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公开(公告)号：US09676766B2
公开(公告)日：2017-06-13
申请号：US13512701
申请日：2010-11-17
申请人： Volker Schulze , Marcus Koppitz , Dirk Kosemund , Hartmut Schirok , Benjamin Bader , Philip Lienau , Antje Margret Wengner , Hans Briem , Simon Holton , Gerhard Siemeister , Stefan Prechtl , Ulf Bömer
发明人： Volker Schulze , Marcus Koppitz , Dirk Kosemund , Hartmut Schirok , Benjamin Bader , Philip Lienau , Antje Margret Wengner , Hans Briem , Simon Holton , Gerhard Siemeister , Stefan Prechtl , Ulf Bömer
IPC分类号： A61K31/437 , A61K31/5377 , C07D491/08 , C07D471/04
CPC分类号： C07D471/04 , A61K31/437 , A61K31/5377 , A61K2300/00
摘要： The present invention relates to triazolopyridine compounds of general formula (I) which are Monopolar Spindle 1 kinase (Mps-1 or TTK) inhibitors: Formula (I), in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis proliferative of diseases, as well as to intermediate compounds useful in the preparation of said compounds.
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公开(公告)号：US09468642B2
公开(公告)日：2016-10-18
申请号：US13635734
申请日：2011-03-16
申请人： Ulrich Klar , Marcus Koppitz , Dirk Kosemund , Rolf Bohlmann , Benjamin Bader , Philip Lienau , Gerhard Siemeister , Stefan Prechtl , Duy Nguyen , William Scott
发明人： Ulrich Klar , Marcus Koppitz , Dirk Kosemund , Rolf Bohlmann , Benjamin Bader , Philip Lienau , Gerhard Siemeister , Stefan Prechtl , Duy Nguyen , William Scott
IPC分类号： C07D487/14 , A61K31/519 , C07D487/04 , A61K45/06
CPC分类号： A61K31/519 , A61K45/06 , C07D487/04 , C07D487/14
摘要： The present invention relates to imidazopyrazine compounds of general Formula (I): in which X, R1, R2, R3a, R3b, R4a, R4b, R4C, and R4D are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.
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3.发明授权公开(公告)号：US09340528B2
公开(公告)日：2016-05-17
申请号：US13393583
申请日：2010-08-24
申请人： Benjamin Bader , Ulf Bömer , Stuart Ince , Marcus Koppitz , Philip Lienau , Tobias Marquardt , Duy Nguyen , Stefan Prechtl , Gerhard Siemeister , Christof Wegscheid-Gerlach
发明人： Benjamin Bader , Ulf Bömer , Stuart Ince , Marcus Koppitz , Philip Lienau , Tobias Marquardt , Duy Nguyen , Stefan Prechtl , Gerhard Siemeister , Christof Wegscheid-Gerlach
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D401/14 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D487/04
CPC分类号： C07D401/14 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D487/04
摘要： The present invention relates to substituted aminoquinoxaline compounds of general formula (I) in which (II), R2, R3, R4, R6, R7, n and m are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.
摘要翻译： 本发明涉及通式（I）的取代氨基喹喔啉化合物，其中（II），R2，R3，R4，R6，R7，n和m如说明书和权利要求书中所给出，涉及制备所述化合物的方法 涉及包含所述化合物的药物组合物和组合，用于制备用于治疗或预防疾病的药物组合物的所述化合物的用途，以及可用于制备所述化合物的中间体化合物。
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公开(公告)号：US09255100B2
公开(公告)日：2016-02-09
申请号：US13822175
申请日：2011-09-06
申请人： Ulrich Klar , Marcus Koppitz , Rolf Jautelat , Dirk Kosemund , Rolf Bohlmann , Philip Lienau , Gerhard Siemeister , Antje Margret Wengner
发明人： Ulrich Klar , Marcus Koppitz , Rolf Jautelat , Dirk Kosemund , Rolf Bohlmann , Philip Lienau , Gerhard Siemeister , Antje Margret Wengner
IPC分类号： C07D487/04 , A61K31/5025 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D471/04
CPC分类号： C07D487/04 , A61K31/5025 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D471/04
摘要： The present invention relates to substituted imidazopyridazine compounds of general formula (I), which are Mps-1 (Monopolar Spindle 1) Kinase inhibitors (also known as Tyrosine Threonine Kinase, TTK) in which R3, R5, and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
摘要翻译： 本发明涉及通式（I）的取代的咪唑并哒嗪化合物，其是Mps-1（单极主轴1）激酶抑制剂（也称为酪氨酸苏氨酸激酶，TTK），其中R3，R5和A如 对于制备所述化合物的方法，涉及包含所述化合物的药物组合物和组合，以及所述化合物用于制备用于治疗或预防疾病，特别是高增殖和/或血管生成障碍的药物组合物的用途 ，作为唯一的药剂或与其它活性成分组合。
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![6-thio-substituted imidazo[1,2-a]pyrazines as Mps-1 inhibitors](/abs-image/US/2015/12/15/US09212184B2/abs.jpg.150x150.jpg)
5.发明授权公开(公告)号：US09212184B2
公开(公告)日：2015-12-15
申请号：US13995055
申请日：2011-12-13
申请人： Marcus Koppitz , Ulrich Klar , Rolf Jautelat , Dirk Kosemund , Rolf Bohlmann , Benjamin Bader , Philip Lienau , Gerhard Siemeister
发明人： Marcus Koppitz , Ulrich Klar , Rolf Jautelat , Dirk Kosemund , Rolf Bohlmann , Benjamin Bader , Philip Lienau , Gerhard Siemeister
IPC分类号： A61K31/4985 , C07D241/54 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to substituted imidazopyrazine compounds of general formula (I): (I) in which R1, R2, R3, R4 and R5 are as defined in the claims, to methods of and intermediates for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
摘要翻译： 本发明涉及通式（I）的取代的咪唑并吡嗪化合物：其中R 1，R 2，R 3，R 4和R 5如权利要求中所定义，其中R 1，R 2，R 3，R 4和R 5如上述定义的方法和制备所述化合物的中间体， 包含所述化合物的组合以及所述化合物用于制备用于治疗或预防疾病，特别是高增殖性和/或血管生成障碍的药物组合物作为唯一试剂或与其它活性成分组合的用途。
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6.发明授权Sulfone-substituted anilinopyrimidine derivatives as CDK inhibitors, the production thereof, and use as a medicine 有权砜取代的苯胺基嘧啶衍生物作为CDK抑制剂，其制备及用作药物公开(公告)号：US08802686B2
公开(公告)日：2014-08-12
申请号：US13125144
申请日：2009-10-08
IPC分类号： A61K31/505 , C07D239/24
CPC分类号： C07D239/47
摘要： The invention relates to sulphone-substituted anilinopyrimidine derivatives of the formula (I), to its preparation processes, and to its use as medicament for treating various diseases.
摘要翻译： 本发明涉及式（I）的砜取代的苯胺基嘧啶衍生物及其制备方法，以及其用作治疗各种疾病的药物。
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公开(公告)号：US08729082B2
公开(公告)日：2014-05-20
申请号：US13264627
申请日：2010-04-24
申请人： Marcus Koppitz , Benjamin Bader , Ulf Bömer , Bertolt Kreft , Philip Lienau , Tobias Marquardt , Stefan Prechtl , Gerhard Siemeister , Christof Wegscheid-Gerlach
发明人： Marcus Koppitz , Benjamin Bader , Ulf Bömer , Bertolt Kreft , Philip Lienau , Tobias Marquardt , Stefan Prechtl , Gerhard Siemeister , Christof Wegscheid-Gerlach
IPC分类号： A61K31/4985 , A61K31/5377 , C07D487/04
CPC分类号： C07D487/02
摘要： The present invention relates to substituted imidazoquinoxaline compounds of general formula (I) as inhibitors of Mps-1 Kinase or TTK, and being active against inflammation and cancer.
摘要翻译： 本发明涉及作为Mps-1激酶或TTK的抑制剂的通式（I）的取代咪唑并喹喔啉化合物，并且对炎症和癌症具有活性。
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8.发明申请6-SUBSTITUTED IMIDAZOPYRAZINES FOR USE AS MPS-1 AND TKK INHIBITORS IN THE TREATMENT OF HYPERPROLIFERATIVE DISORDERS 审中-公开用作MPS-1和TKK抑制剂治疗高血压病症的6-取代咪唑吡嗪公开(公告)号：US20140135319A1
公开(公告)日：2014-05-15
申请号：US13995069
申请日：2011-12-13
申请人： Marcus Koppitz , Ulrich Klar , Rolf Jautelat , Dirk Kosemund , Rolf Bohlmann , Benjamin Bader , Philip Lienau , Gerhard Siemeister
发明人： Marcus Koppitz , Ulrich Klar , Rolf Jautelat , Dirk Kosemund , Rolf Bohlmann , Benjamin Bader , Philip Lienau , Gerhard Siemeister
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to substituted imidazopyrazine compounds of general formula (I): in which R1, R2, R3, R4 and R5 are as defined in the claims, to methods of and intermediates for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
摘要翻译： 本发明涉及通式（I）的取代的咪唑并嗪化合物：其中R 1，R 2，R 3，R 4和R 5如权利要求中所定义，涉及制备所述化合物的方法和中间体，药物组合物和组合，其包含所述 化合物和所述化合物用于制备用于治疗或预防疾病，特别是高增殖和/或血管生成障碍的药物组合物作为唯一试剂或与其它活性成分组合的用途。
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公开(公告)号：US20130338133A1
公开(公告)日：2013-12-19
申请号：US13822175
申请日：2011-09-06
申请人： Ulrich Klar , Marcus Koppitz , Rolf Jautelat , Dirk Kosemund , Rolf Bohlmann , Philip Lienau , Gerhard Siemeister , Antje Margret Wengner
发明人： Ulrich Klar , Marcus Koppitz , Rolf Jautelat , Dirk Kosemund , Rolf Bohlmann , Philip Lienau , Gerhard Siemeister , Antje Margret Wengner
IPC分类号： C07D487/04 , A61K45/06 , A61K31/5377 , A61K31/506 , C07D471/04 , A61K31/5025
CPC分类号： C07D487/04 , A61K31/5025 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D471/04
摘要： The present invention relates to substituted imidazopyridazine compounds of general formula (I), which are Mps-1 (Monopolar Spindle 1) Kinase inhibitors (also known as Tyrosine Threonine Kinase, TTK) in which R3, R5, and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
摘要翻译： 本发明涉及通式（I）的取代的咪唑并哒嗪化合物，其是Mps-1（单极主轴1）激酶抑制剂（也称为酪氨酸苏氨酸激酶，TTK），其中R3，R5和A如 对于制备所述化合物的方法，涉及包含所述化合物的药物组合物和组合，以及所述化合物用于制备用于治疗或预防疾病，特别是高增殖和/或血管生成障碍的药物组合物的用途 ，作为唯一的药剂或与其它活性成分组合。
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10.发明授权Sulfoximine-substituted pyrimidines as CDK- and/or VEGF inhibitors, their production and use as pharmaceutical agents 失效磺酰亚胺取代的嘧啶作为CDK和/或VEGF抑制剂，其生产和用作药剂公开(公告)号：US08507510B2
公开(公告)日：2013-08-13
申请号：US12095947
申请日：2004-10-12
IPC分类号： A01N43/54 , A61K31/505 , C07D239/02
CPC分类号： C07D239/47 , C07D239/48
摘要： This invention relates to pyrimidine derivatives of general formula I in which Q, R1, R2, R3, R4, R5, X, and m have the meanings that are contained in the description, as inhibitors of cyclin-dependent kinases and VEGF-receptor tyrosine kinases, their production as well as their use as medications for treatment of various diseases.
摘要翻译： 本发明涉及通式I的嘧啶衍生物，其中Q，R 1，R 2，R 3，R 4，R 5，X和m具有说明书中所含的含义，作为细胞周期蛋白依赖性激酶和VEGF受体酪氨酸的抑制剂 激酶，它们的生产以及用作治疗各种疾病的药物。
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