公开(公告)号：US20170239259A1

公开(公告)日：2017-08-24

申请号：US14569201

申请日：2014-12-12

申请人： Kyeong 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

发明人： Kyeong 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

IPC分类号： A61K31/5375 ,  A61K31/167 ,  A61K31/196 ,  A61K31/40 ,  A61K31/34 ,  A61K9/08 ,  A61K31/417 ,  A61K9/00 ,  A61K9/14 ,  A61K9/20 ,  A61K9/48 ,  A61K31/24 ,  A61K31/4409

CPC分类号： A61K31/5375 ,  A61K9/0019 ,  A61K9/08 ,  A61K9/14 ,  A61K9/20 ,  A61K9/48 ,  A61K31/167 ,  A61K31/196 ,  A61K31/24 ,  A61K31/34 ,  A61K31/40 ,  A61K31/417 ,  A61K31/4409 ,  C07C233/07 ,  C07C235/28 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C2603/74 ,  C07D295/088

摘要： 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.