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公开(公告)号：US09993568B2
公开(公告)日：2018-06-12
申请号：US14898932
申请日：2015-05-27
发明人： Yong Zu Kim , Tae Kyo Park , Sung Ho Woo , Sun Young Kim , Jong Un Cho , Doo Hwan Jung , Ji Young Min , Hyang Sook Lee , Yun Hee Park , Jeong Hee Ryu , Kyu Man Oh , Yeong Soo Oh , Jeiwook Chae , Ho Young Song , Chul-Woong Chung , Jeon Yang
CPC分类号： A61K47/6871 , A61K47/549 , A61K47/6801 , A61K47/6803 , A61K47/6811 , A61K47/6813 , A61K47/6855 , A61K47/6889 , A61K47/69 , A61K2039/505 , C07D249/04 , C07D487/04 , C07D519/00 , C07K16/32 , C07K19/00 , C07K2317/24
摘要： Provided are methods of use of compounds comprising a self-immolative group, which compounds may include a protein (for example, an oligopeptide, a polypeptide, an antibody, or the like) having substrate-specificity for a target and an active agent (for example, a drug, a toxin, a ligand, a detection probe, or the like) having a specific function or activity.
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公开(公告)号：US11975076B2
公开(公告)日：2024-05-07
申请号：US17525582
申请日：2021-11-12
发明人： Yong Zu Kim , Yeong Soo Oh , Jeiwook Chae , Ho Young Song , Chul-Woong Chung , Yun Hee Park , Hyo Jung Choi , Kyung Eun Park , Hyoungrae Kim , Jinyeong Kim , Ji Young Min , Sung Min Kim , Byung Soo Lee , Dong Hyun Woo , Ji Eun Jung , Su In Lee
CPC分类号： A61K47/6889 , A61K47/60 , A61K47/6803 , A61K47/6817 , A61K47/6849 , A61K47/6855 , A61K47/6883 , A61P35/00
摘要： The present invention relates to antibody-drug conjugates (ADCs) wherein a plurality of active agents are conjugated to an antibody through at least one branched linker. The branched linker may comprise a branching unit, and two active agents are coupled to the branching unit through a secondary linker and the branching unit is coupled to the antibody by a primary linker. The active agents may be the same or different. In certain such embodiments, two or more such branched linkers are conjugated to the antibody, e.g., 2-4 branched linkers, which may each be coupled to a different C-terminal cysteine of a heavy or light chain of the antibody. The branched linker may comprise one active agent coupled to the branching unit by a first branch and a second branch that comprises a polyethylene glycol moiety coupled to the branching unit. In certain such embodiments, two or more such branched linkers are conjugated to the antibody, e.g., 2-4 branched linkers, which may each be coupled to a different C-terminal cysteine of a heavy or light chain of the antibody.
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公开(公告)号：US20220218840A1
公开(公告)日：2022-07-14
申请号：US17525582
申请日：2021-11-12
发明人： Yong Zu Kim , Yeong Soo Oh , Jeiwook Chae , Ho Young Song , Chul-Woong Chung , Yun Hee Park , Hyo Jung Choi , Kyung Eun Park , Hyoungrae Kim , Jinyeong Kim , Ji Young Min , Sung Min Kim , Byung Soo Lee , Dong Hyun Woo , Ji Eun Jung , Su In Lee
摘要： The present invention relates to antibody-drug conjugates (ADCs) wherein a plurality of active agents are conjugated to an antibody through at least one branched linker. The branched linker may comprise a branching unit, and two active agents are coupled to the branching unit through a secondary linker and the branching unit is coupled to the antibody by a primary linker. The active agents may be the same or different. In certain such embodiments, two or more such branched linkers are conjugated to the antibody, e.g., 2-4 branched linkers, which may each be coupled to a different C-terminal cysteine of a heavy or light chain of the antibody. The branched linker may comprise one active agent coupled to the branching unit by a first branch and a second branch that comprises a polyethylene glycol moiety coupled to the branching unit. In certain such embodiments, two or more such branched linkers are conjugated to the antibody, e.g., 2-4 branched linkers, which may each be coupled to a different C-terminal cysteine of a heavy or light chain of the antibody.
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公开(公告)号：US11167040B2
公开(公告)日：2021-11-09
申请号：US15779450
申请日：2016-11-23
发明人： Yong Zu Kim , Yeong Soo Oh , Jeiwook Chae , Ho Young Song , Chul-Woong Chung , Yun Hee Park , Hyo Jung Choi , Kyung Eun Park , Hyoungrae Kim , Jinyeong Kim , Ji Young Min , Sung Min Kim , Byung Soo Lee , Dong Hyun Woo , Ji Eun Jung , Su In Lee
摘要： In some aspects, the invention relates to an antibody-drug conjugate, comprising an antibody; a linker; and at least two active agents. In preferred embodiments, the linker comprises a peptide sequence of a plurality of amino acids, and at least two of the active agents are covalently coupled to side chains of the amino acids. The antibody-drug conjugate may comprise a self-immolative group, preferably two-self-immolative groups. The linker may comprise an O-substituted oxime, e.g., wherein the oxygen atom of the oxime is substituted with a group that covalently links the oxime to the active agent; and the carbon atom of the oxime is substituted with a group that covalently links the oxime to the antibody.
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公开(公告)号：US20200297865A1
公开(公告)日：2020-09-24
申请号：US15779446
申请日：2016-11-23
发明人： Yong Zu Kim , Yeong Soo Oh , Jeiwook Chae , Ho Young Song , Chul-Woong Chung , Yun Hee Park , Hyo Jung Choi , Kyung Eun Park , Hyoungrae Kim , Jinyeong Kim , Ji Young Min , Sung Min Kim , Byung Soo Lee , Dong Hyun Woo , Ji Eun Jung , Su In Lee
摘要： In some aspects, the invention relates to an antibody-drug conjugate, comprising an antibody; a linker; and an active agent. The antibody-drug conjugate may comprise a self-immolative group. The linker may comprise an O-substituted oxime, e.g., wherein the oxygen atom of the oxime is substituted with a group that covalently links the oxime to the active agent; and the carbon atom of the oxime is substituted with a group that covalently links the oxime to the antibody.
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公开(公告)号：US20190151465A1
公开(公告)日：2019-05-23
申请号：US15779444
申请日：2016-11-23
发明人： Yong Zu Kim , Yeong Soo Oh , Jeiwook Chae , Ho Young Song , Chul-Woong Chung , Yun Hee Park , Hyo Jung Choi , Kyung Eun Park , Hyoungrae Kim , Jinyeong Kim , Ji Young Min , Sung Min Kim , Byung Soo Lee , Dong Hyun Woo , Ji Eun Jung , Su In Lee
摘要： The present invention relates to antibody-drug conjugates (ADCs) wherein a plurality of active agents are conjugated to an antibody through at least one branched linker. The branched linker may comprise a branching unit, and two active agents are coupled to the branching unit through a secondary linker and the branching unit is coupled to the antibody by a primary linker. The active agents may be the same or different. In certain such embodiments, two or more such branched linkers are conjugated to the antibody, e.g., 2-4 branched linkers, which may each be coupled to a different C-terminal cysteine of a heavy or light chain of the antibody. The branched linker may comprise one active agent coupled to the branching unit by a first branch and a second branch that comprises a polyethylene glycol moiety coupled to the branching unit. In certain such embodiments, two or more such branched linkers are conjugated to the antibody, e.g., 2-4 branched linkers, which may each be coupled to a different C-terminal cysteine of a heavy or light chain of the antibody.
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