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公开(公告)号:US20210346523A1
公开(公告)日:2021-11-11
申请号:US17373987
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:US20210052747A1
公开(公告)日:2021-02-25
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: 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: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: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:US20220249594A1
公开(公告)日:2022-08-11
申请号:US17596956
申请日:2020-02-18
发明人: Robert ZHAO , Qingliang YANG , Yuanyuan HUANG , Shun GAI , Hangbo YE , Linyao ZHAO , Huihui GUO , Lu BAI , Wenjun LI , Junxiang JIA , Zhixiang GUO , Jun ZHENG , Xiaoxiao CHEN , Xiangfei KONG , Chen LIN , Yong DU , Yu ZHANG , Lei ZHOU , Xiuzhen ZHANG , Xiuhong ZHENG , Binbin CHEN , Yanlei YANG , Meng DAI , Yifang XU , Zhongliang FAN , Xiaomai ZHOU , Xingyan JIANG , Miaomiao CHEN , Lingli ZHANG , Yanhua LI
摘要: A formulation of conjugates of tubulysin analogs with a cell-binding molecule having a structure represented by Formula (I), wherein T, L, m, n, ----, R1, R2, R3, R4, R1, R6, R7, R1, R9, R10, R11, R12, and R13 are as defined herein, can be used for targeted treatment of cancer, autoimmune disease, and infectious disease.
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公开(公告)号:US20210393790A1
公开(公告)日:2021-12-23
申请号:US17389922
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:US20230071112A1
公开(公告)日:2023-03-09
申请号:US17835419
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 propioloyl, 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:US20210369855A1
公开(公告)日:2021-12-02
申请号:US17387205
申请日:2021-07-28
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:US20200079820A1
公开(公告)日:2020-03-12
申请号:US16078080
申请日:2016-04-20
发明人: Robert Yongxin ZHAO , Qingliang YANG , Yuanyuan HUANG , Shun GAI , Hangbo YE , Chengyu YANG , Huihui GUO , Xiaomai ZHOU , Hongsheng XIE , Qianqian TONG , Minjun CAO , Linyao ZHAO , Junxiang JIA , Wenjun LI , Xiaotao ZUO , Chen LIN , Yifang XU , Zixiang GUO
摘要: The present invention is related to novel cytotoxic agents, derivatives of Amanita toxins of Formula (I), wherein , - - - , R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, L, m, n and Q are defined herein, the preparation and the therapeutic uses in the targeted treatment of cancers, autoimmune disorders, and infectious diseases.
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公开(公告)号:US20190125894A1
公开(公告)日:2019-05-02
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
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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