公开(公告)号：EP4291195A1

公开(公告)日：2023-12-20

申请号：EP22753443.5

申请日：2022-02-11

申请人： The Medical College of Wisconsin, Inc.

发明人： SHISHODIA, Shifali ,  GOETZ, Christopher J. ,  OLP, Michael D. ,  SMITH, Brian Christopher

IPC分类号： A61K31/517 ,  C07D239/88 ,  C07D239/91 ,  A61P35/00

公开(公告)号：EP4087575A1

公开(公告)日：2022-11-16

申请号：EP21738197.9

申请日：2021-01-07

申请人： Resverlogix Corp.

发明人： LEBIODA, Kenneth, Eugene ,  HALLIDAY, Christopher, Ross Armstrong ,  KHAN, Aziz, Naeem

IPC分类号： A61K31/517 ,  A61K31/40 ,  A61K31/403 ,  A61K31/427 ,  A61K31/4985 ,  A61K31/513 ,  A61K31/522 ,  A61K38/095 ,  A61P9/00 ,  A61P9/10 ,  C07D207/16 ,  C07D209/52 ,  C07D239/91 ,  C07D401/04 ,  C07D417/14 ,  C07D473/06 ,  C07D487/04

公开(公告)号：EP4008717A2

公开(公告)日：2022-06-08

申请号：EP21211967.1

申请日：2021-12-02

申请人： Martin-Luther-Universität Halle-Wittenberg

发明人： HÜTTELMAIER, Stefan ,  MÜLLER, Simon ,  BLEY, Nadine ,  DAILEN, Garcia Martinez ,  SIPPL, Wolfgang ,  GHAZY, Ehab

IPC分类号： C07D333/28 ,  C07D333/38 ,  C07D239/91 ,  C07D495/04 ,  C07D417/12 ,  C07D409/06 ,  C07C237/42 ,  C07C237/30 ,  C07C233/00 ,  C07D295/15 ,  C07D333/78 ,  C07D333/68 ,  C07D409/12 ,  A61P35/00 ,  A61K31/381 ,  A61K31/517 ,  A61K31/519 ,  A61K31/495

摘要： The presented invention provides compounds of formula (I) and (VIII),


or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein R 1 , R 2 , W, X, Y, Z, m, n and o are as defined herein. Said compounds of formula (I) are inhibitors of insulin-like growth factor 2 mRNA binding proteins (IGF2BP). Provided are novel inhibitors of IGF2BPs and processes for manufacturing the same. Efficacy of the new compounds is shown in solid cancer models.

公开(公告)号：EP3681874B1

公开(公告)日：2022-04-06

申请号：EP18856020.5

申请日：2018-09-12

发明人： LU, Bingwei

IPC分类号： C07D239/91 ,  A61K31/517 ,  C07D239/95

公开(公告)号：EP3624804B1

公开(公告)日：2022-02-16

申请号：EP18801840.2

申请日：2018-05-15

发明人： CHERN, Ji-Wang ,  YU, Chao-Wu ,  LIU, Jia-Rong ,  HO, Yi-Hsun ,  WU, Chia-Yu ,  HUANG, Chan-Hui ,  HUNG, Pei-Yun

IPC分类号： A61K31/517 ,  C07D239/88 ,  C07D239/91 ,  C07D239/96

公开(公告)号：EP3094332B1

公开(公告)日：2018-09-12

申请号：EP15737924.9

申请日：2015-01-14

申请人： The Trustees of Columbia University in the City of New York

发明人： STOCKWELL, Brent, R. ,  YANG, Wan, Seok ,  LARRAUFIE, Marie-Helene

IPC分类号： A61K31/517 ,  C07D239/88 ,  C07D239/91

CPC分类号： C07D239/91 ,  C07D239/88 ,  C07D403/10

摘要： The present invention provides, inter alia, compounds having the structure of formula (I): Compositions containing such compounds are also provided. Methods for using such compounds or compositions for treating or ameliorating the effects of a cancer having a cell that harbors an oncogenic RAS mutation, for modulating a lipoxygenase in a ferroptosis cell death pathway, and for depleting reduced glutathione (GSH) in a cell harboring an oncogenic RAS mutation are further provided.

公开(公告)号：EP3348548A1

公开(公告)日：2018-07-18

申请号：EP16843639.2

申请日：2016-09-06

申请人： Zhejiang Huahai Pharmaceutical Co., Ltd ,  Shanghai Synergy Pharmaceutical Sciences Co., Ltd

发明人： GE, Jian ,  LI, Yunfei ,  ZHANG, Zhen ,  WANG, Yijin ,  WANG, Jiamiao ,  CHENG, Tao

IPC分类号： C07D239/91 ,  C07D217/24 ,  A61K31/517 ,  A61P9/00

CPC分类号： A61K31/5355 ,  A61K31/4418 ,  A61K31/517 ,  A61K31/519 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P25/28 ,  C07D217/24 ,  C07D239/91

摘要： Provided are a type of compounds that can be used for treating cardiovascular diseases and compositions containing the compounds. The compounds and the compositions can improve lipid metabolism disorders by increasing high-density lipoprotein cholesterol in blood; in addition, the compounds and the compositions can also release nitric oxide, and reduce the onset risk of cardiovascular diseases by means of relaxing blood vessels, lowering blood pressure, inhibiting platelet adhesion and aggregation and maintaining vascular tension, and thus play an important role in preventing and treating the occurrence and development of cardiovascular diseases.

公开(公告)号：EP3334725A1

公开(公告)日：2018-06-20

申请号：EP16835823.2

申请日：2016-08-10

申请人： Dana-Farber Cancer Institute, Inc.

发明人： POLYAK, Kornelia ,  SHU, Shaokun ,  BRADNER, James E. ,  LIN, Charles Yang

IPC分类号： C07D401/14 ,  A61K31/517 ,  C07D239/91

CPC分类号： A61K31/635 ,  A61K31/137 ,  A61K31/5415 ,  A61K31/551 ,  A61K45/06 ,  C07D215/42 ,  C07D255/04 ,  C07D471/04 ,  C07D495/14 ,  G01N33/6872 ,  G01N2800/52 ,  A61K2300/00

摘要： The present disclosure provides combination therapy comprising a BET inhibitor and a protein phosphatase 2A (PP2A) activator, a B-cell lymphoma-2 (Bcl-2) inhibitor, a B-cell lymphoma-extra large (Bcl-xl) inhibitor, a casein kinase 2 (CK2) inhibitor, and/or a mediator complex subunit 1 (MEDl) for cancer. The combination therapy is expected to be synergistic in treating the cancer, compared to the monotherapy. Methods for identifying a subject having a cancer that is resistant to or at risk of developing resistance to bromodomain and extra terminal (BET) inhibitor therapy are also provided.

公开(公告)号：EP2900643B1

公开(公告)日：2017-09-27

申请号：EP13756318.5

申请日：2013-08-27

申请人： Merck Patent GmbH

发明人： DORSCH, Dieter ,  BUCHSTALLER, Hans-Peter

IPC分类号： C07D239/91 ,  A61K31/517 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  C07D401/10 ,  C07D403/10 ,  C07D417/10

CPC分类号： C07D239/91 ,  A61K31/517 ,  A61K31/541 ,  A61K31/551 ,  C07D401/04 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D417/10

公开(公告)号：EP3094332A4

公开(公告)日：2017-06-14

申请号：EP15737924

申请日：2015-01-14

申请人： UNIV COLUMBIA

发明人： STOCKWELL BRENT R ,  YANG WAN SEOK ,  LARRAUFIE MARIE-HELENE

IPC分类号： A61K31/517 ,  C07D239/88 ,  C07D239/91

CPC分类号： C07D239/91 ,  C07D239/88 ,  C07D403/10

摘要： The present invention provides, inter alia, compounds having the structure of formula (I): Compositions containing such compounds are also provided. Methods for using such compounds or compositions for treating or ameliorating the effects of a cancer having a cell that harbors an oncogenic RAS mutation, for modulating a lipoxygenase in a ferroptosis cell death pathway, and for depleting reduced glutathione (GSH) in a cell harboring an oncogenic RAS mutation are further provided.

摘要翻译： 本发明尤其提供具有式（I）结构的化合物：还提供含有这些化合物的组合物。 使用这些化合物或组合物来治疗或改善具有致癌基因RAS突变的细胞的作用，用于调节加铁细胞死亡途径中的脂肪氧合酶的作用，以及用于消耗含有病毒的细胞的还原型谷胱甘肽（GSH）的作用的方法 进一步提供致癌RAS突变。