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1.发明申请公开(公告)号：US20160184265A1
公开(公告)日：2016-06-30
申请号：US15066425
申请日：2016-03-10
申请人： Heather Elizabeth BURKS , Michael A. DECHANTSREITER , Guo HE , Jill NUNEZ , Stefan PEUKERT , Clayton SPRINGER , Yingchuan SUN , Noel Marie-France THOMSEN , George Scott TRIA , Bing YU
发明人： Heather Elizabeth BURKS , Michael A. DECHANTSREITER , Guo HE , Jill NUNEZ , Stefan PEUKERT , Clayton SPRINGER , Yingchuan SUN , Noel Marie-France THOMSEN , George Scott TRIA , Bing YU
IPC分类号： A61K31/381 , A61K45/06
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.
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公开(公告)号：US20140235660A1
公开(公告)日：2014-08-21
申请号：US14178652
申请日：2014-02-12
申请人： Heather Elizabeth BURKS , Michael A. DECHANTSREITER , Guo HE , Jill NUNEZ , Stefan PEUKERT , Clayton SPRINGER , Yingchuan SUN , Noel Marie-France THOMSEN , George Scott TRIA , Bing YU
发明人： Heather Elizabeth BURKS , Michael A. DECHANTSREITER , Guo HE , Jill NUNEZ , Stefan PEUKERT , Clayton SPRINGER , Yingchuan SUN , Noel Marie-France THOMSEN , George Scott TRIA , Bing YU
IPC分类号： C07D333/64 , A61K45/06 , C07D413/04 , A61K31/422 , A61K31/506 , A61K31/4436 , C07D333/66 , C07D413/12 , A61K31/4245 , A61K31/4196 , A61K31/381 , C07D409/12
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。
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公开(公告)号：US08877801B2
公开(公告)日：2014-11-04
申请号：US14178652
申请日：2014-02-12
申请人： Heather Elizabeth Burks , Michael A. Dechantsreiter , Guo He , Jill Nunez , Stefan Peukert , Clayton Springer , Yingchuan Sun , Noel Marie-France Thomsen , George Scott Tria , Bing Yu
发明人： Heather Elizabeth Burks , Michael A. Dechantsreiter , Guo He , Jill Nunez , Stefan Peukert , Clayton Springer , Yingchuan Sun , Noel Marie-France Thomsen , George Scott Tria , Bing Yu
IPC分类号： A61K31/381 , C07D333/64 , A61K45/06 , A61K31/506 , C07D413/12 , A61K31/422 , C07D413/04 , C07D333/66 , A61K31/4245 , A61K31/4196 , C07D409/12 , A61K31/4436
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。
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4.发明授权Benzothiophene derivatives and compositions thereof as selective estrogen receptor degraders 有权苯并噻吩衍生物及其组合物作为选择性雌激素受体降解物公开(公告)号：US09561211B2
公开(公告)日：2017-02-07
申请号：US15066425
申请日：2016-03-10
申请人： Heather Elizabeth Burks , Michael A. Dechantsreiter , Guo He , Jill Nunez , Stefan Peukert , Clayton Springer , Yingchuan Sun , Noel Marie-France Thomsen , George Scott Tria , Bing Yu
发明人： Heather Elizabeth Burks , Michael A. Dechantsreiter , Guo He , Jill Nunez , Stefan Peukert , Clayton Springer , Yingchuan Sun , Noel Marie-France Thomsen , George Scott Tria , Bing Yu
IPC分类号： A61K31/00 , A61K31/381 , C07D333/64 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/4436 , A61K31/506 , A61K45/06 , C07D333/66 , C07D409/12 , C07D413/04 , C07D413/12 , C07D409/04 , C07D409/10 , C07D417/12 , A61K31/397 , A61K31/4025 , A61K31/404 , A61K31/41 , A61K31/428 , A61K31/5377
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。
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5.发明申请BENZOTHIOPHENE DERIVATIVES AND COMPOSITIONS THEREOF AS SELECTIVE ESTROGEN RECEPTOR DEGRADERS 有权作为选择性雌激素受体降解剂的苯并噻吩衍生物及其组合物公开(公告)号：US20150361065A1
公开(公告)日：2015-12-17
申请号：US14768341
申请日：2014-02-12
申请人： Heather Elizabeth BURKS , Michael A. DECHANTSREITER , Guo HE , Jill NUNEZ , Stefan PEUKERT , Clayton SPRINGER , Yingchuan SUN , Neoel Marie-France THOMSEN , George Scott TRIA , Bing YU
发明人： Heather Elizabeth BURKS , Michael A. DECHANTSREITER , Guo HE , Jill NUNEZ , Stefan PEUKERT , Clayton SPRINGER , Yingchuan SUN , Noel Marie-France THOMSEN , George Scott TRIA , Bing YU
IPC分类号： C07D333/64 , A61K31/381 , C07D409/04 , A61K31/4436 , C07D409/10 , A61K31/4025 , A61K31/41 , A61K31/397 , C07D413/04 , A61K31/422 , C07D409/12 , A61K31/404 , C07D413/12 , A61K31/4245 , A61K31/4196 , C07D333/66 , C07D417/12 , A61K31/428 , A61K31/5377 , A61K45/06
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。
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