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公开(公告)号：EP3380125A1
公开(公告)日：2018-10-03
申请号：EP16868095.7
申请日：2016-11-23
发明人： KIM, Yong Zu , OH, Yeong Soo , CHAE, Jeiwook , SONG, Ho Young , CHUNG, Chul-Woong , PARK, Yun Hee , CHOI, Hyo Jung , PARK, Kyung Eun , KIM, Hyoungrae , KIM, Jinyeong , MIN, Ji Young , KIM, Sung Min , LEE, Byung Soo , WOO, Dong Hyun , JUNG, Ji Eun , LEE, Su In
CPC分类号： A61K47/6863 , A61K47/6803 , A61K47/6855 , A61K47/6857 , A61K47/6889
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：EP3380124A1
公开(公告)日：2018-10-03
申请号：EP16868091.6
申请日：2016-11-23
发明人： KIM, Yong Zu , OH, Yeong Soo , CHAE, Jeiwook , SONG, Ho Young , CHUNG, Chul-Woong , PARK, Yun Hee , CHOI, Hyo Jung , PARK, Kyung Eun , KIM, Hyoungrae , KIM, Jinyeong , MIN, Ji, Young , KIM, Sung, Min , LEE, Byung Soo , WOO, Dong Hyun , JUN, Ji Eun , LEE, Su In
CPC分类号： A61K47/6811 , A61K38/00 , A61K47/549 , A61K47/60 , A61K47/6845 , A61K47/6855 , A61K47/6867 , A61K47/6889 , Y02A50/471 , Y02A50/475
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：EP3380126A1
公开(公告)日：2018-10-03
申请号：EP16868096.5
申请日：2016-11-23
发明人： KIM, Yong Zu , OH, Yeong Soo , CHAE, Jeiwook , SONG, Ho Young , CHUNG, Chul-Woong , PARK, Yun Hee , CHOI, Hyo Jung , PARK, Kyung Eun , KIM, Hyoungrae , KIM, Jinyeong , MIN, Ji Young , KIM, Sung Min , LEE, Byung Soo , WOO, Dong Hyun , JUNG, Ji Eun , LEE, Su In
CPC分类号： A61K47/6883 , A61K47/6803 , A61K47/6849 , A61K47/6855 , A61K47/6889
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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