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公开(公告)号：US11897877B2
公开(公告)日：2024-02-13
申请号：US17319231
申请日：2021-05-13
发明人： Swen Hoelder , Julian Blagg , Savade Solanki , Hannah Woodward , Sebastien Gaston Andre Naud , Vassilios Bavetsias , Peter Sheldrake , Paolo Innocenti , Kwai-Ming J. Cheung , Butrus Atrash
IPC分类号： C07D471/04 , C07D401/14 , C07D413/14 , C07D401/04 , C07D405/04 , C07D519/00 , A61K31/519
CPC分类号： C07D471/04 , A61K31/519 , C07D401/04 , C07D401/14 , C07D405/04 , C07D413/14 , C07D519/00
摘要： The present invention relates to compounds of formula I
wherein R1, R4, Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.-
公开(公告)号：US20160222009A1
公开(公告)日：2016-08-04
申请号：US15091887
申请日：2016-04-06
发明人： Swen Hoelder , Julian Blagg , Savade Solanki , Hannah Woodward , Sebastien Naud , Vassilios Bavetsias , Peter Sheldrake , Paolo Innocenti , Kwai-Ming J. Cheung , Butrus Atrash
IPC分类号： C07D471/04 , C07D519/00 , C07D401/04 , C07D405/04 , C07D401/14 , C07D413/14
CPC分类号： C07D471/04 , A61K31/519 , C07D401/04 , C07D401/14 , C07D405/04 , C07D413/14 , C07D519/00
摘要： The present invention relates to compounds of formula I wherein R1, R4, Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.
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公开(公告)号：US20160220570A1
公开(公告)日：2016-08-04
申请号：US15091980
申请日：2016-04-06
发明人： Swen Hoelder , Julian Blagg , Savade Solanki , Hannah Woodward , Sebastien Naud , Vassilios Bavetsias , Peter Sheldrake , Paolo Innocenti , Kwai-Ming J. Cheung , Butrus Atrash
IPC分类号： A61K31/519
CPC分类号： C07D471/04 , A61K31/519 , C07D401/04 , C07D401/14 , C07D405/04 , C07D413/14 , C07D519/00
摘要： The present invention relates to compounds of formula I wherein R1, R4, Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.
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公开(公告)号：US20200165241A1
公开(公告)日：2020-05-28
申请号：US16598717
申请日：2019-10-10
发明人： Swen Hoelder , Julian Blagg , Savade Solanki , Hannah Woodward , Sebastien Gaston Andre Naud , Vassilios Bavetsias , Peter Sheldrake , Paolo Innocenti , Kwai-Ming J. Cheung , Butrus Atrash
IPC分类号： C07D471/04 , A61K31/519 , C07D519/00 , C07D405/04 , C07D401/04 , C07D413/14 , C07D401/14
摘要： The present invention relates to compounds of formula I wherein R1, R4, Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.
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公开(公告)号：US20180141944A1
公开(公告)日：2018-05-24
申请号：US15864499
申请日：2018-01-08
发明人： Swen Hoelder , Julian Blagg , Savade Solanki , Hannah Woodward , Sebastien Naud , Vassilios Bavetsias , Peter Sheldrake , Paolo Innocenti , Kwai-Ming J. Cheung , Butrus Atrash
IPC分类号： C07D471/04 , A61K31/519 , C07D519/00 , C07D401/14 , C07D401/04 , C07D413/14 , C07D405/04
CPC分类号： C07D471/04 , A61K31/519 , C07D401/04 , C07D401/14 , C07D405/04 , C07D413/14 , C07D519/00
摘要： The present invention relates to compounds of formula I wherein R1, R4, Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.
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公开(公告)号：US09890157B2
公开(公告)日：2018-02-13
申请号：US15091887
申请日：2016-04-06
发明人： Swen Hoelder , Julian Blagg , Savade Solanki , Hannah Woodward , Sebastien Naud , Vassilios Bavetsias , Peter Sheldrake , Paolo Innocenti , Kwai-Ming J. Cheung , Butrus Atrash
IPC分类号： A01N43/90 , A61K31/519 , C07D471/00 , C07D471/04 , C07D401/14 , C07D413/14 , C07D401/04 , C07D405/04 , C07D519/00
CPC分类号： C07D471/04 , A61K31/519 , C07D401/04 , C07D401/14 , C07D405/04 , C07D413/14 , C07D519/00
摘要： The present invention relates to compounds of formula I wherein R1, R4, Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.
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公开(公告)号：US12110286B2
公开(公告)日：2024-10-08
申请号：US16616901
申请日：2018-05-25
发明人： Benjamin Richard Bellenie , Michael K. Carter , Kwai Ming Jack Cheung , Owen Alexander Davis , Swen Hoelder , Matthew Garth Lloyd , Ana Varela Rodriguez , Hannah Woodward , Paolo Innocenti
IPC分类号： C07D401/14 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/08 , C07D487/04
CPC分类号： C07D401/14 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/08 , C07D487/04
摘要： The present invention relates to compounds of Formula I that function as inhibitors of BCL6 (B-cell lymphoma 6) activity: wherein X1, X2, R1, R2 and R3 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which BCL6 activity is implicated.
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![N2-phenyl-pyrido[3,4-d]pyrimidine-2, 8-diamine derivatives and their use as Mps1 inhibitors](/abs-image/US/2018/02/27/US09902721B2/abs.jpg.150x150.jpg)
8.发明授权公开(公告)号：US09902721B2
公开(公告)日：2018-02-27
申请号：US15121432
申请日：2015-02-27
发明人： Hannah Woodward , Paolo Innocenti , Sebastien Naud , Julian Blagg , Swen Hoelder
IPC分类号： A01N43/90 , A61K31/519 , C07D471/00 , C07D487/00 , C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00
摘要： The present invention relates to compounds of formula I: wherein R1, R2, R3 and R4 are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.
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公开(公告)号：US20220402912A1
公开(公告)日：2022-12-22
申请号：US17319231
申请日：2021-05-13
发明人： Swen Hoelder , Julian Blagg , Savade Solanki , Hannah Woodward , Sebastien Gaston Andre Naud , Vassilios Bavetsias , Peter Sheldrake , Paolo Innocenti , Kwai-Ming J. Cheung , Butrus Atrash
IPC分类号： C07D471/04 , A61K31/519 , C07D413/14 , C07D401/14 , C07D405/04 , C07D401/04 , C07D519/00
摘要： The present invention relates to compounds of formula I wherein R1, R4, Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.
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公开(公告)号：US20210147382A1
公开(公告)日：2021-05-20
申请号：US16616901
申请日：2018-05-25
发明人： Benjamin Richard Bellenie , Michael K. Carter , Kwai Ming Jack Cheung , Owen Alexander Davis , Swen Hoelder , Matthew Garth Lloyd , Ana Varela Rodriguez , Hannah Woodward , Paolo Innocenti
IPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D401/12 , C07D417/14 , C07D405/14 , C07D487/04 , C07D471/08 , C07D471/04
摘要： The present invention relates to compounds of Formula I that function as inhibitors of BCL6 (B-cell lymphoma 6) activity: wherein X1, X2, R1, R2 and R3 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which BCL6 activity is implicated.
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