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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：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：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：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：US20220323602A1
公开(公告)日：2022-10-13
申请号：US17835041
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：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：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：US20230165930A1
公开(公告)日：2023-06-01
申请号：US18156709
申请日：2023-01-19
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： Described is a 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. Also described are 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：US20230149502A1
公开(公告)日：2023-05-18
申请号：US18156793
申请日：2023-01-19
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： Described is a 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. Also described are 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：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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