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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：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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