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1. KR1020200097222 - TARGET PROTEIN EED DEGRADATION-INDUCING DEGRADUCER, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING EED-, EZH2-, OR PRC2-RELATED DISEASES INCLUDING SAME AS ACTIVE INGREDIENT

Office
République de Corée
Numéro de la demande 1020200015266
Date de la demande 07.02.2020
Numéro de publication 1020200097222
Date de publication 18.08.2020
Type de publication A
CIB
C07D 487/04
CCHIMIE; MÉTALLURGIE
07CHIMIE ORGANIQUE
DCOMPOSÉS HÉTÉROCYCLIQUES
487Composés hétérocycliques contenant des atomes d'azote comme uniques hétéro-atomes dans le système condensé, non prévus par les groupes C07D451/-C07D477/187
02dans lesquels le système condensé contient deux hétérocycles
04Systèmes condensés en ortho
A61K 31/519
ANÉCESSITÉS COURANTES DE LA VIE
61SCIENCES MÉDICALE OU VÉTÉRINAIRE; HYGIÈNE
KPRÉPARATIONS À USAGE MÉDICAL, DENTAIRE OU POUR LA TOILETTE
31Préparations médicinales contenant des ingrédients actifs organiques 
33Composés hétérocycliques
395ayant l'azote comme hétéro-atome d'un cycle, p.ex. guanéthidine ou rifamycines
495ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p.ex. pipérazine
505Pyrimidines; Pyrimidines hydrogénées, p.ex. triméthoprime
519condensées en ortho ou en péri avec des hétérocycles
A61P 35/00
ANÉCESSITÉS COURANTES DE LA VIE
61SCIENCES MÉDICALE OU VÉTÉRINAIRE; HYGIÈNE
PACTIVITÉ THÉRAPEUTIQUE SPÉCIFIQUE DE COMPOSÉS CHIMIQUES OU DE PRÉPARATIONS MÉDICINALES
35Agents anticancéreux
C07D 401/14
CCHIMIE; MÉTALLURGIE
07CHIMIE ORGANIQUE
DCOMPOSÉS HÉTÉROCYCLIQUES
401Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote
14contenant au moins trois hétérocycles
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
A61K 31/519
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
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 401/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14containing three or more hetero rings
Déposants 한국화학연구원
한국생명공학연구원
KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY
Inventeurs HWANG JONG YEON
HA JAE DU
CHO SUNG YUN
KIM PILHO
황종연
YUN CHANG SOO
하재두
KIM HYUN JIN
조성윤
PARK SUNG GOO
김필호
PARK BYOUNG CHUL
윤창수
KIM JEONG HOON
김현진
KIM SUNHONG
박성구
박병철
김정훈
김선홍
Mandataires 특허법인필앤온지
Données relatives à la priorité 1020190014633 07.02.2019 KR
Titre
(EN) TARGET PROTEIN EED DEGRADATION-INDUCING DEGRADUCER, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING EED-, EZH2-, OR PRC2-RELATED DISEASES INCLUDING SAME AS ACTIVE INGREDIENT
(KO) 표적 단백질 EED 분해 유도 데그라듀서, 이의 제조방법 및 이를 유효성분으로 함유하는 EED, EZH2, 또는 PRC2 관련 질환의 예방 또는 치료용 약학적 조성물
Abrégé
(EN)
The present invention relates to a target protein degradation-inducing degraducer, a method for preparing the same, and a pharmaceutical composition for preventing or treating EED-, EZH2- or PRC2-related diseases including the same as an active ingredient. The present invention provides a novel compound represented by the chemical formula of ULB-L-PTM, which is a degraducer compound inducing degradation of a target protein, i.e. EED (embryonic ectoderm development) or PRC2 (polycomb repressive complex 2), using cereblon E3 ubiquitin ligase, VHL (von Hippel-Lindau tumor suppressor) E3 ubiquitin ligase, MDM2 (Mouse double minute 2 homolog) E3 ubiquitin ligase, or cIAP (Cellular Inhibitor of Apoptosis Protein 1) E3 ubiquitin ligase, and significantly realizes a target protein degradation-inducing activity through UPS (Ubiquitin Proteasome System). Therefore, the compound can be used advantageously as an active ingredient of a pharmaceutical composition for preventing or treating the target protein-related diseases or conditions and a health-aid food composition for preventing or alleviating the target protein-related diseases or conditions. COPYRIGHT KIPO 2021

(KO)
본 발명은 표적 단백질 분해 유도 데그라듀서, 이의 제조방법 및 이를 유효성분으로 함유하는 EED, EZH2, 또는 PRC2 관련 질환의 예방 또는 치료용 약학적 조성물에 관한 것이다. 본 발명에 따른 화학식 1로 표시되는 신규 화합물은, 세레브론(cereblon) E3 유비퀴틴 리가제, VHL(von Hippel-Lindau tumor suppressor) E3 유비퀴틴 리가제, MDM2(Mouse double minute 2 homolog) E3 유비퀴틴 리가제, cIAP(Cellular Inhibitor of Apoptosis Protein 1) E3 유비퀴틴 리가제를 활용한, 타깃 단백질, 즉, EED(embryonic ectoderm development) 또는 PRC2 (polycomb repressive complex 2)의 분해를 유도하는 데그라듀서 (Degraducer) 화합물로서, UPS(Ubiquitin Proteasome System)을 통하여 타깃 단백질 분해 유도 활성을 현저하게 달성하는 측면이 있는 바, 이를 유효성분으로 함유하는 타깃 단백질 관련 질환 또는 병태의 예방 또는 치료용 약학적 조성물, 및 예방 또는 개선용 건강기능식품 조성물을 제공할 수 있는 유용한 효과가 있다.

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EP2020753191This application is not viewable in PATENTSCOPE because the national phase entry has not been published yet or the national entry is issued from a country that does not share data with WIPO or there is a formatting issue or an unavailability of the application.