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1.发明申请公开(公告)号：US20230071711A1
公开(公告)日：2023-03-09
申请号：US17690587
申请日：2022-03-09
发明人： Tongfei Wu , Dirk Brehmer , Lijs Beke , An Boeckx , Gaston Stanislas Marcella Diels , Ronaldus Amodus Hendrika Joseph Gilissen , Edward Charles Lawson , Vineet Pande , Marcus Cornelis Bernardus Catharina Paradé , Wim Bert Griet Schepens , Johannes Wilhelmus John F. Thuring , Marcel Viellevoye , Weimei Sun , Lieven Meerpoel
IPC分类号： A61K31/7076 , A61K31/519 , A61K31/53 , C07D471/04 , A61P35/00 , A61K31/5025
摘要： The present invention relates novel 6-6 bicyclic aromatic ring substituted nucleoside analogues of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PRMT5 inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
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公开(公告)号：US20210371433A1
公开(公告)日：2021-12-02
申请号：US17378417
申请日：2021-07-16
发明人： Tongfei Wu , Dirk Brehmer , Lijs Beke , An Jason Boeckx , Gaston Stanislas Marcella Diels , Edward Charles Lawson , Lieven Meerpoel , Vineet Pande , Marcus Cornelius Bernardus Catharina Parade , Wim Bert Griet Schepens , Weimei Sun , Johannes Wilhelmus John F. Thuring , Marcel Viellevoye
IPC分类号： C07D519/00 , A61P35/00 , A61K9/00 , C07D487/04 , A61K9/20 , A61K9/06
摘要： The present invention relates to novel novel monocyclic and bicyclic ring system substituted carbanucleoside analogues of Formula (I), wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PRMT5 inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
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公开(公告)号：US11993614B2
公开(公告)日：2024-05-28
申请号：US17378417
申请日：2021-07-16
发明人： Tongfei Wu , Dirk Brehmer , Lijs Beke , An Boeckx , Gaston Stanislas Marcella Diels , Edward Charles Lawson , Lieven Meerpoel , Vineet Pande , Marcus Cornelius Bernardus Catharina Parade , Wim Bert Griet Schepens , Weimei Sun , Johannes Wilhelmus John F. Thuring , Marcel Viellevoye
IPC分类号： A61P35/00 , A61K9/00 , A61K9/06 , A61K9/20 , A61K31/519 , C07D487/04 , C07D519/00 , A61K45/06
CPC分类号： C07D519/00 , A61K9/0019 , A61K9/0053 , A61K9/0095 , A61K9/06 , A61K9/2059 , A61K31/519 , A61P35/00 , C07D487/04 , A61K45/06
摘要： The present invention relates to novel monocyclic and bicyclic ring system substituted carbanucleoside analogues of Formula (I), wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PRMT5 inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
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公开(公告)号：US20190381019A1
公开(公告)日：2019-12-19
申请号：US16440302
申请日：2019-06-13
发明人： Tianbao Lu , Peter J. Connolly , Maxwell David Cummings , Joseph Kent Barbay , Kevin D. Kreutter , Tongfei Wu , Gaston Stanislas Marcella Diels , Jan Willem Thuring , Ulrike Philippar , James Patrick Edwards , Fang Shen
IPC分类号： A61K31/444 , A61K31/519 , A61K39/395 , C07D407/14 , C07D403/14 , C07D413/14 , A61K31/5377 , A61P35/00
摘要： Disclosed are compounds, compositions and methods for treating of diseases, syndromes, conditions, and disorders that are affected by the modulation of MALT 1. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R4, R5, and G, are defined herein.
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公开(公告)号：US11883367B2
公开(公告)日：2024-01-30
申请号：US17690587
申请日：2022-03-09
发明人： Tongfei Wu , Dirk Brehmer , Lijs Beke , An Boeckx , Gaston Stanislas Marcella Diels , Ronaldus Arnodus Hendrika Joseph Gilissen , Edward Charles Lawson , Vineet Pande , Marcus Cornelis Bernardus Catharina Paradé , Wim Bert Griet Schepens , Johannes Wilhelmus John F. Thuring , Marcel Viellevoye , Weimei Sun , Lieven Meerpoel
IPC分类号： A01N43/04 , A61K31/70 , A61K31/7076 , A61K31/519 , A61K31/53 , C07D471/04 , A61P35/00 , A61K31/5025
CPC分类号： A61K31/7076 , A61K31/5025 , A61K31/519 , A61K31/53 , A61P35/00 , C07D471/04
摘要： The present invention relates novel 6-6 bicyclic aromatic ring substituted nucleoside analogues of Formula (I)
wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PRMT5 inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.-
公开(公告)号：US11098062B2
公开(公告)日：2021-08-24
申请号：US16336934
申请日：2017-10-02
发明人： Tongfei Wu , Dirk Brehmer , Lijs Beke , An Boeckx , Gaston Stanislas Marcella Diels , Edward Charles Lawson , Lieven Meerpoel , Vineet Pande , Marcus Cornelis Bernardus Catharina Paradé , Wim Bert Griet Schepens , Weimei Sun , Johannes Wilhelmus John F. Thuring , Marcel Viellevoye
IPC分类号： C07D519/00 , C07D487/04 , A61P35/00 , A61K9/00 , A61K9/20 , A61K9/06 , A61K45/06
摘要： The present invention relates to novel novel monocyclic and bicyclic ring system substituted carbanucleoside analogues of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PRMT5 inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
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公开(公告)号：US10898504B2
公开(公告)日：2021-01-26
申请号：US16082020
申请日：2017-02-24
发明人： Didier Jean-Claude Berthelot , Dirk Brehmer , Lijs Beke , An Boeckx , Gaston Stanislas Marcella Diels , Ronaldus Arnodus Hendrika Joseph Gilissen , Edward Charles Lawson , Vineet Pande , Marcus Cornelis Bernardus Catharina Parade , Wim Bert Griet Schepens , Brian Christopher Shook , Johannes Wilhelmus John F. Thuring , Marcel Viellevoye , Weimei Sun , Tongfei Wu , Lieven Meerpoel
IPC分类号： A01N43/04 , A61K31/70 , A61K31/7076 , A61K31/706 , A61K31/7064
摘要： The present invention relates novel substituted nucleoside analogues of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PRMT5 inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
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公开(公告)号：US10888550B2
公开(公告)日：2021-01-12
申请号：US16440356
申请日：2019-06-13
发明人： Tianbao Lu , Peter J. Connolly , Maxwell David Cummings , Gaston Stanislas Marcella Diels , Jan Willem Thuring , Ulrike Philippar , James Patrick Edwards , Didier Jean-Claude Berthelot , Tongfei Wu
IPC分类号： A61K31/437 , A61P35/00 , A61K31/519 , C07D471/04 , C07K16/28
摘要： Disclosed are compounds, compositions and methods for treating of diseases, syndromes, conditions, and disorders that are affected by the modulation of MALT1. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R4, R5, R6, R7, G1 and G2, are defined herein.
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公开(公告)号：US10017509B2
公开(公告)日：2018-07-10
申请号：US15300956
申请日：2015-04-02
发明人： Gaston Stanislas Marcella Diels , Bruno Schoentjes , Matthias Luc Aime Versele , Didier Jean-Claude Berthelot , Marc Willems , Marcel Viellevoye , Werner Constant Johan Embrechts , Berthold Wroblowski , Lieven Meerpoel
IPC分类号： C07D471/22 , C07D498/22
CPC分类号： C07D471/22 , C07D498/22 , Y02P20/582
摘要： The present invention relates to substituted macrocylic pyrimidine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention have EF2K inhibitory activity and optionally also Vps34 inhibitory activity. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
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公开(公告)号：US11318157B2
公开(公告)日：2022-05-03
申请号：US16825024
申请日：2020-03-20
发明人： Tongfei Wu , Dirk Brehmer , Lijs Beke , An Boeckx , Gaston Stanislas Marcella Diels , Ronaldus Arnodus Hendrika Joseph Gilissen , Edward Charles Lawson , Vineet Pande , Marcus Cornelis Bernardus Catharina Paradé , Wim Bert Griet Schepens , Johannes Wilhelmus John F. Thuring , Marcel Viellevoye , Weimei Sun , Lieven Meerpoel
IPC分类号： A61K31/7076 , A61K31/519 , A61K31/53 , C07D471/04 , A61P35/00 , A61K31/5025
摘要： Embodiments of the present invention relate to 6-6 bicyclic aromatic ring substituted nucleoside analogues, including, for example, the following compound: Embodiments of the present invention also relate to uses of the disclosed compounds for the inhibition of protein arginine methyltransferase 5 (PRMT5).
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