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公开(公告)号:US20210308277A1
公开(公告)日:2021-10-07
申请号:US16348749
申请日:2016-11-14
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: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: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: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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