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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: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: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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