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公开(公告)号：EP4426729A1
公开(公告)日：2024-09-11
申请号：EP22889295.6
申请日：2022-11-02
发明人： ZHAO, Robert , YANG, Qingliang , YE, Hangbo , JIA, Junxiang , ZHANG, Lingli , HUANG, Yuanyuan , LI, Wenjun , WANG, Juan , GUO, Huihui , YE, Zhicang , ZHAO, Linyao , BAI, Lu , LIU, Xiaolei
IPC分类号： C07K16/00 , C07K16/28 , A61K39/395 , A61K47/68 , A61P35/00
CPC分类号： A61K47/6867 , A61K47/68037
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公开(公告)号：EP4168009A1
公开(公告)日：2023-04-26
申请号：EP20932660.2
申请日：2020-06-19
发明人： ZHAO, Robert , YANG, Qingliang , YE, Hangbo , HUANG, Yuanyuan , XU, Yifang , ZHAO, Gengxiang , CHEN, Diancheng , GUO, Huihui , KONG, Xiangfei , LI, Wenjun , BAI, Lu , CAI, Xiang , ZHANG, Xiuzhen , JIA, Junxiang , GUO, Zhixiang , HUANG, Shangma , WANG, Xiaoxu , ZHENG, Jun , DU, Yong , LI, Yanhua , ZHENG, Yunxia , LIN, Chen , CHEN, Xiaoxiao , ZHENG, Wei , JIANG, Xinyan , ZHANG, Lingli , YE, Riping , CHEN, Miaomiao
IPC分类号： A61K31/4745 , C07K16/00 , C07D491/22 , A61K31/47 , A61K39/395 , A61P35/00
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公开(公告)号：EP3991752A1
公开(公告)日：2022-05-04
申请号：EP19936127.0
申请日：2019-06-29
发明人： ZHAO, Robert , YANG, Qingliang , ZHAO, Linyao , HUANG, Yuanyuan , YE, Hangbo , GAI, Shun , LAI, Juan , LI, Wenjun , BAI, Lu , CAO, Minjun
摘要： The present invention relates to the conjugates of Tubulysin derivatives (anologs) and cell-binding molecules using branched (side-chain) linkers, and the resulting conjugates have better pharmacokinetic properties, and thus can more accurately target and kill abnormal cells. The invention also relates to the conjugation methods of the Tubulysin derivatives (anologs) to cell-binding molecules, and methods for synthesizing the small molecules, and methods of using the conjugates for targeted therapy for cancers, infections and autoimmune diseases. The conjugates of Tubulysin derivatives with long branched linkers demonstrated increased half-life, minimal exposure to non-targeted cells, tissues or organs in system circulation, leading to reduced off-target toxicity.
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公开(公告)号：EP3986463A1
公开(公告)日：2022-04-27
申请号：EP19935314.5
申请日：2019-06-24
发明人： ZHAO, Robert Yongxin , YANG, Qingliang , ZHAO, Linyao , HUANG, Yuanyuan , YE, Hangbo , GAI, Shun , JIA, Junxiang , BAI, Lu , LI, Wenjun , GUO, Zhixiang , LIN, Chen , ZHENG, Jun , GUO, Huihui , CAO, Minjun , KONG, Xiangfei , DU, Yong , XU, Yifang , ZHOU, Xiaomai , XIE, Hongsheng , ZHANG, Xiuzhen , CHEN, Miaomiao , LIU, Xiaolei , CAI, Xiang , CHEN, Binbin , YANG, Yanlei , ZHANG, Lingli
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公开(公告)号：EP3917576A1
公开(公告)日：2021-12-08
申请号：EP19913293.7
申请日：2019-01-31
发明人： ZHAO, Robert Yongxin , YANG, Qingliang , LEI, Jun , HUANG, Yuanyuan , ZHAO, Linyao , YE, Hangbo , GAI, Shun , CAO, Mingjun , TONG, Qianqian , BAI, Lu , GUO, Zhixiang , YANG, Chengyu , ZHOU, Xiaomai , XIE, Hongsheng , XU, Yifang , GUO, Huihui , JIA, Junxiang , ZHENG, Jun , LIN, Cheng , ZHUO, Xiaotao , LI, Wenjun , DU, Yong , KONG, Xiangfei , CHEN, Binbin , YANG, Yanlei , TONG, Yanhong , CHEN, Xiaoxiao , LI, Yanhua , ZHANG, Xiuzheng , LAI, Juan
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公开(公告)号：EP3867250A1
公开(公告)日：2021-08-25
申请号：EP18936601.6
申请日：2018-10-12
发明人： ZHAO, Robert Yongxin , YANG, Qingliang , HUANG, Yuanyuan , ZHAO, Linyao , YE, Hangbo , ZHUO, Xiaotao , YANG, Chengyu , LEI, Jun , XU, Yifang , GUO, Huihui , LI, Wenjun , GAI, Shun , BAI, Lu , GUO, Zhixiang , JIA, Junxiang , ZHENG, Jun , ZHOU, Xiaomai , XIE, Hongsheng , TONG, Qianqian , CHAO, Mingjun , TONG, Yanhong , YE, Zhicang , LIN, Chen , YANG, Yanlei , CHEN, Binbin
IPC分类号： C07D417/14 , A61P31/00
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公开(公告)号：EP3986476A1
公开(公告)日：2022-04-27
申请号：EP20831886.5
申请日：2020-02-18
发明人： ZHAO, Robert , YANG, Qingliang , HUANG, Yuanyuan , GAI, Shun , YE, Hangbo , ZHAO, Linyao , GUO, Huihui , BAI, Lu , LI, Wenjun , JIA, Junxiang , GUO, Zhixiang , ZHENG, Jun , CHEN, Xiaoxiao , KONG, Xiangfei , LIN, Chen , DU, Yong , ZHANG, Yu , ZHOU, Lei , ZHANG, Xiuzhen , ZHENG, Xiuhong , CHEN, Binbin , YANG, Yanlei , DAI, Meng , XU, Yifang , FAN, Zhongliang , ZHOU, Xiaomai , JIANG, Xingyan , CHEN, Miaomiao , ZHANG, Lingli , LI, Yanhua
IPC分类号： A61K47/68 , A61K31/426 , A61K9/08 , C07D277/56 , A61P35/00
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公开(公告)号：EP3818062A1
公开(公告)日：2021-05-12
申请号：EP18925690.2
申请日：2018-07-05
发明人： ZHAO, Robert Yongxin , ZHUO, Xiaotao , YANG, Qingliang , ZHAO, Linyao , HUANG, Yuanyuan , YE, Hangbo , YANG, Chengyu , LEI, Jun , GAI, Shun , GUO, Huihui , JIA, Junxiang , BAI, Lu , XIE, Hongsheng , ZHOU, Xiaomai , GUO, Zhixiang , LI, Wenjun , CAO, Mingjun , ZHENG, Jun , YE, Zhichang , YANG, Yanlei
IPC分类号： C07D487/04 , A61K31/5517 , A61P35/00
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公开(公告)号：EP3888691A1
公开(公告)日：2021-10-06
申请号：EP21171676.6
申请日：2016-11-14
发明人： ZHAO, Yongxin Robert , YANG, Qingliang , HUANG, Yuanyuan , GAI, Shun , YE, Hangbo , ZHAO, Linyao , YANG, Chengyu , GUO, Huihui , ZHOU, Xiaomai , XIE, Hongsheng , ZHU, Haifeng , XU, Yifang , TONG, Qianqian , JIA, Junxiang , CAO, Minjun , LI, Wenjun , GAO, Shuihong , GUO, Zhixiang , BAI, Lu , LI, Chen , YANG, Yanlei , WANG, Chunyan , YE, Zhichang
摘要： The present invention relates to linkers having a group of propiolyl, substituted acryl (acryloyl), or disubstituted propanoyl, and using such linkers for the conjugation of compounds, in particular, cytotoxic agents to a cell-binding molecule.
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公开(公告)号：EP3621652A1
公开(公告)日：2020-03-18
申请号：EP17936036.7
申请日：2017-12-31
发明人： ZHAO, Robert Yongxin , YANG, Qingliang , HUANG, Yuanyuan , ZHAO, Linyao , GAI, Shun , YE, Hangbo , LEI, Jun , XU, Yifang , CAO, Mingjun , GUO, Huihui , JIA, Junxiang , TONG, Qianqian , LI, Wenjun , ZHOU, Xiaomai , XIE, Hongsheng , BAI, Lu , CAI, Xiang , ZHUO, Xiaotao , ZHANG, Xiuzheng , ZHENG, Jun
IPC分类号： A61K47/00
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