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公开(公告)号：US20230077225A1
公开(公告)日：2023-03-09
申请号：US17869575
申请日：2022-07-20
发明人： Xiaolun Wang , Aaron Craig Burns , James Gail Christensen , John Michael Ketcham , John David Lawson , Matthew Arnold Marx , Christopher Ronald Smith , Shelley Allen , James F. Blake , Mark Joseph Chicarelli , Joshua Ryan Dahlke , Donghua Dai , Jay Bradford Fell , John Peter Fischer , Macedonio J. Mejia , Brad Newhouse , Phong Nguyen , Jacob Matthew O'Leary , Spencer Pajk , Martha E. Rodriguez , Pavel Savechenkov , Tony P. Tang , Guy P.A. Vigers , Qian Zhao , Dean Russell Kahn , John Gaudino , Michael Christopher Hilton
IPC分类号： C07D519/00
摘要： The present invention relates to compounds that inhibit KRas G12D. In particular, the present invention relates to compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.
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公开(公告)号：US20230279025A1
公开(公告)日：2023-09-07
申请号：US18015691
申请日：2021-02-25
发明人： Xiaolun Wang , Aaron Craig Burns , James Gail Christensen , John Michael Ketcham , John David Lawson , Matthew Arnold Marx , Christopher Ronald Smith , Shelley Allen , James Francis Blake , Mark Joseph Chicarelli , Joshua Ryan Dahlke , Donghua Dai , Jay Bradford Fell , John Peter Fischer , Macedonio J. Mejia , Brad Newhouse , Phong Nguyen , Jacob Matthew O'Leary , Spencer Pajk , Martha E. Rodriguez , Pavel Savechenkov , Tony P. Tang , Guy P.A. Vigers , Qian Zhao , Dean Russell Kahn , John Gaudino , Michael Christopher Hilton
IPC分类号： C07D519/00
CPC分类号： C07D519/00 , C07B2200/05
摘要： The present invention relates to compounds that inhibit KRas G12D, In particular, the present invention relates to compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.
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公开(公告)号：US20190062330A1
公开(公告)日：2019-02-28
申请号：US16173726
申请日：2018-10-29
发明人： James F. Blake , Laurence E. Burgess , Mark Joseph Chicarelli , James Gail Christensen , Jay Bradford Fell , John P. Fischer , John J. Gaudino , Erik James Hicken , Ronald Jay Hinklin , Matthew Randolf Lee , Matthew Arnold Marx , Macedonio J. Mejia , Martha E. Rodriguez , Pavel Savechenkov , Tony P. Tang , Guy P.A. Vigers , Henry J. Zecca
IPC分类号： C07D471/04 , C07D519/00
摘要： The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
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公开(公告)号：US20210380570A1
公开(公告)日：2021-12-09
申请号：US17053273
申请日：2019-05-06
发明人： Matthew Arnold Marx , Matthew Randolph Lee , James F. Blake , Mark Joseph Chicarelli , Jay Bradford Fell , John P. Fischer , Erik James Hicken , Pavel Savechenkov , Tony Tang , Guy P.A. Vigers , Henry J. Zecca
IPC分类号： C07D413/14 , C07D413/06 , A61P35/00
摘要： The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
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公开(公告)号：US20180072723A1
公开(公告)日：2018-03-15
申请号：US15814279
申请日：2017-11-15
发明人： James F. Blake , Laurence E. Burgess , Mark Joseph Chicarelli , James Gail Christensen , Jay Bradford Fell , John P. Fischer , John J. Gaudino , Erik James Hicken , Ronald Jay Hinklin , Matthew Randolf Lee , Matthew Arnold Marx , Macedonio J. Mejia , Martha E. Rodriguez , Pavel Savechenkov , Tony P. Tang , Guy P.A. Vigers , Henry J. Zecca
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D519/00
摘要： The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
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公开(公告)号：US20240309020A1
公开(公告)日：2024-09-19
申请号：US18644056
申请日：2024-04-23
发明人： Xiaolun Wang , Aaron Craig Burns , James Gail Christensen , John Michael Ketcham , John David Lawson , Matthew Arnold Marx , Christopher Ronald Smith , Shelley Allen , James F. Blake , Mark Joseph Chicarelli , Joshua Ryan Dahlke , Donghua Dai , Jay Bradford Fell , John Peter Fischer , Macedonio J. Mejia , Brad Newhouse , Phong Nguyen , Jacob Matthew O'Leary , Spencer Pajk , Martha E. Rodriguez , Pavel Savechenkov , Tony P. Tang , Guy P.A. Vigers , Qian Zhao , Dean Russell Kahn , John Gaudino , Michael Christopher Hilton
IPC分类号： C07D519/00
CPC分类号： C07D519/00
摘要： The present invention relates to compounds that inhibit KRas G12D. In particular, the present invention relates to compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.
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公开(公告)号：US11964989B2
公开(公告)日：2024-04-23
申请号：US17869575
申请日：2022-07-20
发明人： Xiaolun Wang , Aaron Craig Burns , James Gail Christensen , John Michael Ketcham , John David Lawson , Matthew Arnold Marx , Christopher Ronald Smith , Shelley Allen , James F. Blake , Mark Joseph Chicarelli , Joshua Ryan Dahlke , Donghua Dai , Jay Bradford Fell , John Peter Fischer , Macedonio J. Mejia , Brad Newhouse , Phong Nguyen , Jacob Matthew O'Leary , Spencer Pajk , Martha E. Rodriguez , Pavel Savechenkov , Tony P. Tang , Guy P.A. Vigers , Qian Zhao , Dean Russell Kahn , John Gaudino , Michael Christopher Hilton
IPC分类号： C07D519/00
CPC分类号： C07D519/00
摘要： Compounds that inhibit KRas G12D. In particular, compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor, and in particular, methods of treating cancer. The compounds have a general structure represented by Formula (I):
or a pharmaceutically acceptable salt thereof.-
公开(公告)号：US20190144444A1
公开(公告)日：2019-05-16
申请号：US16191190
申请日：2018-11-14
发明人： James F. Blake , Laurence E. Burgess , Mark Joseph Chicarelli , James Gail Christensen , Adam Cook , Jay Bradford Fell , John P. Fischer , Matthew Arnold Marx , Macedonio J. Mejia , Pavel Savechenkov , Guy P.A. Vigers , Christopher Ronald Smith , Martha E. Rodriguez
IPC分类号： C07D471/04 , C07D491/08 , A61P35/00
摘要： The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
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公开(公告)号：US20140148436A1
公开(公告)日：2014-05-29
申请号：US14170272
申请日：2014-01-31
发明人： Ian S. Mitchell , Keith L. Spencer , Peter Stengel , Yongxin Han , Nicolas C. Kallan , Mark Munson , Guy P.A. Vigers , James Blake , Anthony Piscopio , John Josey , Scott Miller , Dengming Xiao , Rui Xu , Chang Rao , Bing Wang , April L. Bernacki
IPC分类号： C07D239/94 , C07D403/12 , C07D495/04 , C07D491/048 , C07D231/56 , C07D401/12 , C07D409/04 , C07D401/04 , C07D409/12 , C07D487/04
CPC分类号： C07D239/94 , B41M3/008 , B44F1/10 , C07D231/56 , C07D237/28 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D409/04 , C07D409/12 , C07D471/04 , C07D487/04 , C07D491/048 , C07D495/04 , G09F13/16 , Y10T428/24802 , Y10T428/24851 , Y10T428/25 , Y10T428/31507 , Y10T428/31551 , Y10T428/31786 , Y10T428/31855
摘要： The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
摘要翻译： 本发明提供包括分解对映异构体，非对映异构体，溶剂化物和药学上可接受的盐的化合物，其包含式为：A-L-CR，其中CR为环状核心基团，L为连接基团，A如本文所定义。 还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。
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公开(公告)号：US20160152576A9
公开(公告)日：2016-06-02
申请号：US14170272
申请日：2014-01-31
发明人： Ian S. Mitchell , Keith L. Spencer , Peter Stengel , Yongxin Han , Nicolas C. Kallan , Mark Munson , Guy P.A. Vigers , James Blake , Anthony Piscopio , John Josey , Scott Miller , Dengming Xiao , Rui Xu , Chang Rao , Bing Wang , April L. Bernacki
IPC分类号： C07D239/94 , C07D403/12 , C07D495/04 , C07D491/048 , C07D231/56 , C07D401/12 , C07D409/04 , C07D401/04 , C07D409/12 , C07D487/04
CPC分类号： C07D239/94 , B41M3/008 , B44F1/10 , C07D231/56 , C07D237/28 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D409/04 , C07D409/12 , C07D471/04 , C07D487/04 , C07D491/048 , C07D495/04 , G09F13/16 , Y10T428/24802 , Y10T428/24851 , Y10T428/25 , Y10T428/31507 , Y10T428/31551 , Y10T428/31786 , Y10T428/31855
摘要： The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
摘要翻译： 本发明提供包括分解对映异构体，非对映异构体，溶剂化物和药学上可接受的盐的化合物，其包含式为：A-L-CR，其中CR为环状核心基团，L为连接基团，A如本文所定义。 还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。
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