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1. (WO2012053787) ARYLOXY PHENOXY ACRYLIC COMPOUND HAVING HIF-1 INHIBITION ACTIVITY, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS AN ACTIVE INGREDIENT
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2012/053787    International Application No.:    PCT/KR2011/007710
Publication Date: 26.04.2012 International Filing Date: 17.10.2011
IPC:
C07C 235/38 (2006.01), C07C 231/02 (2006.01), A61K 31/167 (2006.01), A61P 35/00 (2006.01)
Applicants: KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY [KR/KR]; 111, Gwahangno, Yuseong-gu Daejeon 305-806 (KR) (For All Designated States Except US).
DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION [KR/KR]; 26, Pil-dong 3(sam)-ga, Jung-gu Seoul 100-715 (KR) (For All Designated States Except US).
LEE, Kyeong [KR/KR]; (KR) (For US Only).
WON, Mi Sun [KR/KR]; (KR) (For US Only).
KIM, Hwan Mook [KR/KR]; (KR) (For US Only).
PARK, Song Kyu [KR/KR]; (KR) (For US Only).
LEE, Kiho [KR/KR]; (KR) (For US Only).
LEE, Ki Hoon [KR/KR]; (KR) (For US Only).
LEE, Chang Woo [KR/KR]; (KR) (For US Only).
LEE, Jung Joon [KR/KR]; (KR) (For US Only).
CHUNG, Kyung Sook [KR/KR]; (KR) (For US Only).
KIM, Bo Kyung [KR/KR]; (KR) (For US Only).
JIN, Yinglan [CN/KR]; (KR) (For US Only).
LEE, Seung-hee [KR/KR]; (KR) (For US Only)
Inventors: LEE, Kyeong; (KR).
WON, Mi Sun; (KR).
KIM, Hwan Mook; (KR).
PARK, Song Kyu; (KR).
LEE, Kiho; (KR).
LEE, Ki Hoon; (KR).
LEE, Chang Woo; (KR).
LEE, Jung Joon; (KR).
CHUNG, Kyung Sook; (KR).
KIM, Bo Kyung; (KR).
JIN, Yinglan; (KR).
LEE, Seung-hee; (KR)
Agent: LEE, Won Hee; 8th Fl. Sung-ji Heights II 642-16 Yoksam-dong, Kangnam-ku Seoul 135-080 (KR)
Priority Data:
10-2010-0102661 20.10.2010 KR
Title (EN) ARYLOXY PHENOXY ACRYLIC COMPOUND HAVING HIF-1 INHIBITION ACTIVITY, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS AN ACTIVE INGREDIENT
(FR) COMPOSÉ ARYLOXYPHÉNOXYACRYLIQUE AYANT UNE ACTIVITÉ D'INHIBITION DU HIF-1, SON PROCÉDÉ DE PRÉPARATION, ET COMPOSITION PHARMACEUTIQUE LE CONTENANT À TITRE DE PRINCIPE ACTIF
(KO) HIF-1 활성을 저해하는 아릴옥시페녹시아크릴계 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 약학적 조성물
Abstract: front page image
(EN)The present invention relates to a compound having HIF-1 inhibition activity, to a method for preparing same, and to a pharmaceutical composition containing same as an active ingredient. The compound of the present invention exhibits anticancer activity by inhibiting the activity of HIF-1, which is a transcription factor that plays a significant role in cancer cell growth and metastasis, and does not indicate non-selective, cytotoxic anti-tumour activity. Accordingly, the compound or a pharmaceutically acceptable salt thereof according to the present invention inhibits HIF-1 activity, and therefore can be used as a therapeutic agent for solid tumours such as colon cancer, liver cancer, stomach cancer and breast cancer. In addition, the compound or the pharmaceutically acceptable salt thereof according to the present invention can be used as an active ingredient for a therapeutic agent for diabetic retinopathy or arthritis which may become worse when hypoxia-induced VEGF expression by HIF-1 increases.
(FR)Cette invention concerne un composé ayant une activité d'inhibition du HIF-1, un procédé pour le préparer et une composition pharmaceutique le contenant à titre de principe actif. Le composé selon la présente invention manifeste une activité anticancéreuse par inhibition de l'activité du HIF-1, qui est un facteur de transcription qui joue un rôle significatif dans la croissance et la métastase des cellules cancéreuses, et n'indique pas une activité antitumorale cytotoxique, non sélective. Par conséquent, le composé ou un sel de qualité pharmaceutique de celui-ci selon la présente invention inhibe l'activité du HIF-1, et peut, par conséquent, être utilisé à titre d'agent thérapeutique pour traiter les tumeurs solides telles que le cancer du côlon, le cancer du foie, le cancer de l'estomac et le cancer du sein. De plus, le composé ou son sel de qualité pharmaceutique selon la présente invention peut être utilisé à titre de principe actif pour un agent thérapeutique destiné à traiter la rétinopathie diabétique ou l'arthrite qui peuvent empirer quand l'expression par le HIF-1 du VEGF induit par l'hypoxie augmente.
(KO)본 발명은 HIF-1 활성을 저해하는 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 약학적 조성물에 관한 것이다. 본 발명에 따른 화합물은 비선택적인 세포독성에 의해 항암 활성을 나타내는 것이 아니라, 암세포의 성장 및 전이에 중요한 역할을 하는 전사인자인 HIF-1의 활성을 저해하여 항암 활성을 나타낸다. 따라서, 본 발명에 따른 화합물 또는 이의 약학적으로 허용되는 염은 HIF-1 활성을 저해하여 대장암, 간암, 위암 및 유방암 등의 다양한 고형암 질환의 치료제로 사용될 수 있다. 또한, 본 발명에 따른 화합물 또는 이의 약학적으로 허용되는 염은 저산소 상태에서 HIF-1에 의한 VEGF의 발현이 증가되어 악화되는 당뇨병성 망막증이나 관절염 치료제의 유효성분으로 사용될 수 있다.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, 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 (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (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, ML, MR, NE, SN, TD, TG).
Publication Language: Korean (KO)
Filing Language: Korean (KO)