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Title:
ARYLOXYPHENOXYACETYL-BASED COMPOUND HAVING HIF-1 INHIBITION ACTIVITY, PREPARATION METHOD THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME AS AN ACTIVE INGREDIENT
Document Type and Number:
WIPO Patent Application WO/2012/053768
Kind Code:
A2
Abstract:
Disclosed are a compound inhibitory of HIF-1 activity, a method for preparing the same, and a pharmaceutical composition comprising the same as an active ingredient. The compound has anticancer activity which is attributable to its inhibitory activity against HIF-1, but not to non-selective cellular toxicity. Thus, having inhibitory activity against HIF-1, the compound or a pharmaceutically acceptable salt thereof can be used as an ingredient in an anticancer agent for various cancers including large intestine cancer, hepatic cancer, stomach cancer and breast cancer. Further, the compound or a pharmaceutically acceptable salt thereof is applicable to the treatment of diabetic retinopathy or arthritis which is aggravated upon the activation of VEGFA by HIF-1.

Inventors:
WON MI-SUN (KR)
KIM HWAN-MOOK (KR)
LEE KYEONG (KR)
PARK SONG-KYU (KR)
LEE KI-HO (KR)
LEE CHANG-WOO (KR)
LEE JUNG-JOON (KR)
CHUNG KYUNG-SOOK (KR)
KIM BO-KYUNG (KR)
JIN YING-LAN (KR)
Application Number:
PCT/KR2011/007589
Publication Date:
April 26, 2012
Filing Date:
October 12, 2011
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Assignee:
KOREA RES INST OF BIOSCIENCE (KR)
UNIV DONGGUK IND ACAD COOP (KR)
WON MI-SUN (KR)
KIM HWAN-MOOK (KR)
LEE KYEONG (KR)
PARK SONG-KYU (KR)
LEE KI-HO (KR)
LEE CHANG-WOO (KR)
LEE JUNG-JOON (KR)
CHUNG KYUNG-SOOK (KR)
KIM BO-KYUNG (KR)
JIN YING-LAN (KR)
International Classes:
C07C235/38; A61K31/167; A61P35/00; C07C231/02
Domestic Patent References:
WO2008004798A12008-01-10
Other References:
SHANTHAVEERAPPA K. BOOVANAHALLI ET AL.: 'Synthesis of (aryloxyacetylamino)-i sonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF) -1 alpha inhibitors' BIOORGANIC & MEDICINAL CHEMISTRY LETTERS vol. 17, no. 22, 2007, pages 5376 - 5379
JAE YOON CHUNG ET AL.: 'Pharmacophore-based 3D-QSAR of HIF-1 Inhibitors' AR CH. PHARM. RES.. vol. 32, no. 3, 2009, pages 317 - 323
KYEONG LEE ET AL.: 'LW6, a novel HIF-1 inhibitor, promotes proteasomal degra dation of HIF-l avia upregulation of VHL in a colon cancer cell line' BIOCHE MICAL PHARMACOLOGY vol. 80, no. 7, 23 June 2010, pages 982 - 989
Attorney, Agent or Firm:
ROH, Jae-Chull (4F. Halla Building,641-17, Yeoksam-dong, Gangnam-gu, Seoul 135-909, KR)
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Claims: