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1. (WO2018164549) NOVEL COMPOUND HAVING MALATE DEHYDROGENASE INHIBITORY ACTIVITY AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING CANCER COMPRISING SAME AS ACTIVE INGREDIENT
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Pub. No.: WO/2018/164549 International Application No.: PCT/KR2018/002861
Publication Date: 13.09.2018 International Filing Date: 09.03.2018
IPC:
C07C 235/38 (2006.01) ,A61K 31/192 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
235
Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
02
having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
32
the carbon skeleton containing six-membered aromatic rings
38
having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
185
Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
19
Carboxylic acids, e.g. valproic acid
192
having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
Applicants:
동국대학교 산학협력단 DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION [KR/KR]; 서울시 중구 필동로1길 30 30, Pildong-ro 1-gil, Jung-gu, Seoul 04620, KR
한국생명공학연구원 KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY [KR/KR]; 대전시 유성구 과학로 125 125, Gwahak-ro, Yuseong-gu, Daejeon 34141, KR
Inventors:
이경 LEE, Kyeong; KR
원미선 WON, Mi Sun; KR
반현승 BAN, Hyun Seung; KR
김민경 KIM, Minkyoung; KR
김보경 KIM, Bo Kyung; KR
Agent:
이명진 LEE, Myoung-Jin; KR
Priority Data:
10-2017-002991609.03.2017KR
10-2018-002739708.03.2018KR
Title (EN) NOVEL COMPOUND HAVING MALATE DEHYDROGENASE INHIBITORY ACTIVITY AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING CANCER COMPRISING SAME AS ACTIVE INGREDIENT
(FR) NOUVEAU COMPOSÉ AYANT UNE ACTIVITÉ INHIBITRICE DE MALATE DÉSHYDROGÉNASE ET COMPOSITION PHARMACEUTIQUE DESTINÉE À PRÉVENIR OU À TRAITER LE CANCER LE CONTENANT À TITRE DE PRINCIPE ACTIF
(KO) 말릭산 탈수소효소 저해 활성을 갖는 신규 화합물 및 이를 유효성분으로 포함하는 암 예방 또는 치료용 약학적 조성물
Abstract:
(EN) The present invention relates to a compound exhibiting inhibitory activity of at least one of malate dehydrogenases 1 (MDH1) and malate dehydrogenases 2 (MDH2), and a pharmaceutical composition for preventing or treating cancer comprising the same as an active ingredient. The inventors of the present invention have experimentally confirmed that the compound exhibiting the MDH1 and/or MDH2 inhibitory activity has an inhibitory effect on mitochondrial respiration in cancer cells, an excellent inhibitory effect on cancer cell growth, etc.. Thus, the compound of the present invention is expected to be effectively used as a pharmaceutical composition for treating cancer.
(FR) La présente invention concerne un composé présentant une activité inhibitrice d'au moins une des malate déshydrogénases 1 (MDH1) et/ou malate déshydrogénases 2 (MDH2), et une composition pharmaceutique destinée à prévenir ou à traiter le cancer le contenant à titre de principe actif. Les inventeurs de la présente invention ont confirmé expérimentalement que le composé présentant l'activité inhibitrice de MDH1 et/ou MDH2 a un effet inhibiteur sur la respiration mitochondriale dans les cellules cancéreuses, un excellent effet inhibiteur sur la croissance des cellules cancéreuses, etc. Par conséquent, le composé selon la présente invention devrait être utilisé de manière efficace sous forme de composition pharmaceutique pour traiter le cancer.
(KO) 본 발명은 MDH1 (malate dehydrogenases 1) 및 MDH2 (malate dehydrogenases 2) 중 어느 하나 이상의 억제 활성을 나타내는 화합물 및 이를 유효성분으로 포함하는, 암 예방 또는 치료용 약학적 조성물에 관한 것이다. 본 발명자들은 MDH1 및/또는 MDH2 억제 활성을 나타내는 화합물의 암세포 내 미토콘드리아 호흡 억제 효과 및 우수한 암세포 성장 억제 효과 등을 실험적으로 확인하였는바, 본 발명의 화합물은 암을 치료하기 위한 약학적 조성물로 유용하게 사용될 수 있을 것으로 기대된다.
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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, JO, JP, KE, KG, KH, KN, KP, 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)