14 , C07D239/48 , C07D241/26
摘要: A synthesis and an application of a phosphatase degrader, belonging to the field of chemical medicine. The phosphatase degrader is a compound represented by formula I, or a salt thereof, or a deuterated compound thereof, or a stereoisomer thereof, or a solvate thereof, or a hydrate thereof, or a prodrug thereof. The compound can be used as a phosphatase degrader, especially as an SHP2 protein degrader, can treat malignant diseases such as tumors, and has good application prospects.
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公开(公告)号:EP3831828A1
公开(公告)日:2021-06-09
申请号:EP19840292.7
申请日:2019-07-25
发明人: FAN, Lei , WANG, Fei , WU, Xiaoquan , XU, Kexin , CHEN, Ke , LUO, Tongchuan , ZHANG, Shaohua , HUO, Yongxu , TU, Zhilin , LI, Xinghai , CHEN, Yuanwei
IPC分类号: C07D471/04 , C07D487/04 , A61K31/407 , A61P35/00 , A61P31/18
摘要: Provided area compound as depicted in formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof; Experimental results show that the compound provided has a good inhibitory effect on the proliferation of human prostate cancer cells CWR22RV1 and breast cancer cells; and combined use of the compound with an androgen receptor inhibitor HC-1119 significantly enhances the inhibitory effect on prostate cancer cells, and the inhibitory effect increases with increased concentration. The compound provided by the present specification can not only be used independently to prepare an antineoplastic agent, but can also be used in combination with other agents having antineoplastic effects, such as an androgen receptor inhibitor, or other targeting drugs etc., to prepare an antineoplastic agent having stronger therapeutic effects, especially an agent for treating prostate cancer and breast cancer.
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