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.

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.

公开(公告)号：US20170152251A1

公开(公告)日：2017-06-01

申请号：US15325521

申请日：2014-07-18

Applicant: GREEN CROSS CORPORATION ,  LEGOCHEM BIOSCIENCES,INC.

Inventor： Soongyu CHOI ,  Jungsub CHOI ,  So-Hyun YOON ,  Yoo Hoon KIM ,  Jae Yeon KIM ,  Suk Ho LEE ,  Young Lag CHO ,  Ho Young SONG ,  Dae Yon LEE ,  Sung Yoon BAEK ,  Sang Eun CHAE ,  Tae Kyo PARK ,  Sung Ho WOO ,  Yong Zu KIM

IPC: C07D413/14

CPC classification number: C07D413/14 ,  A61K31/53 ,  A61P7/02 ,  A61P9/00 ,  A61P29/00 ,  C07B2200/13 ,  C07D253/065 ,  C07D409/10

Abstract: The present invention relates to a novel crystalline form of 5-chloro-N-({(5S)-2-oxo-3-[4-(5,6-dihydro-4H-[1,2,4]triazin-1-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide methanesulfonate and a pharmaceutical composition containing the same. The novel crystalline form of a compound according to the present invention exhibits excellent stability even in high-temperature and humidity environments, and thus can be favorably used to prevent or treat diseases, such as thrombosis, myocardial infarction, atherosclerosis, inflammation, stroke, angina pectoris, restenosis after angioplasty, and thromboembolism.