公开(公告)号：US09752151B2

公开(公告)日：2017-09-05

申请号：US14779874

申请日：2014-03-27

申请人： THE ASAN FOUNDATION ,  UNIVERSITY OF ULSAN FOUNDATION FOR INDUSTRY COOPERATION

发明人： Tae Won Kim ,  Dong Hoon Jin ,  Seung Woo Hong ,  Jai Hee Moon ,  Jae Sik Shin ,  Jin Sun Kim ,  Kyung Ah Jung ,  Jung Shin Lee ,  Eun Kyung Choi ,  Jae Lyun Lee ,  Yong Sang Hong ,  Kyu Pyo Kim ,  Ky Youb Nam ,  Bong Cheol Kim

IPC分类号： A01N43/52 ,  A61K31/415 ,  C12N15/113 ,  A61K31/4245 ,  C12Q1/68 ,  G01N33/50 ,  A23L33/13

CPC分类号： C12N15/1137 ,  A23L33/13 ,  A23V2002/00 ,  A61K31/4245 ,  C12N15/113 ,  C12N2310/11 ,  C12N2310/12 ,  C12N2310/122 ,  C12N2310/14 ,  C12N2310/531 ,  C12Q1/6886 ,  C12Q2600/136 ,  C12Q2600/158 ,  G01N33/5011

摘要： The present invention relates to a composition for treatment or metastasis suppression of cancers which includes a p34 expression inhibitor or activity inhibitor as an active ingredient. According to the present invention, the p34 protein knock-down causes monoubiquitination of PTEN and accordingly nuclear localization of PTEN is induced, as a result, an Akt pathway which is related to survival, proliferation, invasive properties and metastatic properties of tumors is inhibited, and thus there is an effect of significantly reducing clonogenic potential and tumor forming potential of various cancer cells which simultaneously express PTEN and NEDD4-1. Consequently, the p34 gene expression inhibitor or p34 protein activity inhibitor according to the present invention can be effectively used as a treatment agent or a metastasis suppression agent for cancers.

公开(公告)号：US20180327851A1

公开(公告)日：2018-11-15

申请号：US15742408

申请日：2016-07-06

申请人： THE ASAN FOUNDATION

发明人： Dong Hoon Jin ,  Seung Woo Hong ,  Jai Hee Moon ,  Jae Sik Shin ,  Seung Mi Kim ,  Dae Hee Lee ,  Eun Young Lee ,  Jung Shin Lee ,  Bong Choel Kim

IPC分类号： C12Q1/6886

摘要： The present invention relates to a method for determining sensitivity to a simultaneous inhibitor against poly ADP ribose polymerase (PARP) and Tankyrase. According to the present invention, a colorectal treatment effect can be maximized by sorting patients having sensitivity to the simultaneous inhibitor against PARP and Tankyrase.

公开(公告)号：US09617261B2

公开(公告)日：2017-04-11

申请号：US14977011

申请日：2015-12-21

申请人： The Asan Foundation

发明人： Gilnam Lee ,  Hye Sun Jeon ,  Ki Joon Jeon ,  Chul Yun Rhim ,  Jin Sung Kim ,  Jeongbeob Seo ,  Suk Young Cho ,  Choung Soo Kim ,  Jung Shin Lee ,  Eun Kyung Choi ,  Jung Jin Hwang ,  Bongcheol Kim

IPC分类号： C07D221/04 ,  C07D471/04 ,  C07D271/10 ,  C07D271/113 ,  C07D413/04

CPC分类号： C07D471/04 ,  C07D221/04 ,  C07D271/10 ,  C07D271/113 ,  C07D413/04

摘要： The invention provides novel substituted heterocyclic compounds represented by Formula I and Formula II, or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of MEK and are useful in the treatment of inflammatory diseases, cancer and other hyperproliferative diseases. The invention further provides a method of treatment for inflammatory diseases, cancer and other hyperproliferative diseases in mammals, especially humans.

公开(公告)号：US20160040168A1

公开(公告)日：2016-02-11

申请号：US14779874

申请日：2014-03-27

申请人： THE ASAN FOUNDATION ,  UNIVERSITY OF ULSAN FOUNDATION FOR INDUSTRY COOPERATION

发明人： Tae Won Kim ,  Dong Hoon Jin ,  Seung Woo Hong ,  Jai Hee MOON ,  Jae Sik Shin ,  Jin Sun Kim ,  Kyung Ah Jung ,  Jung Shin Lee ,  Eun Kyung Choi ,  Jae Lyun Lee ,  Yong Sang Hong ,  Kyu Pyo Kim ,  Ky Youb Nam ,  Bong Cheol Kim

IPC分类号： C12N15/113 ,  A23L1/30 ,  G01N33/50 ,  A61K31/4245 ,  C12Q1/68

CPC分类号： C12N15/1137 ,  A23L33/13 ,  A23V2002/00 ,  A61K31/4245 ,  C12N15/113 ,  C12N2310/11 ,  C12N2310/12 ,  C12N2310/122 ,  C12N2310/14 ,  C12N2310/531 ,  C12Q1/6886 ,  C12Q2600/136 ,  C12Q2600/158 ,  G01N33/5011

摘要： The present invention relates to a composition for treatment or metastasis suppression of cancers which includes a p34 expression inhibitor or activity inhibitor as an active ingredient. According to the present invention, the p34 protein knock-down causes monoubiquitination of PTEN and accordingly nuclear localization of PTEN is induced, as a result, an Akt pathway which is related to survival, proliferation, invasive properties and metastatic properties of tumors is inhibited, and thus there is an effect of significantly reducing clonogenic potential and tumor forming potential of various cancer cells which simultaneously express PTEN and NEDD4-1. Consequently, the p34 gene expression inhibitor or p34 protein activity inhibitor according to the present invention can be effectively used as a treatment agent or a metastasis suppression agent for cancers.

摘要翻译： 本发明涉及包含p34表达抑制剂或活性抑制剂作为活性成分的癌症治疗或转移抑制组合物。 根据本发明，p34蛋白敲低引起PTEN的单泛素化，因此诱导PTEN的核定位，结果与抑制肿瘤的存活，增殖，侵袭性质和转移性质有关的Akt途径， 因此具有显着降低同时表达PTEN和NEDD4-1的各种癌细胞的克隆潜能和肿瘤形成潜力的作用。 因此，本发明的p34基因表达抑制剂或p34蛋白活性抑制剂可以有效地用作癌症的治疗剂或转移抑制剂。

公开(公告)号：US10683553B2

公开(公告)日：2020-06-16

申请号：US15742408

申请日：2016-07-06

申请人： THE ASAN FOUNDATION

发明人： Dong Hoon Jin ,  Seung Woo Hong ,  Jai Hee Moon ,  Jae Sik Shin ,  Seung Mi Kim ,  Dae Hee Lee ,  Eun Young Lee ,  Jung Shin Lee ,  Bong Choel Kim

IPC分类号： C12Q1/68 ,  C12Q1/6886

摘要： The present invention relates to a method for determining sensitivity to a simultaneous inhibitor against poly ADP ribose polymerase (PARP) and Tankyrase. According to the present invention, a colorectal treatment effect can be maximized by sorting patients having sensitivity to the simultaneous inhibitor against PARP and Tankyrase.

公开(公告)号：US20160108041A1

公开(公告)日：2016-04-21

申请号：US14977011

申请日：2015-12-21

申请人： The Asan Foundation

发明人： Gilnam Lee ,  Hye Sun Jeon ,  Ki Joon Jeon ,  Chul Yun Rhim ,  Jin Sung Kim ,  Jeongbeob Seo ,  Suk Young Cho ,  Choung Soo Kim ,  Jung Shin Lee ,  Eun Kyung Choi ,  Jung Jin Hwang ,  Bongcheol Kim

IPC分类号： C07D471/04 ,  C07D413/04 ,  C07D221/04

CPC分类号： C07D471/04 ,  C07D221/04 ,  C07D271/10 ,  C07D271/113 ,  C07D413/04

摘要： The invention provides novel substituted heterocyclic compounds represented by Formula I and Formula II, or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of MEK and are useful in the treatment of inflammatory diseases, cancer and other hyperproliferative diseases. The invention further provides a method of treatment for inflammatory diseases, cancer and other hyperproliferative diseases in mammals, especially humans.

摘要翻译： 本发明提供由式I和式II表示的新型取代的杂环化合物或其药学上可接受的盐，溶剂合物，多晶型物，酯，互变异构体或前药，以及包含这些化合物的组合物。 所提供的化合物可用作MEK的抑制剂，并且可用于治疗炎性疾病，癌症和其它过度增生性疾病。 本发明还提供了一种治疗哺乳动物，特别是人类的炎性疾病，癌症和其它过度增生性疾病的方法。