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公开(公告)号:US20200069814A1
公开(公告)日:2020-03-05
申请号:US16488764
申请日:2017-04-06
发明人: Robert Yongxin ZHAO , Yuanyuan HUANG , Qingliang YANG , Shun GAI , Hangbo YE , Linyao ZHAO , Chengyu YANG , Yifang XU , Huihui GUO , Minjun CHAO , Qianqian TONG , Wenjun LI , Xiang CAI , Xiaomai ZHOU , Hongsheng XIE , Junxiang JIA , Haifeng ZHU , Zhixiang GUO , Shuihong GAO , Chunyan WANG , Chen LIN , Yanlei YANG , Zhicang YE , Jie PENG , Jun XU , Xiaotao ZUO , Qingyu SU
IPC分类号: A61K47/68
摘要: A conjugation of a cytotoxic drug to a cell-binding molecule with a bis-linker (dual-linker) as shown in Formula (I). Bis-linkage methods of making a conjugate of a cytotoxic drug/molecule to a cell-binding agent in a specific manner are also described, as well as application of the conjugates for the treatment of a cancer, or an autoimmune disease, or an infectious disease. wherein “” is an optional bond; X, Y, Z1, and Z2 are a functional group; m1 and n are a integer; L1 and L2 are a linker.
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公开(公告)号:US20190330149A1
公开(公告)日:2019-10-31
申请号:US16407367
申请日:2019-05-09
发明人: R. Yongxin ZHAO , Yue ZHANG , Yourang MA
IPC分类号: C07D207/40 , A61K47/64 , A61K47/68 , A61K45/06
摘要: A conjugate of a potent cytotoxic agent with a cell-surface receptor binding molecule having a Formula (I), wherein T, L, m, n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, and R13 are defined herein, can be used for targeted treatment of cancer, autoimmune disease, and infectious disease.
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公开(公告)号:US20190127401A1
公开(公告)日:2019-05-02
申请号:US16228437
申请日:2018-12-20
发明人: Robert Yongxin ZHAO , Xing LI , Yuangyuang HUANG , Qingliang YANG
IPC分类号: C07F9/30 , C07F9/572 , C07F9/6558 , A61K47/68 , C07F9/6561 , C07F9/32 , A61K38/07 , C07F9/58
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:US20180110876A1
公开(公告)日:2018-04-26
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
CPC分类号: A61K47/6889 , A61K47/6803 , A61K47/6811 , A61K47/6849 , A61K47/6851 , C07D207/46 , C07F9/572 , C07F9/65583 , C07K16/00 , C07K16/2878
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:US20170152274A1
公开(公告)日:2017-06-01
申请号:US15118726
申请日:2014-02-28
发明人: Robert Yongxin ZHAO , Xing LI , Yuangyuang HUANG , Qingliang YANG
IPC分类号: C07F9/30 , C07F9/58 , A61K38/07 , C07F9/6561 , C07F9/572 , C07F9/32 , C07F9/6558
CPC分类号: C07F9/301 , A61K38/07 , A61K47/6803 , A61K47/6807 , A61K47/6809 , A61K47/6811 , A61K47/6817 , A61K47/6851 , A61K47/6889 , C07F9/302 , C07F9/3211 , C07F9/3217 , C07F9/572 , C07F9/58 , C07F9/65583 , C07F9/6561 , C07F9/65616
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:US20230010108A1
公开(公告)日:2023-01-12
申请号:US17284091
申请日:2018-10-12
发明人: Robert Yongxin ZHAO , Qingliang YANG , Yuanyuan HUANG , Linyao ZHAO , Hangbo YE , Xiaotao ZHUO , Chengyu YANG , Jun LEI , Yifang XU , Huihui GUO , Wenjun LI , Shun GAI , Lu BAI , Zhixiang GUO , Junxiang JIA , Jun ZHENG , Xiaomai ZHOU , Hongsheng XIE , Qianqian TONG , Mingjun CHAO , Yanhong TONG , Zhicang YE , Chen LIN , Yanlei YANG , Binbin CHEN
IPC分类号: C07D403/12 , C07D417/12 , C07D413/14 , C07D417/14 , C07D403/14 , C07D498/22 , C07D498/12 , A61K47/54 , A61K45/06 , A61K47/68
摘要: The present invention relates to a conjugate of a cytotoxic drug/molecule to a cell-binding molecule with a bis-linker (a dual-linker) containing a 2,3-diaminosuccinyl group. It also relates to preparation of the conjugate of a cytotoxic drug/molecule to a cell-binding molecule with the bis-linker, particularly when the drug having functional groups of amino, hydroxyl, diamino, amino-hydroxyl, dihydroxyl, carboxyl, hydrazine, aldehyde and thiol for conjugation with the bis-linker in a specific manner, as well as the therapeutic use of the conjugates.
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公开(公告)号:US20230001001A1
公开(公告)日:2023-01-05
申请号:US17390064
申请日:2021-07-30
发明人: Robert Yongxin ZHAO , Yuanyuan HUANG , Qingliang YANG , Shun GAI , Hangbo YE , Linyao ZHAO , Chengyu YANG , Yifang XU , Huihui GUO , Minjun CHAO , Qianqian TONG , Wenjun LI , Xiang CAI , Xiaomai ZHOU , Hongsheng XIE , Junxiang JIA , Haifeng ZHU , Zhixiang GUO , Shuihong GAO , Chunyan WANG , Chen LIN , Yanlei YANG , Zhicang YE , Jie PENG , Jun XU , Xiaotao ZUO , Qingyu SU
IPC分类号: A61K47/68 , C07D413/12 , C07D487/04 , C07D498/22 , C07D498/04 , C07D513/22
摘要: A conjugation of a cytotoxic drug to a cell-binding molecule with a bis-linker (dual-linker) as shown in Formula (I). Bis-linkage methods of making a conjugate of a cytotoxic drug/molecule to a cell-binding agent in a specific manner are also described, as well as application of the conjugates for the treatment of a cancer, or an autoimmune disease, or an infectious disease. wherein “” is an optional bond; X, Y, Z1, and Z2 are a functional group; m1 and n are a integer; L1 and L2 are a linker.
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公开(公告)号:US20220378951A1
公开(公告)日:2022-12-01
申请号:US17355286
申请日:2021-06-23
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:US20220313838A1
公开(公告)日:2022-10-06
申请号:US17835395
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:US20220313837A1
公开(公告)日:2022-10-06
申请号:US17835311
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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