Difluorocarbene radiosynthesis
US-2024383827-A1 · Nov 21, 2024 · US
US9266872B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9266872-B2 |
| Application number | US-201414256808-A |
| Country | US |
| Kind code | B2 |
| Filing date | Apr 18, 2014 |
| Priority date | Oct 21, 2011 |
| Publication date | Feb 23, 2016 |
| Grant date | Feb 23, 2016 |
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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.
Opening claim text (preview).
What is claimed is: 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.
Non-condensed quinolines and containing further heterocyclic rings · CPC title
condensed with carbocyclic rings · CPC title
1,3-Thiazoles · CPC title
in position 3 · CPC title
Nitrogen atoms · CPC title
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