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.

公开(公告)号：US20230310640A1

公开(公告)日：2023-10-05

申请号：US17758241

申请日：2020-12-30

Applicant: LEGOCHEM BIOSCIENCES, INC.

Inventor： Ho Young SONG ,  Yun-Hee PARK ,  Kun Jung LEE ,  Ji Hye OH ,  Sung Min KIM ,  Kyung Eun PARK ,  Yong Gyu PARK ,  Hyun Min RYU ,  Na Ra HAN ,  Chul Woong CHUNG ,  Jei Wook CHAE ,  Yong Zu KIM

IPC: A61K47/68 ,  A61K47/54 ,  A61P35/00

CPC classification number: A61K47/6871 ,  A61K47/545 ,  A61K47/549 ,  A61K47/6803 ,  A61P35/00

Abstract: The present invention relates to a pyrrolobenzodiazepine derivative compound, a conjugate of the same with a ligand, and the use of the same. The pyrrolobenzodiazepine derivative compound is more stable in plasma, is stable even in circulation, and exhibits excellent efficacy. In particular, the conjugate of the pyrrolobenzodiazepine derivative compound with a ligand has a great advantage in that it is possible to target and specifically treat proliferative disease such as cancer, maximize drug efficacy, and minimize the expression of side effects since the conjugate more stably reaches the target cell and effectively exerts drug efficacy while toxicity is greatly reduced as a linker technology that allows drugs to be easily released within cancer cells and maximize drug efficacy is incorporated.