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.

公开(公告)号：US08940936B2

公开(公告)日：2015-01-27

申请号：US13880642

申请日：2011-10-17

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： C07C233/07 ,  A61K31/167 ,  C07C235/28 ,  C07C311/16 ,  C07D295/088

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.

摘要翻译： 本发明涉及抑制HF-1活性的化合物，其制备方法以及含有该化合物作为活性成分的药物组合物。 本发明的化合物通过非选择性细胞毒性表现出抗癌活性，但通过抑制HIF-1的活性，该转录因子在癌细胞生长和转移中起重要作用。 因此，根据本发明的化合物或其药学上可接受的盐抑制HIF-1活性，因此可以用作结肠癌，肝癌，胃癌和乳腺癌等实体瘤的治疗剂。 此外，根据本发明的化合物或其药学上可接受的盐可以用作用于糖尿病性视网膜病变或关节炎的治疗剂的活性成分，当HIF-1的缺氧诱导的VEGF表达增加时，可能变差。

公开(公告)号：US20130237542A1

公开(公告)日：2013-09-12

申请号：US13880642

申请日：2011-10-17

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： C07C235/28 ,  C07D295/088 ,  C07C311/16

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.

摘要翻译： 本发明涉及抑制HF-1活性的化合物，其制备方法以及含有该化合物作为活性成分的药物组合物。 本发明的化合物通过非选择性细胞毒性表现出抗癌活性，但通过抑制HIF-1的活性，该转录因子在癌细胞生长和转移中起重要作用。 因此，根据本发明的化合物或其药学上可接受的盐抑制HIF-1活性，因此可以用作结肠癌，肝癌，胃癌和乳腺癌等实体瘤的治疗剂。 此外，根据本发明的化合物或其药学上可接受的盐可以用作用于糖尿病性视网膜病变或关节炎的治疗剂的活性成分，当HIF-1的缺氧诱导的VEGF表达增加时，可能变差。