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公开(公告)号：US20230399341A1
公开(公告)日：2023-12-14
申请号：US18250419
申请日：2021-11-04
发明人： David A. Candito , Joanna L. Chen , Anthony Donofrio , Xavier Fradera , Peter H. Fuller , Shuhei Kawamura , Bing Li , Jongwon Lim , Ping Liu , Joey L. Methot , Anilkumar G. Nair , Alexander Pasternak , Brandon A. Vara , Elsie C. Yu
IPC分类号： C07D498/04 , C07D401/12 , C07D519/00 , C07D401/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D471/04 , C07D405/14 , C07D495/04 , C07D413/04
CPC分类号： C07D498/04 , C07D401/12 , C07D519/00 , C07D401/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D471/04 , C07D405/14 , C07D495/04 , C07D413/04
摘要： Compounds of the following formula (I); or the pharmaceutically acceptable salts thereof, are inhibitors of haematopoietic progenitor kinase 1 (HPK1) useful in the treatment of diseases or disorders associated with HPK1. Also disclosed herein are uses of these compounds in the potential treatment or prevention of an HPK1-associated disease or disorder. Also disclosed herein are compositions comprising one or more of the compounds. Further disclosed herein are uses of these compositions in the potential prevention or treatment of an HPK1-associated disease or disorder.
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公开(公告)号：US11993602B2
公开(公告)日：2024-05-28
申请号：US17266474
申请日：2019-08-05
申请人： Merck Sharp & Dohme LLC , David Witter , Shuhei Kawamura , Michelle Machacek , Ryan Quiroz , Michael H. Reutershan , Sebastian Schneider , Phieng Siliphaivanh , Yingchun Ye , Charles S. Yeung
发明人： David Witter , Shuhei Kawamura , Michelle Machacek , Ryan Quiroz , Michael H. Reutershan , Sebastian Schneider , Phieng Siliphaivanh , Yingchun Ye , Charles S. Yeung
IPC分类号： C07D487/04 , C07D519/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention provides a compound of Formula (I) Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.
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公开(公告)号：US20230114091A1
公开(公告)日：2023-04-13
申请号：US17783967
申请日：2020-12-14
发明人： Michelle Machacek , Michael D. Altman , Shuhei Kawamura , Michael H. Reutershan , David L. Sloman , Phieng Siliphaivanh , Sebastian E. Schneider , Charles S. Yeung , David J. Witter , Craig R. Gibeau
IPC分类号： C07D471/10 , C07D519/00
摘要： The present invention provides a compound of Formula (I) (I) and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are PRMT5 inhibitors. Also provided are methods of making compounds of Formula I, pharmaceutical compositions comprising compounds of Formula I, and methods of using these compounds to treat cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.
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公开(公告)号：US20230092404A1
公开(公告)日：2023-03-23
申请号：US17787135
申请日：2020-12-14
发明人： Michelle Machacek , Michael D. Altman , Shuhei Kawamura , David L. Sloman , David J. Witter , Craig R. Gibeau
IPC分类号： C07D519/00
摘要： The present invention provides a compound selected from: and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are PRMT5 inhibitors. Also provided are methods of making compounds disclosed herein, pharmaceutical compositions comprising compounds disclosed herein, and methods of using these compounds to treat cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.
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公开(公告)号：US20240239788A1
公开(公告)日：2024-07-18
申请号：US18555640
申请日：2022-04-15
发明人： David L. Sloman , Gianni Chessari , Patrick Schöpf , Steven Howard , Yuichi Kawai , Kazuaki Shibata , Hiroki Asakura , Takao Uno , Takeshi Sagara , Masayuki Nakamura , Yu Kobayakawa , David Jonathan Bennett , Indu Bharathan , Thomas H. Graham , Yongxin Han , Zahid Hussain , Xiaoshen Ma , Mihir Mandal , Ryan D. Otte , Anandan Palani , Uma Swaminathan , Mycah Uehling , Yingchun Ye , Ryan Chau , Alec H. Christian , Symon Gathiaka , Timothy J. Henderson , Elisabeth T. Hennessy , Andrew J. Hoover , Shuhei Kawamura , Igri Kolaj , Thomas W. Lyons , Matthew J. Mitcheltree , Aaron Sather
IPC分类号： C07D451/06 , A61K31/517 , A61K31/519 , A61K31/5377 , A61K45/06 , C07D471/08 , C07D519/00
CPC分类号： C07D451/06 , A61K31/517 , A61K31/519 , A61K31/5377 , A61K45/06 , C07D471/08 , C07D519/00
摘要： Compounds or their pharmaceutically acceptable salts can inhibit the G12D mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds disclosed herein or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.
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公开(公告)号：US20230416225A1
公开(公告)日：2023-12-28
申请号：US18251259
申请日：2021-11-04
发明人： Abdelghani Achab , David A. Candito , Anthony Donofrio , Xavier Fradera , Shuhei Kawamura , Samuel M. Levi , Bing Li , Anilkumar G. Nair , Alexander Pasternak , Brandon A. Vara , Elsie C. Yu
IPC分类号： C07D401/12 , C07D413/14 , C07D401/14 , C07D405/14 , C07D239/49 , C07D471/04 , C07D498/04 , C07D487/04 , C07D405/12 , C07D403/12 , C07D417/14 , C07D409/14 , C07D451/02
CPC分类号： C07D401/12 , C07D413/14 , C07D401/14 , C07D405/14 , C07D239/49 , C07D471/04 , C07D498/04 , C07D487/04 , C07D405/12 , C07D403/12 , C07D417/14 , C07D409/14 , C07D451/02
摘要： Compounds of the formula I: or the pharmaceutically acceptable salts thereof, are inhibitors of haematopoietic progenitor kinase 1 (HPK1) useful in the treatment of diseases or disorders associated with HPK1. Also disclosed herein are uses of these compounds in the potential treatment or prevention of an HPK1-associated disease or disorder. Also disclosed herein are compositions comprising one or more of the compounds. Further disclosed herein are uses of these compositions in the potential prevention or treatment of an HPK1-associated disease or disorder.
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