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公开(公告)号：US10435391B2
公开(公告)日：2019-10-08
申请号：US15568025
申请日：2016-04-20
Inventor： Linda N. Casillas , John David Harling , Afjal Hussain Miah , Mark David Rackham , Ian Edward David Smith
IPC: C07D403/14 , A61P35/00 , C07D401/14 , C07D417/14 , C07D487/04 , A61P29/00
Abstract: The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of diseases and conditions mediated by the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.
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公开(公告)号：US10336744B2
公开(公告)日：2019-07-02
申请号：US15568006
申请日：2016-04-20
Inventor： John David Harling , Ian Edward David Smith
IPC: C07D417/14 , A61K31/4725 , A61K31/519 , C07D417/12 , C07D487/04 , A61K47/54 , A61K47/66
Abstract: The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of diseases and conditions mediated by the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.
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Patent Agency Ranking
公开(公告)号：US10781205B2
公开(公告)日：2020-09-22
申请号：US16094564
申请日：2017-04-18
Inventor： Linda N. Casillas , John David Harling , Afjal Hussain Miah , Mark David Rackham , Ian Edward David Smith
IPC: C07D471/04 , C07D417/14 , C07D471/10 , C07D519/00 , A61P37/00 , A61P29/00
Abstract: The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of diseases and conditions mediated by the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.
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4.发明申请Compounds & Methods for the Enhanced Degradation of Targeted Proteins & Other Polypeptides by an E3 Ubiquitin Ligase 审中-公开通过E3泛素连接酶增强靶向蛋白质和其他多肽降解的化合物和方法公开(公告)号：US20140356322A1
公开(公告)日：2014-12-04
申请号：US14371956
申请日：2013-01-11
Applicant: YALE UNIVERSITY , GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED , CAMBRIDGE ENTERPRISE LIMITED UNIVERSITY OF CAMBRIDGE
Inventor： Craig M. Crews , Dennis Buckley , Alessio Ciulli , William Jorgensen , Peter C. Gareiss , Inge Van Molle , Jeffrey Gustafson , Hyun-Seop Tae , Julien Michel , Dentin Wade Hoyer , Anke G. Roth , John David Harling , Ian Edward David Smith , Afjal Hussain Miah , Sebastien Andre Campos , Joelle Le
IPC: C07D413/14 , A61K38/05 , A61K31/5377 , A61K31/437 , A61K31/454 , A61K31/4439 , A61K31/427 , A61K31/422 , C07K5/08 , C07J43/00 , C07D471/04 , C07D417/14 , C07D413/06 , A61K45/06 , A61K38/06
Abstract: The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins that are degraded and/or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds of the present invention, consistent with the degradation/inhibition of targeted polypeptides.
Abstract translation: 本发明涉及双功能化合物，其可用作靶向泛素化的调节剂，特别是多种多肽和其它由本发明的双功能化合物降解和/或以其它方式抑制的蛋白质的抑制剂。 特别地，本发明涉及化合物，其一端含有与泛素连接酶结合的VHL配体，另一端含有结合靶蛋白的部分，使得靶蛋白置于接近泛素处 连接酶以实现该蛋白质的降解（和抑制）。 与靶向多肽的降解/抑制一致，本发明显示出与本发明化合物相关的广泛的药理学活性。
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公开(公告)号：US10730862B2
公开(公告)日：2020-08-04
申请号：US14371956
申请日：2013-01-11
Applicant: YALE UNIVERSITY , GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED , CAMBRIDGE ENTERPRISE LIMITED UNIVERSITY OF CAMBRIDGE
Inventor： Craig M. Crews , Dennis Buckley , Alessio Ciulli , William Jorgensen , Peter C. Gareiss , Inge Van Molle , Jeffrey Gustafson , Hyun-Seop Tae , Julien Michel , Denton Wade Hoyer , Anke G. Roth , John David Harling , Ian Edward David Smith , Afjal Hussain Miah , Sebastien Andre Campos , Joelle Le
IPC: C07D413/14 , C07D417/12 , C07D417/14 , C07D401/06 , C07D401/10 , C07D403/06 , C07D405/06 , C07D405/12 , C07D207/16 , C07D413/12 , C07D207/26 , C12N9/00 , A61K47/54 , A61K47/64 , A61K47/55 , A61K31/422 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61K38/05 , A61K38/06 , A61K45/06 , C07D413/06 , C07D471/04 , C07J43/00
Abstract: The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins that are degraded and/or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds of the present invention, consistent with the degradation/inhibition of targeted polypeptides.
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公开(公告)号：US20190119271A1
公开(公告)日：2019-04-25
申请号：US16094564
申请日：2017-04-18
Inventor： Linda N. CASILLAS , John David HARLING , Afjal Hussain MIAH , Mark David RACKHAM , Ian Edward David Smith
IPC: C07D471/04 , C07D417/14 , C07D471/10 , C07D519/00
Abstract: The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of diseases and conditions mediated by the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.
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公开(公告)号：US09988376B2
公开(公告)日：2018-06-05
申请号：US14898782
申请日：2014-07-01
IPC: C07D417/14 , C07D413/14 , C07D409/12 , C07D409/14 , A61K31/422 , A61K31/427 , A61K31/435 , A61K31/496 , A61K38/05 , A61K45/06 , C07D471/10 , C07K5/062
CPC classification number: C07D417/14 , A61K31/422 , A61K31/427 , A61K31/435 , A61K31/496 , A61K38/05 , A61K45/06 , C07D409/12 , C07D409/14 , C07D413/14 , C07D471/10 , C07K5/06052
Abstract: A compound of formula (I): or a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor.
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