公开(公告)号：US20190151465A1

公开(公告)日：2019-05-23

申请号：US15779444

申请日：2016-11-23

Applicant: LEGOCHEM BIOSCIENCES, INC.

Inventor： 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

IPC: A61K47/68 ,  A61K47/60 ,  A61P35/00

Abstract: 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.

公开(公告)号：US10183997B2

公开(公告)日：2019-01-22

申请号：US15276209

申请日：2016-09-26

Applicant: LegoChem Biosciences, Inc.

Inventor： Yong Zu Kim ,  Yun Hee Park ,  Jeong Hee Ryu ,  Ho Young Song ,  Jeiwook Chae ,  Chul-Woong Chung ,  Ji Eun Jung ,  Hyo Jung Choi

IPC: C07D301/10 ,  C07K16/28 ,  A61K47/68 ,  A61K31/351

Abstract: In some aspects, the invention relates to an antibody-drug conjugate, comprising an anti-CD19 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.

公开(公告)号：US10118965B2

公开(公告)日：2018-11-06

申请号：US15276231

申请日：2016-09-26

Applicant: LegoChem Biosciences, Inc.

Inventor： Yong Zu Kim ,  Yun Hee Park ,  Hyo Jung Choi ,  Ji Eun Jung ,  Jeong Hee Ryu ,  Ho Young Song ,  Jeiwook Chae ,  Chul-Woong Chung

IPC: C07K16/28 ,  A61K47/68

Abstract: In some aspects, the invention relates to an antibody-drug conjugate, comprising an anti-epidermal growth factor receptor (“EGFR”) 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 drug; and the carbon atom of the oxime is substituted with a group that covalently links the oxime to the antibody.

公开(公告)号：US20170088621A1

公开(公告)日：2017-03-30

申请号：US15276231

申请日：2016-09-26

Applicant: LegoChem Biosciences, Inc.

Inventor： Yong Zu Kim ,  Yun Hee Park ,  Hyo Jung Choi ,  Ji Eun Jung ,  Jeong Hee Ryu ,  Ho Young Song ,  Jeiwook Chae ,  Chul-Woong Chung

IPC: C07K16/28

CPC classification number: C07K16/2863 ,  A61K47/6817 ,  A61K47/6849 ,  A61K47/6889

Abstract: In some aspects, the invention relates to an antibody-drug conjugate, comprising an anti-epidermal growth factor receptor (“EGFR”) 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 drug; and the carbon atom of the oxime is substituted with a group that covalently links the oxime to the antibody.