公开(公告)号：US20220226496A1

公开(公告)日：2022-07-21

申请号：US17607678

申请日：2020-04-29

Applicant: LEGOCHEM BIOSCIENCES, INC.

Inventor： Ho Young SONG ,  Yun-Hee PARK ,  Sang Eun CHAE ,  Ju Yuel BAEK ,  Kyung Eun PARK ,  Ju Young LEE ,  Su In LEE ,  Jeiwook CHAE ,  Chang Sun LEE ,  Yong Zu KIM

IPC: A61K47/68 ,  A61K47/54 ,  A61K47/60 ,  A61K45/06

Abstract: The present invention relates to a ligand-drug conjugate including a ligand; a linker that is connected to the ligand by a covalent bond and has a tris structure represented by a specific structural formula; and an active agent connected to the linker by a covalent bond. In the ligand-drug conjugate, the active agent is bound by the tris structure of the linker, and thus a greater number of active agents can be connected through one linker. Accordingly, a greater number of active agents per antibody binding can be delivered to the target cell, and the drug and/or toxin can stably reach the target cell and effectively exert the drug efficacy.

公开(公告)号：US20220096641A1

公开(公告)日：2022-03-31

申请号：US17420007

申请日：2020-01-03

Applicant: LEGOCHEM BIOSCIENCES, INC.

Inventor： Ho Young SONG ,  Juyuel BAEK ,  Sung Min KIM ,  Hyoung Rae KIM ,  Hyeun Joung LEE ,  Ju Young LEE ,  Kun Jung LEE ,  Yun-Hee PARK ,  Chang Sik PARK ,  Hwan Hee OH ,  Jihye OH ,  Jeiwook CHAE ,  Yong Zu KIM ,  Sang Eun CHAE ,  Hyunmin RYU ,  Nara HAN ,  Min Ji CHOI

IPC: A61K47/55 ,  A61K47/68 ,  A61P35/00 ,  C07D487/04 ,  C07H15/26

Abstract: The present invention relates to a novel pyrrolobenzodiazepine dimer compound or a pharmaceutically acceptable salt thereof, a ligand-drug conjugate compound thereof, or a composition containing the same and therapeutic use of the same as an anticancer agent. The pyrrolobenzodiazepine dimer compound according to the present invention exhibits anticancer activity equivalent to or superior to that of existing anticancer agents when being applied to a ligand-drug conjugate as a drug and administered as well as exhibits low activity and greatly diminished toxicity in the free toxin form and thus has a significantly improved therapeutic index. Hence, the pyrrolobenzodiazepine dimer compound is highly industrially applicable in that targeting of proliferative diseases such as cancer is possible, specific treatment of the proliferative diseases is possible, the drug efficacy can be maximized, and the expression of side effects can be minimized.