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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：US20230165931A1
公开(公告)日：2023-06-01
申请号：US18156748
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：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：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：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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