公开(公告)号：EP3360870A1

公开(公告)日：2018-08-15

申请号：EP18156411.3

申请日：2014-02-12

申请人： Novartis AG

发明人： BURKS, Heather Elizabeth ,  DECHANTSREITER, Michael A. ,  HE, Guo ,  NUNEZ, Jill ,  PEUKERT, Stefan ,  SPRINGER, Clayton ,  SUN, Yingchuan ,  THOMSEN, Noel Marie-France ,  TRIA, George Scott ,  YU, Bing

IPC分类号： C07D333/64 ,  C07D333/66 ,  C07D409/04 ,  C07D409/10 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  A61K31/381 ,  A61P35/00

CPC分类号： A61K31/381 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/4436 ,  A61K31/4745 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61P35/00 ,  C07D333/64 ,  C07D333/66 ,  C07D409/04 ,  C07D409/10 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates to compounds of formula I:

in which n, m, X, Y 1 , R 1 , R 2 , R 3 , R 4 and R 5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.

公开(公告)号：EP2958907A1

公开(公告)日：2015-12-30

申请号：EP14708992.4

申请日：2014-02-12

申请人： Novartis AG

发明人： BURKS, Heather Elizabeth ,  DECHANTSREITER, Michael A. ,  HE, Guo ,  NUNEZ, Jill ,  PEUKERT, Stefan ,  SPRINGER, Clayton ,  SUN, Yingchuan ,  THOMSEN, Noel Marie-France ,  TRIA, George Scott ,  YU, Bing

IPC分类号： C07D333/64 ,  C07D333/66 ,  C07D409/04 ,  C07D409/10 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  A61K31/381 ,  A61P35/00

CPC分类号： A61K31/381 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/4436 ,  A61K31/4745 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61P35/00 ,  C07D333/64 ,  C07D333/66 ,  C07D409/04 ,  C07D409/10 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates to compounds of formula I: in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.

摘要翻译： 本发明涉及式I化合物：其中n，m，X，Y 1，R 1，R 2，R 3，R 4和R 5在本发明概述中定义; 能够成为雌激素受体的有效拮抗剂和降解物。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂以及使用这些化合物和组合物来管理与异常雌激素受体活性相关的疾病或病症的方法。

公开(公告)号：EP2958907B1

公开(公告)日：2018-02-28

申请号：EP14708992.4

申请日：2014-02-12

申请人： Novartis AG

发明人： BURKS, Heather Elizabeth ,  DECHANTSREITER, Michael A. ,  HE, Guo ,  NUNEZ, Jill ,  PEUKERT, Stefan ,  SPRINGER, Clayton ,  SUN, Yingchuan ,  THOMSEN, Noel Marie-France ,  TRIA, George Scott ,  YU, Bing

IPC分类号： C07D333/64 ,  C07D333/66 ,  C07D409/04 ,  C07D409/10 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  A61K31/381 ,  A61P35/00

CPC分类号： A61K31/381 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/4436 ,  A61K31/4745 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61P35/00 ,  C07D333/64 ,  C07D333/66 ,  C07D409/04 ,  C07D409/10 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates to compounds of formula I: in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.