发明公开
- 专利标题: AROMATIC AMINE AR AND BET TARGETING PROTEIN DEGRADATION CHIMERA COMPOUND AND USE
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申请号: EP20809358.3申请日: 2020-05-15
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公开(公告)号: EP3971176A1公开(公告)日: 2022-03-23
- 发明人: DU, Wu , LV, Haibin , LI, Haibo , QIN, Dekun , AI, Chaowu , LI, Yu , DUAN, Jingyi , TU, Zhilin , ZHANG, Chengzhi , CHEN, Yuanwei , LI, Xinghai
- 申请人: Hinova Pharmaceuticals Inc.
- 申请人地址: CN Chengdu, Sichuan 610041 No. 1 4th Floor RongYao Building A 5 Keyuan South Road High-Tech Zone
- 代理机构: Altmann Stößel Dick Patentanwälte PartG mbB
- 优先权: CN201910415060 20190517
- 国际公布: WO2020233512 20201126
- 主分类号: C07D401/04
- IPC分类号: C07D401/04 ; C07D307/52 ; C07D235/06 ; C07D207/16 ; A61K31/4025 ; A61P35/00
摘要:
An aromatic amine androgen receptor (AR) and BET targeting protein degradation chimera compound and its use. Specifically provided is a compound represented by formula I. Experimental results show that the compound can target and degrade both AR and BRD4, and down-regulate the expression of AR and BRD4 proteins; the compound can inhibit the proliferation of a variety of prostate cancer cells; the compound can inhibit the proliferation of a prostate cancer cell line LNCaP/AR, which overexpresses the AR, and can achieve a good inhibition effect on a prostate cancer cell line 22RV1, which is resistant to a marketed prostate cancer drug (enzalutamide); the compound also shows good metabolic stability, and has a good application prospect in the preparation of an AR and/or BET protein degradation targeting chimera, and a drug for the treatment of related diseases regulated by the AR and BET.
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