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公开(公告)号：US11046688B2
公开(公告)日：2021-06-29
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： A61K31/519 , C07D471/04 , C07D401/14 , C07D413/14 , C07D401/04 , C07D405/04 , 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：US10479788B2
公开(公告)日：2019-11-19
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： A61K31/519 , C07D471/04 , C07D401/14 , C07D413/14 , C07D401/04 , C07D405/04 , 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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![N2-phenyl-pyrido[3,4-D]pyrimidine-2, 8-diamine derivatives and their use as Mps1 inhibitors](/abs-image/US/2019/09/03/US10399974B2/abs.jpg.150x150.jpg)
3.发明授权公开(公告)号：US10399974B2
公开(公告)日：2019-09-03
申请号：US15861287
申请日：2018-01-03
发明人： Hannah Woodward , Paolo Innocenti , Sebastien Naud , Julian Blagg , Swen Hoelder
IPC分类号： A61K31/519 , 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：US09834552B2
公开(公告)日：2017-12-05
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： A01N43/90 , A61K31/519 , 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：US09834541B2
公开(公告)日：2017-12-05
申请号：US14437561
申请日：2013-10-02
发明人： Kai Schiemann , Frank Stieber , Julian Blagg , Aurelie Mallinger , Dennis Waalboer , Christian Rink , Simon Ross Crumpler
IPC分类号： C07D471/10 , A61K31/444 , A61K31/4545 , C07D401/04 , C07D401/14 , A61K31/5377 , A61K31/499 , A61K31/4709 , C07D417/14 , C07D491/10 , C07D498/10
CPC分类号： C07D401/14 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/499 , A61K31/5377 , C07D401/04 , C07D417/14 , C07D471/10 , C07D491/10 , C07D498/10
摘要： The invention provides novel substituted 2-aminopyridine compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases.
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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：US20160296514A1
公开(公告)日：2016-10-13
申请号：US15069012
申请日：2016-03-14
IPC分类号： A61K31/4725 , A61K31/5355 , A61K31/4985 , A61K31/519 , A61K31/496 , A61K31/4747 , A61K31/4375 , A61K31/506 , A61K31/541
CPC分类号： A61K31/4725 , A61K31/4375 , A61K31/4747 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/519 , A61K31/5355 , A61K31/541 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/107
摘要： The present invention relates to compounds of formula II wherein X, Y, R2, R3, R4 and Ar 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.
摘要翻译： 其中X，Y，R 2，R 3，R 4和Ar全部如本文所定义。 已知本发明的化合物通过与Mps1激酶本身的相互作用直接或间接地抑制单轴1（Mps1，也称为TTK）激酶的心轴检查点功能。 特别地，本发明涉及这些化合物作为治疗和/或预防增殖性疾病如癌症的治疗剂的用途。 本发明还涉及制备这些化合物的方法以及包含它们的药物组合物。
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10.发明申请PYRIDINE AND PYRIMIDINE BASED COMPOUNDS AS WNT SIGNALING PATHWAY INHIBITORS FOR THE TREATMENT OF CANCER 审中-公开作为Wnt信号途径抑制剂治疗癌症的吡啶和吡啶基化合物公开(公告)号：US20140350015A1
公开(公告)日：2014-11-27
申请号：US14303448
申请日：2014-06-12
IPC分类号： C07D471/10 , C07D413/14 , C07D417/14 , C07D409/14 , C07D401/04 , C07D401/14
CPC分类号： C07D471/10 , C07D213/74 , C07D401/04 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to pyridine and pyrimidine based compounds, pharmaceutical compositions comprising these compounds and their potential use as therapeutic agents for the treatment and/or prevention of cancer.
摘要翻译： 本发明涉及基于吡啶和嘧啶的化合物，包含这些化合物的药物组合物及其作为用于治疗和/或预防癌症的治疗剂的潜在用途。
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