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1.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：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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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：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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