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公开(公告)号:EP3411074A2
公开(公告)日:2018-12-12
申请号:EP16715987.0
申请日:2016-02-04
发明人: ZHAO, Robert Yongxin , YANG, Qingliang , HUANG, Yuanyuan , GAI, Shun , ZHAO, Linyao , YE, Hangbo , GUO, Huihui , TONG, qianqian , CAO, Minjun , JIA, Junxiang , YANG, Chengyu , LI, Wenjun , ZHOU, Xiaomai , XIE, Hongsheng , LIN, Chen , GUO, Zhixiang , YE, Zhicang
IPC分类号: A61K47/48 , C07D417/14 , C07D339/00 , A61P31/00 , A61P35/00 , A61P37/00
CPC分类号: A61K49/0058 , A61K47/6803 , A61K47/6809 , A61K47/6817 , A61K47/6829 , A61K47/6889 , A61K49/0021 , A61K49/0032 , A61K49/0043 , C07D207/08 , C07D277/56 , C07D417/12 , C07D417/14 , C07D498/18 , C07D513/22 , C07D519/00
摘要: The present invention relates to novel linkers containing a 2,3-disubstituted succinic group, or 2-monosubstituted, or 2,3-disubstituted fumaric or maleic (trans (E)- or cis (Z)- butenedioic), or acetylenedicarboxyl group for conjugation of a cytotoxic agent, and/or one or more different functional molecules per linker to a cell-binding molecule, through bridge linking pairs of thiols on the cell-binding molecule specifically. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.
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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: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:EP4426727A2
公开(公告)日:2024-09-11
申请号:EP21879565.6
申请日:2021-11-03
发明人: ZHAO, Robert , YANG, Qingliang , LIU, Xiaolei , ZHANG, Lingli , HUANG, Yuanyuan , LI, Wenjun , YE, Hangbo , WANG, Juan , GUO, Huihui , ZHOU, You
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:EP3606922A1
公开(公告)日:2020-02-12
申请号:EP17904588.5
申请日:2017-04-06
发明人: ZHAO, Robert Yongxin , HUANG, Yuanyuan , YANG, Qingliang , GAI, Shun , YE, Hangbo , ZHAO, Linyao , YANG, Chengyu , XU, Yifang , GUO, Huihui , CHAO, Minjun , TONG, Qianqian , LI, Wenjun , CAI, Xiang , ZHOU, Xiaomai , XIE, Hongsheng , JIA, Junxiang , ZHU, Haifeng , GUO, Zhixiang , GAO, Shuihong , WANG, Chunyan , LIN, Chen , YANG, Yanlei , YE, Zhicang , PENG, Jie , XU, Jun , ZUO, Xiaotao , SU, Qingyu
IPC分类号: C07D417/14 , A61P31/00
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公开(公告)号:EP3912982A1
公开(公告)日:2021-11-24
申请号:EP21184933.6
申请日:2015-03-19
发明人: SUN, Sanxing , ZHAO, Robert Yongxin , LI, Xing , GUO, Huihui , JIA, Junxiang , XIE, Hongsheng , ZHOU, Xiaomai , HUANG, Yuanyuan , YANG, Qingliang , ZHUO, Xiaotao , YE, Hangbo , GAI, Shun , QU, Lan , LI, Wenjun , LIN, Chen
IPC分类号: C07F9/6558 , C07F9/572 , C07D207/46
摘要: The present invention provides hydrophilic linkers that are useful for linking drugs to cell-binding ligands in ligand-drug conjugates, such as antibody-drug conjugates. The ligand-drug conjugate comprises a cell-binding ligand capable of binding to a particular cell population, and a drug connected to the ligand by a hydrophilic linker. The hydrophilic linker comprises one or more hydrophilic groups then render the linker hydrophilic. The hydrophilic linker may also comprise functional groups at the two termini for coupling to the drug and the cell-binding ligand respectively.
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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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