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公开(公告)号：US20230115871A1
公开(公告)日：2023-04-13
申请号：US17622360
申请日：2019-06-24
发明人： Robert Yongxin ZHAO , Qingliang YANG , Linyao ZHAO , Yuanyuan HUANG , Hangbo YE , Shun GAI , Junxiang JIA , Lu BAI , Wenjun LI , Zhixiang GUO , Chen LIN , Jun ZHENG , Huihui GUO , Minjun CAO , Xiangfei KONG , Yong DU , Yifang XU , Xiaomai ZHOU , Hongsheng XIE , Xiuzhen ZHANG , Miaomiao CHEN , Xiaolei LIU , Xiang CAI , Binbin CHEN , Yanlei YANG , Lingli ZHANG
IPC分类号： A61K47/68
摘要： The present invention relates to the conjugation of cytotoxic drug to a cell-binding molecule with a side-chain linker. It provides side-chain linkage methods of making a conjugate of a cytotoxic molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and immunological disorders.
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公开(公告)号：US20230057350A1
公开(公告)日：2023-02-23
申请号：US17426813
申请日：2019-01-31
发明人： Robert Yongxin ZHAO , Qingliang YANG , Jun LEI , Yuanyuan HUANG , Linyao ZHAO , Hangbo YE , Shun GAI , Mingjun CAO , Qianqian TONG , Lu BAI , Zhixiang GUO , Chengyu YANG , Xiaomai ZHOU , Hongsheng XIE , Yifang XU , Huihui GUO , Junxiang JIA , Jun ZHENG , Cheng LIN , Xiaotao ZHUO , Wenjun LI , Yong DU , Xiangfei KONG , Binbin CHEN , Yanlei YANG , Yanhong TONG , Xiaoxiao CHEN , Yanhua LI , Xiuzheng ZHANG , Juan LAI
摘要： Provided herein is the conjugation of an amanita toxin compound to a cell-binding molecule with branched linkers for having better targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of an amanita molecule to a cell-binding ligand, as well as methods of using the conjugate in targets treatment of cancer, infection and autoimmune disease.
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公开(公告)号：US20220313836A1
公开(公告)日：2022-10-06
申请号：US17835081
申请日：2022-06-08
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：US20210353777A1
公开(公告)日：2021-11-18
申请号：US17373950
申请日：2021-07-13
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 , 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：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：US20210169896A1
公开(公告)日：2021-06-10
申请号：US17256034
申请日：2018-07-05
发明人： Robert Yongxin ZHAO , Xiaotao ZHUO , Qingliang YANG , Linyao ZHAO , Yuanyuan HUANG , Hangbo YE , Chengyu YANG , Jun LEI , Shun GAI , Huihui GUO , Junxiang JIA , Lu BAI , Hongsheng XIE , Xiaomai ZHOU , Zhixiang GUO , Wenjun LI , Mingjun CAO , Jun ZHENG , Zhicang YE , Yanlei YANG
IPC分类号： A61K31/5517 , C07D519/00 , A61K45/06 , A61K47/55 , A61K47/68 , A61K47/54 , A61P35/00
摘要： The present invention relates to novel cross-linked cytotoxic agents, pyrrolobenzodiazepine dimer (PBD) derivatives, and their conjugates to a cell-binding molecule, a method for preparation of the conjugates and the therapeutic use of the conjugates.
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公开(公告)号：US20200276261A1
公开(公告)日：2020-09-03
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
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：US10696699B2
公开(公告)日：2020-06-30
申请号：US16228130
申请日：2018-12-20
发明人： Robert Yongxin Zhao , Xing Li , Yuangyuang Huang , Qingliang Yang
IPC分类号： C07F9/58 , C07F9/30 , C07F9/572 , C07F9/6558 , C07F9/6561 , A61K47/68 , A61K38/07 , C07F9/32
摘要： Cell binding agent-drug conjugates comprising phosphinate-based charged linkers and methods of using such linkers and conjugates are provided.
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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：US20160207949A1
公开(公告)日：2016-07-21
申请号：US14914739
申请日：2013-09-02
发明人： Robert Yongxin Zhao
IPC分类号： C07F9/6561 , A61K47/48 , A61K45/06 , C07K16/28 , A61K31/675 , A61K39/395
CPC分类号： C07F9/6561 , A61K31/675 , A61K39/3955 , A61K45/06 , A61K47/55 , A61K47/6803 , A61K47/6849 , C07F9/5535 , C07F9/65583 , C07K16/2803 , C07K16/2887 , C07K2317/24 , C07K2317/54 , C07K2317/55 , C07K2317/622 , C07K2317/626 , C07K2317/76
摘要： The present invention is related to novel cytotoxic agents, pyrrolo[2,1-c][1,4]benzodiazepine (PBD) derivatives, their conjugates with a cell-binding agent, the preparation and the therapeutic uses in the targeted treatment of cancers, autoimmune disorders, and infectious diseases.
摘要翻译： 本发明涉及新型细胞毒剂，吡咯并[2,1-c] [1,4]苯并二氮杂（PBD）衍生物，它们与细胞结合剂的缀合物，靶向治疗癌症的制备和治疗用途 ，自身免疫性疾病和感染性疾病。
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