US 8,940,936 B2 · Aryloxy phenoxy acrylic compound having HIF-1 inhibition activity, method for preparing same, and pharmaceutical composition containing same as an active ingredient

Aryloxy phenoxy acrylic compound having HIF-1 inhibition activity, method for preparing same, and pharmaceutical composition containing same as an active ingredient

AssigneesKorea Research Institute of Bioscience and Biotechnology, Dongguk University Industry-Academic Cooperation Foundation

InventorsKyeong Lee, Mi Sun Won, Hwan Mook Kim, Song Kyu Park, Kiho Lee, Ki Hoon Lee, Chang Woo Lee, Jung Joon Lee, Kyung Sook Chung, Bo Kyung Kim, Yinglan Jin, Seung-hee Lee

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Abstract

The present invention relates to a compound inhibiting HF-1 activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention demonstrates anticancer activity not by non-selective cytotoxicity but by inhibiting the activity of HIF-1, the transcription factor playing an important role in cancer cell growth and metastasis. Accordingly, the compound or the pharmaceutically acceptable salt thereof according to the present invention inhibits HIF-1 activity, and therefore can be used as a therapeutic agent for solid tumors 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.

Claims19

Dependent claims

A compound represented by the following formula 1 or a pharmaceutically acceptable salt thereof:

(In the formula 1,
R1 is C1-10 straight or branched alkyl, or C8-12 bicyclic ring,
R2 is —H, COOR5, COOR5R6, —SO2NH2, —SO2—(C1-4 straight or branched alkyl), or —CONHR7,
R3 is —H, —OH, or —COO—(C1-4 straight or branched alkyl),
R4 is —H, or C1-4 straight or branched alkyl,
R5 is —H, C1-4 straight or branched alkyl, or C1-4 alkoxy,
R6 is —NH2, or 5-6 membered heterocycle containing one or more N or O,
R7 is —H, or —(CH2)n—R8,
R8 is —H, 5-6 membered heteroaryl containing one or more N or O, or 5-6 membered heterocycle containing one or more N or O, and
n is an integer of 0-4).

7 more elements

Dependencies are inferred from the claim text.

Facts

Application

13/880,642Filed 17 Oct 2011

Priority

KR 10-2010-010266120 Oct 2010

Published

US 2013/0237542 A112 Sep 2013

Granted

27 Jan 2015

Term ends

Not estimatedThe source records don’t support an estimate.

Classification25 codes

A61K 31/5375
Having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines: 1,4-Oxazines, e.g. morpholine
A61K 9/0019
Galenical forms characterised by the site of application: injectable compositions; Intramuscular, intravenous, arterial, subcutaneous…
A61K 9/08
Medicinal preparations characterised by special physical form: solutions
A61K 9/14
Medicinal preparations characterised by special physical form: particulate form, e.g. powders, Processes for size reducing of pure drugs or the…