IP Library › Granted Patent US 9,266,872
Granted Patent B2
US 9,266,872 · App. 14/256,808 · Granted Feb 23, 2016

2-hydroxyarylamide derivative or pharmaceutically acceptable salt thereof, preparation method thereof, and pharmaceutical composition for preventing or treating cancer containing same as active ingredient

Inventors: Semi Kim (Daejeon, KR); Ill Young Lee (Daejeon, KR); Hye-Jin Min (Daejeon, KR); Eun-Hee Nam (Daejeon, KR); Pilho Kim (Daejeon, KR); Chang Soo Yun (Daejeon, KR); Dong Joon Ko (Daejeon, KR)
Assignee: Korea Research Institute of Bioscience and Biotechnology
C07D417/04A61K31/167A61K31/426A61K31/428A61K31/433A61K31/44A61K31/4439A61K31/4709A61K31/505A61K31/5377C07D213/75C07D213/82C07D215/38C07D215/56C07D239/42C07D277/46C07D277/82C07D285/135
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Quick Facts
Patent No.
US 9,266,872
App. No.
14/256,808
Granted
Feb 23, 2016
Kind
B2
Abstract

The present invention relates to a 2-hydroxyarylamide derivative or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition for preventing or treating cancer comprising the same as an active ingredient. The 2-hydroxyarylamide derivative prepared by the present invention is excellent in the inhibition of the activity of TMPRSS4 serine protease and the suppression of the infiltration of TMPRSS4-expressed cancer cells, and thus can be useful as a composition for preventing or treating cancer by inhibiting TMPRSS4 over-expressed in cancer cells, particularly, colorectal cancer, lung cancer, breast cancer, prostate cancer, ovarian cancer, pancreatic cancer, or stomach cancer cells.

Claims (12)

1. A method for inhibiting colorectal cancer metastasis comprising: administrating a pharmaceutically effective dose of a 2-hydroxyarylamide derivative or a pharmaceutically acceptable salt thereof, wherein the 2-hydroxyarylamide derivative is selected from the group consisting of:

(6) 5-chloro-2-hydroxy-N-(3-methoxy-5-(trifluoromethyl)phenyl)benzamide;

(19) 5-chloro-N-(4-cyano-3-(trifluoromethyl)phenyl)-2-hydroxybenzamide;

(25) 5-chloro-2-hydroxy-N-quinoline-3-yl-benzamide;

(27) 5-chloro-N-(2-chloro-4-cyano-phenyl)-2-hydroxy-benzamide;

(28) 5-chloro-2-hydroxy-N-(5-trifluoromethyl-[1,3,4]thiadiazole-2-yl)-benzamide;

(32) 5-chloro-N-(4-chloro-3-(trifluoromethyl)phenyl)-2-hydroxybenzamide;

(36) 5-chloro-2-hydroxy-N-(2-nitro-4-trifluoromethyl-phenyl)-benzamide;

(37) 5-chloro-N-(5-cyano-pyridine-2-yl)-2-hydroxy-benzamide; and

(53) 5-chloro-2-hydroxy-N-(4-phenylthiazole-2-yl)benzamide;

wherein the 2-hydroxyarylamide derivative or a pharmaceutically acceptable salt thereof inhibits the activity of TMPRSS4 (transmembrane protease serine-4).

2. The method of claim 1 , wherein the 2-hydroxyarylamide derivative or a pharmaceutically acceptable salt thereof is administered orally or parenterally.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 1, 2014
From: KIM, SEMI; LEE, ILL YOUNG; MIN, HYE-JIN; NAM, EUN-HEE; KIM, PILHO; YUN, CHANG SOO; KO, DONG JOON
To: KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY
Reel/Frame 032798/0880 →
Priority Claims (2)
KR 10-2011-0107934 · Oct 21, 2011 · national
KR 10-2012-0116733 · Oct 19, 2012 · national
Continuity (2)
Continuation In Part PCTKR2012008626 · Oct 19, 2012
Related Publication 20140221411A1 · Aug 7, 2014