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公开(公告)号：US09199999B2
公开(公告)日：2015-12-01
申请号：US13700956
申请日：2011-05-27
申请人： Ulrich Klar , Marcus Koppitz , Rolf Jautelat , Dirk Kosemund , Rolf Bohlmann , Benjamin Bader , Philip Lienau , Gerhard Siemeister , William Scott
发明人： Ulrich Klar , Marcus Koppitz , Rolf Jautelat , Dirk Kosemund , Rolf Bohlmann , Benjamin Bader , Philip Lienau , Gerhard Siemeister , William Scott
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D491/00 , C07D495/00 , C07D497/00 , C07D487/04 , A61K31/4985
CPC分类号： C07D487/04 , A61K31/4985
摘要： The present invention relates to substituted imidazopyrazine compounds of general formula (I) in which A, R1, R3 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 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）的取代咪唑并吡嗪化合物，其中A，R 1，R 3和R 5如在说明书和权利要求书中所述，涉及制备所述化合物的方法，药物组合物和包含所述化合物的组合， 涉及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使用，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：US20080058358A1
公开(公告)日：2008-03-06
申请号：US11759479
申请日：2007-06-07
申请人： Ulrich Luecking , Duy Nguyen , Arne von Bonin , Oliver von Ahsen , Gerhard Siemeister , Rolf Jautelat , Wolf-Dietrich Doecke
发明人： Ulrich Luecking , Duy Nguyen , Arne von Bonin , Oliver von Ahsen , Gerhard Siemeister , Rolf Jautelat , Wolf-Dietrich Doecke
IPC分类号： A61K31/505 , A61K31/506 , A61P35/00 , C07D239/30 , C07D239/48 , C07D401/12
CPC分类号： C07D401/12 , C07D239/48
摘要： The invention relates to sulphimides as protein kinase inhibitors of the general formula I
摘要翻译： 本发明涉及作为通式I的蛋白激酶抑制剂的硫酰亚胺
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3.发明授权公开(公告)号：US07291624B2
公开(公告)日：2007-11-06
申请号：US10842419
申请日：2004-05-11
申请人： Thomas Brumby , Rolf Jautelat , Olaf Prien , Martina Schäfer , Gerhard Siemeister , Ulrich Lücking , Christoph Huwe
发明人： Thomas Brumby , Rolf Jautelat , Olaf Prien , Martina Schäfer , Gerhard Siemeister , Ulrich Lücking , Christoph Huwe
IPC分类号： A61K31/505 , C07D239/02
CPC分类号： C07D239/42 , C07D231/12 , C07D233/56 , C07D239/47 , C07D239/48 , C07D249/08 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/14 , C07D417/12 , C07D495/10 , C07F9/6512
摘要： This invention relates to pyrimidine derivatives of general formula I in which R1, R2, X, A and B have the meanings that are contained in the description, as inhibitors of the cyclin-dependent kinases, their production as well as their use as medications for treating various diseases.
摘要翻译： 本发明涉及通式I的嘧啶衍生物，其中R 1，R 2，X，A和B具有说明书中所含的含义，作为 细胞周期蛋白依赖性激酶，其生产以及用作治疗各种疾病的药物。
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4.发明申请N-aryl-sulfoximine-substituted pyrimidines as CDK-and/or VEGF inhibitors, their production and use as pharmaceutical agents 失效N-芳基 - 亚磺酰亚胺取代的嘧啶作为CDK和/或VEGF抑制剂，它们的生产和用作药剂公开(公告)号：US20060229325A1
公开(公告)日：2006-10-12
申请号：US11386111
申请日：2006-03-22
IPC分类号： A61K31/513 , A61K31/506 , C07D417/02
CPC分类号： C07D239/48 , C07D239/47 , C07D239/50 , C07D333/48 , C07D401/12 , C07D405/12 , C07D409/12
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具有本说明书所含的含义，作为细胞周期蛋白依赖性激酶和VEGF- 受体酪氨酸激酶，它们的生产以及它们作为用于治疗各种疾病的药物的用途。
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5.发明申请Substituted 2-anilinopyrimidines as cell-cycle-kinase or receptor-tyrosine-kinase inhibitors, their production and use as pharmaceutical agents 审中-公开取代的2-苯胺嘧啶嘧啶作为细胞周期激酶或受体 - 酪氨酸激酶抑制剂，其生产和用作药剂公开(公告)号：US20060111378A1
公开(公告)日：2006-05-25
申请号：US11238134
申请日：2005-09-29
申请人： Arwed Cleve , Ulrich Lucking , Christopher West , Hans Briem , Gerhard Siemeister , Marten Kruger , Rolf Jautelat , Philip Lienau
发明人： Arwed Cleve , Ulrich Lucking , Christopher West , Hans Briem , Gerhard Siemeister , Marten Kruger , Rolf Jautelat , Philip Lienau
IPC分类号： A61K31/513 , A61K31/505 , C07D239/46
CPC分类号： C07D239/47 , C07D239/48
摘要： This invention relates to pyrimidine derivatives of general formula I in which R1, R2, R3, R4, A and D 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 treating various diseases.
摘要翻译： 本发明涉及通式Ⅰ的嘧啶衍生物，其中R 1，R 2，R 3，R 4， >，A和D具有包含在说明书中的含义，作为细胞周期蛋白依赖性激酶和VEGF受体酪氨酸激酶的抑制剂，其生产以及其作为用于治疗各种疾病的药物的用途。
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6.发明申请Sulfoximine-substituted pyrimidines as CDK-and/or VEGF inhibitors, their production and use as pharmaceutical agents 有权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：US20050176743A1
公开(公告)日：2005-08-11
申请号：US10966098
申请日：2004-10-18
IPC分类号： A61K31/506 , A61K31/513 , C07D239/46 , C07D239/48 , C07D43/02
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 5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-受体酪氨酸激酶的抑制剂，其生产及其用途 用于治疗各种疾病的药物。
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![Substituted 6-fluoro-1H-pyrazolo[4,3-b]pyridines and use thereof](/abs-image/US/2016/04/12/US09309239B2/abs.jpg.150x150.jpg)
7.发明授权公开(公告)号：US09309239B2
公开(公告)日：2016-04-12
申请号：US13882118
申请日：2011-11-03
申请人： Markus Follmann , Johannes-Peter Stasch , Gorden Redlich , Jens Ackerstaff , Nils Griebenow , Andreas Knorr , Frank Wunder , Volkhart Min-Jian Li , Joachim Mittendorf , Karl-Heinz Schlemmer , Rolf Jautelat
发明人： Markus Follmann , Johannes-Peter Stasch , Gorden Redlich , Jens Ackerstaff , Nils Griebenow , Andreas Knorr , Frank Wunder , Volkhart Min-Jian Li , Joachim Mittendorf , Karl-Heinz Schlemmer , Rolf Jautelat
IPC分类号： C07D471/04 , A61K31/506 , A61K45/06
CPC分类号： C07D471/04 , A61K31/506 , A61K45/06
摘要： The present application relates to novel substituted 6-fluoro-1H-pyrazolo[4,3-b]pyridines, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for preparing Medicaments for the treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.
摘要翻译： 本申请涉及新的取代的6-氟-1H-吡唑并[4,3-b]吡啶，其制备方法，其用途，单独或组合用于治疗和/或预防疾病，以及 其用于制备药物用于治疗和/或预防疾病，特别是用于治疗和/或预防心血管疾病。
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8.发明申请IMIDAZOPYRAZINES FOR USE AS MPS-1 AND TKK INHIBITORS IN THE TREATMENT HYPERPROLIFERATIVE DISORDERS 审中-公开作为MPS-1和TKK抑制剂用于治疗高血压病症的咪唑吡嗪公开(公告)号：US20130303532A1
公开(公告)日：2013-11-14
申请号：US13994865
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： C07D471/04
CPC分类号： C07D471/04 , 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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9.发明申请SUBSTITUTED 6-IMIDAZOPYRAZINES FOR USE AS MPS-1 AND TKK INHIBITORS IN THE TREATMENT OF HYPERPROLIFERATIVE DISORDERS 有权用作MPS-1和TKK抑制剂治疗高血压疾病的替代的6-IMIDAZOPYRAZES公开(公告)号：US20130267527A1
公开(公告)日：2013-10-10
申请号：US13994335
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 , C07D403/02
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，用于制备所述化合物的方法和中间体， 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：US20130210815A1
公开(公告)日：2013-08-15
申请号：US13700956
申请日：2011-05-27
申请人： Ulrich Klar , Marcus Koppitz , Rolf Jautelat , Dirk Kosemund , Rolf Bohlmann , Benjamin Bader , Philip Lienau , Gerhard Siemeister , William Scott
发明人： Ulrich Klar , Marcus Koppitz , Rolf Jautelat , Dirk Kosemund , Rolf Bohlmann , Benjamin Bader , Philip Lienau , Gerhard Siemeister , William Scott
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/4985
摘要： The present invention relates to substituted imidazopyrazine compounds of general formula (I) in which A, R1, R3 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 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）的取代咪唑并吡嗪化合物，其中A，R 1，R 3和R 5如在说明书和权利要求书中所述，涉及制备所述化合物的方法，药物组合物和包含所述化合物的组合， 涉及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使用，以及可用于制备所述化合物的中间体化合物。
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