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公开(公告)号：US11129910B2
公开(公告)日：2021-09-28
申请号：US16074981
申请日：2016-02-04
发明人： Robert Yongxin Zhao , Qingliang Yang , Yuanyuan Huang , Shun Gai , Linyao Zhao , Hangbo Ye , Huihui Guo , Qianqian Tong , Minjun Cao , Junxiang Jia , Chengyu Yang , Wenjun Li , Xiaomai Zhou , Hongsheng Xie , Chen Lin , Zhixiang Guo , Zhicang Ye
IPC分类号： A61B5/00 , A61B8/00 , A61B10/00 , A61K49/00 , A61K47/68 , C07D417/12 , C07D417/14 , C07D498/18 , C07D513/22 , C07D519/00 , A61K45/06 , A61K31/194
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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2.发明申请公开(公告)号：US20200215206A1
公开(公告)日：2020-07-09
申请号：US16074981
申请日：2016-02-04
发明人： Robert Yongxin Zhao , Qingliang Yang , Yuanyuan Huang , Shun Gai , Linyao Zhao , Hangbo Ye , Huihui Guo , Qianqian Tong , Minjun Cao , Junxiang Jia , Chengyu Yang , Wenjun Li , Xiaomai Zhou , Hongsheng Xie , Chen Lin , Zhixiang Guo , Zhicang Ye
IPC分类号： A61K49/00 , A61K47/68 , C07D519/00 , C07D513/22 , C07D498/18 , C07D417/14 , C07D417/12
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：US11779663B2
公开(公告)日：2023-10-10
申请号：US17093184
申请日：2020-11-09
发明人： Robert Yongxin Zhao , Qingliang Yang , Yuanyuan Huang , Shun Gai , Linyao Zhao , Hangbo Ye , Huihui Guo , Qianqian Tong , Minjun Cao , Junxiang Jia , Chengyu Yang , Wenjun Li , Xiaomai Zhou , Hongsheng Xie , Chen Lin , Zhixiang Guo , Zhicang Ye
IPC分类号： A61B5/00 , A61B8/00 , A61B10/00 , A61K49/00 , A61K47/68 , C07D417/12 , C07D417/14 , C07D498/18 , C07D513/22 , C07D519/00 , A61K45/06 , A61K31/194
CPC分类号： A61K49/0058 , A61K47/6809 , A61K47/6829 , A61K47/6889 , A61K49/0032 , A61K49/0043 , C07D417/12 , C07D417/14 , C07D498/18 , C07D513/22 , C07D519/00 , A61K31/194 , A61K45/06
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：US10456479B2
公开(公告)日：2019-10-29
申请号：US15558917
申请日：2015-03-19
发明人： Sanxing Sun , Robert Yongxin Zhao , Xing Li , Huihui Guo , Junxiang Jia , Hongsheng Xie , Xiaomai Zhou , Yuanyuan Huang , Qingliang Yang , Xiaotao Zhuo , Hangbo Ye , Shun Gai , Lan Qu , Wenjun Li , Chen Lin
IPC分类号： A61K47/68 , C07D207/46 , C07F9/6558 , C07K16/00 , C07K16/28
摘要： Hydrophilic linkers are useful for linking drugs to cell-binding ligands in ligand-drug conjugates, such as antibody-drug conjugates. The ligand-drug conjugate includes 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 includes one or more hydrophilic groups that render the linker hydrophilic. The hydrophilic linker may also include 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：US11998584B2
公开(公告)日：2024-06-04
申请号：US16759175
申请日：2017-12-31
发明人： Robert Yongxin Zhao , Qingliang Yang , Yuanyuan Huang , Linyao Zhao , Shun Gai , Hangbo Ye , Jun Lei , Yifang Xu , Mingjun Cao , Huihui Guo , Junxiang Jia , Qianqian Tong , Wenjun Li , Xiaomai Zhou , Hongsheng Xie , Lu Bai , Xiang Cai , Xiaotao Zhuo , Xiuzheng Zhang , Jun Zheng
CPC分类号： A61K38/07 , A61K45/06 , C07K5/1024
摘要： The present invention relates to the conjugation of a tubulysin analog compound to a cell-binding molecule with branched/side-chain linkers for having better delivery of the conjugate compound and targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of a tubulysin analog molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and autoimmune disease.
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公开(公告)号：US20210308277A1
公开(公告)日：2021-10-07
申请号：US16348749
申请日：2016-11-14
发明人： Yongxin Robert Zhao , Qingliang Yang , Yuanyuan Huang , Shun Gai , Hangbo Ye , Linyao Zhao , Chengyu Yang , Huihui Guo , Xiaomai Zhou , Hongsheng Xie , Haifeng Zhu , Yifang Xu , Qianqian Tong , Junxiang Jia , Minjun Cao , Wenjun Li , Shuihong Gao , Zhixiang Guo , Lu Bai , Chen LI , Yanlei YANG , Chunyan WANG , Zhichang YE
IPC分类号： A61K47/68
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：US10646585B2
公开(公告)日：2020-05-12
申请号：US16226093
申请日：2018-12-19
发明人： Sanxing Sun , Robert Yongxin Zhao , Xing Li , Huihui Guo , Junxiang Jia , Hongsheng Xie , Xiaomai Zhou , Yuanyuan Huang , Qingliang Yang , Xiaotao Zhuo , Hangbo Ye , Shun Gai , Lan Qu , Wenjun Li , Chen Lin
IPC分类号： A61K47/68 , C07F9/572 , C07K16/28 , C07K16/00 , C07F9/6558 , C07D207/46 , C07K16/32 , A61K39/00
摘要： Hydrophilic linkers are useful for linking drugs to cell-binding ligands in ligand-drug conjugates, such as antibody-drug conjugates. The ligand-drug conjugate includes 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 includes one or more hydrophilic groups that render the linker hydrophilic. The hydrophilic linker may also include functional groups at the two termini for coupling to the drug and the cell-binding ligand respectively.
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