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1. (WO2011145777) PHARMACEUTICAL COMPOSITION INCLUDING AN HIF-2Α INHIBITOR AS AN ACTIVE INGREDIENT FOR PREVENTING OR TREATING ARTHRITIS
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2011/145777    International Application No.:    PCT/KR2010/005889
Publication Date: 24.11.2011 International Filing Date: 31.08.2010
IPC:
A61K 38/16 (2006.01), A61K 31/7105 (2006.01), A61P 19/00 (2006.01)
Applicants: GWANGJU INSTITUTE OF SCIENCE AND TECHNOLOGY [KR/KR]; 261 Cheomdan-gwagiro(1 Oryong-dong), Buk-gu Gwangju 500-712 (KR) (For All Designated States Except US).
CHUN, Jang-Soo [KR/KR]; (KR) (For US Only).
YANG, Si Young [KR/KR]; (KR) (For US Only)
Inventors: CHUN, Jang-Soo; (KR).
YANG, Si Young; (KR)
Agent: YANG, Boo-Hyun; Suite 301 Chungdong Building 1659-2 Inhundong, Gwanak-gu Seoul 151-832 (KR)
Priority Data:
10-2010-0047485 20.05.2010 KR
Title (EN) PHARMACEUTICAL COMPOSITION INCLUDING AN HIF-2Α INHIBITOR AS AN ACTIVE INGREDIENT FOR PREVENTING OR TREATING ARTHRITIS
(FR) COMPOSITION PHARMACEUTIQUE COMPRENANT UN INHIBITEUR DE HIF-2Α COMME INGRÉDIENT ACTIF POUR LA PRÉVENTION OU LE TRAITEMENT DE L'ARTHRITE
(KO) HIF-2α 억제제를 유효성분으로 포함하는 관절염 예방 또는 치료용 약제학적 조성물
Abstract: front page image
(EN)The present invention relates to a pharmaceutical composition for preventing or treating arthritis, including, as an active ingredient, a material which inhibits the expression of the hypoxia-inducible factor-2α (HIF-2α) gene or the activity of the HIF-2α protein. According to the present invention, the HIF-2α of the present invention increases the expression thereof in chondrocytes or tissue in which osteoarthritis is induced, and triggers the expression of various cartilage degeneration factors and the activation of mitogen-activated protein (MAP) kinase. In addition, when HIF-2α is inhibited, the expression level of cartilage degeneration factors and the phosphorylation of MAP kinase are significantly reduced by the inhibited degree of HIF-2α. Thus, the composition of the present invention may be applied to the prevention or treatment of arthritis, and may be used for the development of therapeutics for arthritis.
(FR)La présente invention concerne une composition pharmaceutique pour la prévention ou le traitement de l'arthrite, comprenant, comme ingrédient actif, une substance qui inhibe l'expression du gène du facteur 2α pouvant être induit par l'hypoxie (HIF-2α) ou l'activité de la protéine HIF-2α. Selon la présente invention, le HIF-2α de la présente invention augmente l'expression de celui-ci dans les chondrocytes ou les tissus dans lesquels l'ostéoarthrite est induite et déclenche l'expression de différents facteurs de dégénérescence du cartilage et l'activation de la protéine activée par la mitogène (MAP)-kinase. En outre, lorsque le HIF-2α est inhibé, le niveau d'expression de facteurs de dégénérescence du cartilage et la phosphorylation de la MAP kinase sont significativement réduits par le degré d'inhibition de HIF-2α. Par conséquent, la composition de la présente invention peut être appliquée à la prévention ou au traitement de l'arthrite et peut être utilisée pour le développement d'agents thérapeutiques de l'arthrite.
(KO)본 발명은 HIF-2α(hypoxia-inducible factor-2α) 유전자의 발현을 억제하거나, 또는 HIF-2α 단백질의 활성을 억제하는 물질을 유효성분으로 포함하는 관절염 예방 또는 치료용 약제학적 조성물에 관한 것이다. 본 발명에 따르면, 본 발명의 HIF-2α은 골관절염이 유도된 연골세포 또는 조직에서 발현이 증가하고, 다양한 연골퇴행 유발인자의 발현 및 MAP(mitogen-activated protien) 키나제의 활성화를 촉발시킨다. 또한, 본 발명의 HIF-2α를 억제하는 경우, 연골퇴행 유발인자의 발현 레벨 및 MAP 키나제의 인산화가 HIF-2α의 억제 정도에 따라 현저하게 감소하였다. 따라서, 본 발명의 조성물은 관절염의 예방 또는 치료에 적용될 수 있으며, 이를 이용하여 관절염 치료제의 개발에도 이용될 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, RO, RS, RU, 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, 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, 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)