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1. (WO2017176040) HETEROCYCLIC COMPOUND DECOMPOSING RAS AND USES THEREOF
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Pub. No.: WO/2017/176040 International Application No.: PCT/KR2017/003704
Publication Date: 12.10.2017 International Filing Date: 04.04.2017
IPC:
C07D 403/06 (2006.01) ,C07D 235/06 (2006.01) ,C07D 471/04 (2006.01) ,C07D 241/36 (2006.01) ,A61K 31/4178 (2006.01) ,A61K 31/4155 (2006.01) ,A61K 31/4184 (2006.01) ,A61K 31/498 (2006.01) ,A61K 45/06 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
235
Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
02
condensed with carbocyclic rings or ring systems
04
Benzimidazoles; Hydrogenated benzimidazoles
06
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
241
Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
36
condensed with carbocyclic rings or ring systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4164
1,3-Diazoles
4178
not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
415
1,2-Diazoles
4155
not condensed and containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4164
1,3-Diazoles
4184
condensed with carbocyclic rings, e.g. benzimidazoles
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
498
Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45
Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
06
Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
Applicants:
연세대학교 산학협력단 INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY [KR/KR]; 서울시 서대문구 연세로 50, 연세대학교 Yonsei University, 50, Yonsei-ro Seodaemun-gu Seoul 03722, KR
Inventors:
최강열 CHOI, Kang-Yell; KR
한균희 HAN, Gyoonhee; KR
차부현 CHA, Pu-Hyeon; KR
김현태 KIM, Hyuntae; KR
이철호 LEE, Chulho; KR
Agent:
특허법인 충현 CHUNG HYUN PATENT & LAW FIRM; 서울시 서초구 동산로 23 베델회관 8층 Bethel Bldg. 8F., 23, Dongsan-ro Seocho-gu Seoul 06779, KR
Priority Data:
10-2016-004114504.04.2016KR
Title (EN) HETEROCYCLIC COMPOUND DECOMPOSING RAS AND USES THEREOF
(FR) COMPOSÉ HÉTÉROCYCLIQUE DÉCOMPOSANT UNE PROTÉINE RAS ET UTILISATIONS CORRESPONDANTES
(KO) Ras를 분해하는 이종원자고리화합물 및 이의 용도
Abstract:
(EN) The present invention relates to a compound which simultaneously degrades β-catenin and a Ras protein comprising a K-Ras mutation. The compound according to the present invention induces the inhibition of cancer proliferation and the death of cancer cells by regulating a signal input into a key signal transduction system involved with cancer, thereby exhibiting an effect on the treatment of cancer in cancer patients showing resistance to conventional anticancer agents due to Wnt signal transduction abnormality and Ras gene mutation.
(FR) La présente invention concerne un composé qui dégrade simultanément la ß-caténine et une protéine Ras comprenant une mutation K-Ras. Le composé selon la présente invention induit l'inhibition de la prolifération cancéreuse et la mort de cellules cancéreuses par la régulation d'une entrée de signal dans un système de transduction de signal clé impliqué dans le cancer, présentant ainsi un effet sur le traitement du cancer chez des patients atteints d'un cancer montrant une résistance aux agents anticancéreux classiques en raison d'une anomalie de transduction du signal Wnt et d'une mutation du gène de Ras.
(KO) 본 발명은 β-카테닌과 K-Ras 돌연변이를 포함하는 Ras 단백질을 동시에 분해하여 화합물에 관한 것으로, 본 발명에 따른 화합물은 암과 관련되는 핵심적인 주요 신호전달계에 신호유입을 조절하여 암의 증식 억제 및 암 세포의 사멸 유도하여 Wnt 신호전달계 이상과 Ras 유전자 돌연변이로 인해 종래의 항암제에 대하여 저항성을 보이는 암환자의 암 치료에 효과를 나타낸다.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: Korean (KO)
Filing Language: Korean (KO)