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1. WO2020141923 - PYRROLOBENZODIAZEPINE DIMER COMPOUND WITH IMPROVED SAFETY AND USE THEREOF

Publication Number WO/2020/141923
Publication Date 09.07.2020
International Application No. PCT/KR2020/000091
International Filing Date 03.01.2020
IPC
C07D 487/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/5517 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
55having seven-membered rings, e.g. azelastine, pentylenetetrazole
551having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
55131,4-Benzodiazepines, e.g. diazepam
5517condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
A61K 45/06 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 35/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
CPC
C07D 487/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Applicants
  • 주식회사 레고켐 바이오사이언스 LEGOCHEM BIOSCIENCES, INC. [KR]/[KR]
Inventors
  • 송호영 SONG, Ho Young
  • 백주열 BAEK, Juyuel
  • 김성민 KIM, Sung Min
  • 김형래 KIM, Hyoung Rae
  • 이현정 LEE, Hyeun Joung
  • 이주영 LEE, Ju Young
  • 이건중 LEE, Kun Jung
  • 박윤희 PARK, Yun-Hee
  • 박창식 PARK, Chang Sik
  • 오환희 OH, Hwan Hee
  • 오지혜 OH, Jihye
  • 채제욱 CHAE, Jeiwook
  • 김용주 KIM, Yong Zu
  • 채상은 CHAE, Sang Eun
  • 류현민 RYU, Hyunmin
  • 한나라 HAN, Nara
  • 최민지 CHOI, Min Ji
Agents
  • 김보민 KIM, Bo-min
Priority Data
10-2019-000051403.01.2019KR
10-2020-000027002.01.2020KR
Publication Language Korean (KO)
Filing Language Korean (KO)
Designated States
Title
(EN) PYRROLOBENZODIAZEPINE DIMER COMPOUND WITH IMPROVED SAFETY AND USE THEREOF
(FR) COMPOSÉ DIMÈRE DE PYRROLOBENZODIAZÉPINE PRÉSENTANT UNE SÉCURITÉ AMÉLIORÉE ET SON UTILISATION
(KO) 안전성이 향상된 피롤로벤조디아제핀 이량체 화합물 및 이의 용도
Abstract
(EN)
The present invention relates to a novel pyrrolobenzodiazepine dimer compound or a pharmaceutically acceptable salt thereof, a ligand-drug conjugate compound thereof, a composition containing same, and a therapeutic use thereof as an anticancer agent. The pyrrolobenzodiazepine dimer compound according to the present invention, in the form of a free toxin, exhibits an effect of greatly reducing toxicity due to a drop in activity thereof, but when applied and administered to a ligand-drug conjugate as a drug, has anticancer activity equal or superior to that of an existing anticancer agent and exhibits an effect of having a significantly improved therapeutic index. Therefore, the pyrrolobenzodiazepine dimer compound according to the present invention is very industrially useful, in that targeting of proliferative diseases such as cancer, specific treatment, maximization of drug efficacy, and minimization of the expression of side effects are possible.
(FR)
La présente invention concerne un nouveau composé dimère de pyrrolobenzodiazépine ou un sel pharmaceutiquement acceptable de celui-ci, un composé conjugué ligand-médicament de celui-ci, une composition contenant celui-ci et son utilisation thérapeutique en tant qu'agent anticancéreux. Le composé dimère de pyrrolobenzodiazépine selon la présente invention, sous la forme d'une toxine libre, présente un effet de réduction considérable de la toxicité due à une baisse d'activité de celui-ci, mais lorsqu'il est appliqué et administré dans un conjugué ligand-médicament en tant que médicament, présente une activité anticancéreuse supérieure ou égale à celle d'un agent anticancéreux existant et a comme effet de présenter un indice thérapeutique significativement amélioré. Par conséquent, le composé dimère de pyrrolobenzodiazépine selon la présente invention est très utile industriellement, en ce que le ciblage de maladies prolifératives telles que le cancer, le traitement spécifique, la maximisation de l'efficacité du médicament et la réduction au minimum de l'expression des effets secondaires sont possibles.
(KO)
본 발명은 신규한 피롤로벤조디아제핀 이량체 화합물 또는 이의 약학적으로 허용되는 염, 이의 리간드-약물 접합체 화합물, 이를 함유하는 조성물, 및 항암제로서의 이의 치료용도에 관한 것으로서, 본 발명에 따른 피롤로벤조디아제핀 이량체 화합물은 프리 톡신(free toxin) 형태에서는 활성이 떨어져 독성이 크게 감소하는 효과를 나타내면서도 리간드-약물 접합체에 약물로 적용되어 투여되는 경우 항암 활성이 기존 항암제 대비 동등 내지 우수한 것으로 나타났는바 치료지수(therapeutic index)가 현저히 향상되는 효과를 나타내며, 따라서 암과 같은 증식성 질환의 표적화, 특이적 치료, 약효의 극대화 및 부작용 발현의 최소화가 가능하다는 점에서 산업상 매우 유용하다.
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