公开(公告)号：US20140221411A1

公开(公告)日：2014-08-07

申请号：US14256808

申请日：2014-04-18

申请人： Korea Research Institute of Bioscience and Biotechnology

发明人： Semi KIM ,  Ill Young LEE ,  Hye-Jin MIN ,  Eun-Hee NAM ,  Pilho KIM ,  Chang Soo YUN ,  Dong Joon KO

IPC分类号： C07C235/64 ,  C07D215/38 ,  C07D285/135 ,  C07D213/75 ,  C07D417/04 ,  C07D277/46 ,  C07D213/82 ,  C07D215/56 ,  C07D277/82 ,  C07C235/66 ,  C07D239/42

CPC分类号： C07D417/04 ,  A61K31/167 ,  A61K31/426 ,  A61K31/428 ,  A61K31/433 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/505 ,  A61K31/5377 ,  C07D213/75 ,  C07D213/82 ,  C07D215/38 ,  C07D215/56 ,  C07D239/42 ,  C07D277/46 ,  C07D277/82 ,  C07D285/135

摘要： 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.

摘要翻译： 本发明涉及2-羟基芳基酰胺衍生物或其药学上可接受的盐，其制备方法和用于预防或治疗癌症的药物组合物，其包含其作为活性成分。 通过本发明制备的2-羟基芳基酰胺衍生物对TMPRSS4丝氨酸蛋白酶的活性的抑制和TMPRSS4表达的癌细胞的浸润的抑制是优异的，因此可以用作通过抑制来预防或治疗癌症的组合物 TMPRSS4在癌细胞，特别是结肠直肠癌，肺癌，乳腺癌，前列腺癌，卵巢癌，胰腺癌或胃癌细胞中过度表达。