KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY
发明人:
KIM, Semi,김세미,LEE, Ill Young,이일영,MIN, Hye-Jin,민혜진,NAM, Eun-Hee,남은희,KIM, Pilho,김필호,YUN, Chang Soo,윤창수
申请号：
KRKR2012/008626
公开号：
WO2013/058613A2
申请日:
2012.10.19
申请国别(地区):
WO
年份:
2013
代理人:
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 containing 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 invasion of TMPRSS4-expressed cancer cells, and thus can be useful as a composition for preventing or treating cancer by inhibiting TMPRSS4 overexpressed in cancer cells, particularly, colorectal cancer, lung cancer, breast cancer, prostate cancer, ovarian cancer, pancreatic cancer, or stomach cancer cells.La présente invention concerne un dérivé de 2-hydroxyarylamide ou un sel de qualité pharmaceutique de celui-ci, un procédé de préparation de celui-ci et une composition pharmaceutique le contenant comme principe actif pour la prévention ou le traitement du cancer. Le dérivé de 2-hydroxyarylamide préparé selon la présente invention est excellent dans linhibition de lactivité dune sérine protéase TMPRSS4 et linhibition de linvasion de cellules cancéreuses exprimant TMPRSS4, et par conséquent peut être utile comme composition pour la prévention ou le traitement du cancer par linhibition de TMPRSS4 surexprimé dans des cellules cancéreuses, en particulier dans des cellules du cancer colorectal, du cancer du poumon, du cancer du sein, du cancer de la prostate, du cancer de lovaire, du cancer du pancréas ou du cancer de lestomac.본 발명은 2-하이드록시아릴아마이드 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 암 예방 또는 치료용 약학적 조성물에 관한 것이다. 본 발명에 의해 제조된 2-하이드록시아릴아마이드 유도체 화합물은 TMPRSS4 세린프로테아제 활성 저해 효과와 TMPRSS4 발현 암세포 침윤 억제효과가 매우 우수하므로 암 세포, 특히, 대장암, 폐암, 유방암, 전립선암, 난소암, 췌장암 또는 위암 세포 등에서 과발현되는 TMPRSS4를 저해함으로써, 암의 예방 또는 치료용 조성물로 유용하게 사용될 수 있다.
