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公开(公告)号：US20120022084A1
公开(公告)日：2012-01-26
申请号：US13111856
申请日：2011-05-19
申请人： Markus Follmann , Johannes-Peter Stasch , Gorden Redlich , Jens Ackerstaff , Nils Griebenow , Walter Kroh , Andreas Knorr , Eva-Maria Becker , Frank Wunder , Volkhart Min-Jian Li , Elke Hartmann , Joachim Mittendorf , Karl-Heinz Schlemmer , Rolf Jautelat , Donald Bierer
发明人： Markus Follmann , Johannes-Peter Stasch , Gorden Redlich , Jens Ackerstaff , Nils Griebenow , Walter Kroh , Andreas Knorr , Eva-Maria Becker , Frank Wunder , Volkhart Min-Jian Li , Elke Hartmann , Joachim Mittendorf , Karl-Heinz Schlemmer , Rolf Jautelat , Donald Bierer
IPC分类号： A61K31/506 , A61P9/04 , A61P7/00 , A61P9/12 , A61P9/10 , A61P13/12 , C07D471/04 , A61P9/00
CPC分类号： A61K31/506 , A61K45/06 , C07C57/145 , C07C309/04 , C07C309/05 , C07D471/04
摘要： The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
摘要翻译： 本申请涉及新的取代的5-氟-1H-吡唑并吡啶，其制备方法，单独使用或组合用于治疗和/或预防疾病，以及它们用于制备用于治疗和/ 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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![Substituted imidazo[1,2b]pyridazines as kinase inhibitors, their preparation and use as medicaments](/abs-image/US/2010/07/06/US07750000B2/abs.jpg.150x150.jpg)
12.发明授权Substituted imidazo[1,2b]pyridazines as kinase inhibitors, their preparation and use as medicaments 失效取代的咪唑并[1,2b]哒嗪作为激酶抑制剂，其制备和用作药物公开(公告)号：US07750000B2
公开(公告)日：2010-07-06
申请号：US11514308
申请日：2006-09-01
申请人： Olaf Prien , Stuart James Ince , Knut Eis , Christoph Huwe , Ulrich Lücking , Rolf Jautelat , Ulrich Zügel , Judith Günther , Benjamin Bader , Manfred Husemann , Karina Schuck
发明人： Olaf Prien , Stuart James Ince , Knut Eis , Christoph Huwe , Ulrich Lücking , Rolf Jautelat , Ulrich Zügel , Judith Günther , Benjamin Bader , Manfred Husemann , Karina Schuck
IPC分类号： A61K31/4985 , A61K31/5355 , C07D487/04 , C07D413/12 , A61P3/10 , A61P11/06 , A61P29/00 , A61P17/06 , A61P17/00
CPC分类号： C07D487/04
摘要： The invention relates to novel inhibitors of kinases, and pharmaceutical compositions comprising them. The inhibitors are substituted imidazo[1,2b]pyridazines.
摘要翻译： 本发明涉及新型的激酶抑制剂和包含它们的药物组合物。 抑制剂是取代的咪唑并[1,2b]哒嗪。
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13.发明授权公开(公告)号：US07598260B2
公开(公告)日：2009-10-06
申请号：US11819307
申请日：2007-06-26
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R1，R2，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的抑制剂，其生产及其用作药物用途 治疗各种疾病。
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公开(公告)号：US20080167330A1
公开(公告)日：2008-07-10
申请号：US11892967
申请日：2007-08-28
IPC分类号： A61K31/505 , C07D239/48 , C07D239/47 , C07D409/04 , A61P35/00 , C07D239/42 , C07D239/34 , C07D403/02 , A61K31/513 , A61K31/506
CPC分类号： C07D239/47 , C07D239/48 , C07D403/12
摘要： The invention relates to carbamoylsulphoximides as protein kinase inhibitors of the general formula 1.
摘要翻译： 本发明涉及作为通式1的蛋白激酶抑制剂的氨基甲酰基亚砜。
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15.发明申请公开(公告)号：US20080039447A1
公开(公告)日：2008-02-14
申请号：US11819307
申请日：2007-06-26
申请人： Thomas Brumby , Rolf Jautelat , Olaf Prien , Martina Schafer , Gerhard Siemeister , Ulrich Lucking , Christoph Huwe
发明人： Thomas Brumby , Rolf Jautelat , Olaf Prien , Martina Schafer , Gerhard Siemeister , Ulrich Lucking , Christoph Huwe
IPC分类号： A61K31/505 , A61K31/496 , A61K31/5377 , A61K31/551 , A61P17/06 , A61P25/00 , A61P25/16 , A61P25/28 , A61P31/00 , A61P31/12 , A61P31/18 , A61P31/22 , A61P35/00 , A61P35/02 , A61P37/00 , A61P9/00 , C07D239/42 , C07D239/48 , C07D243/08 , C07D401/10 , C07D411/10
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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16.发明授权17α-ALKYL-17β-OXY-ESTRATRIENES AND INTERMEDIATE PRODUCTS FOR THEIR PRODUCTION, USE OF THE 17α-ALKYL-17β-OXY-ESTRATRIENES FOR THE PRODUCTION OF PHARMACEUTICAL AGENTS AS WELL AS PHARMACEUTICAL PREPARATIONS 失效17α-ALKYL-17β-OXY-ESTRATRIENES和其生产中间产品，17α-阿尔基-17β-氧化物酶用于生产药物代谢品，作为药物制剂公开(公告)号：US07018994B2
公开(公告)日：2006-03-28
申请号：US10305418
申请日：2002-11-27
申请人： Rolf Bohlmann , Nikolaus Heinrich , Rolf Jautelat , Jorg Kroll , Orlin Petrov , Andreas Reichel , Jens Hoffmann , Rosemarie Lichtner
发明人： Rolf Bohlmann , Nikolaus Heinrich , Rolf Jautelat , Jorg Kroll , Orlin Petrov , Andreas Reichel , Jens Hoffmann , Rosemarie Lichtner
CPC分类号： C07J43/003 , C07J41/0072
摘要： The invention relates to 17α-alkyl-17β-oxy-estra-1,3,5(10)-trienes that have an antiestrogenic action with general formula I. In addition, the invention also relates to 17-oxo-estra-1,3,5(10)-trienes as well as 17β-hydroxy-estra-1,3,5(10)-trienes as intermediate products in the production of the estratrienes according to the invention. The invention also relates to the use of 17α-alkyl-17β-oxy-estratrienes for the production of pharmaceutical agents as well as pharmaceutical preparations that contain at least one 17α-alkyl-17β-oxy-estratriene as well as at least one pharmaceutically compatible vehicle.
摘要翻译： 本发明涉及具有通式I的抗雌激素作用的17α-烷基-17β-氧 - 雌-1,3,5（10） - 三烯。此外，本发明还涉及17-氧代 - 雌-1 3,5（10） - 三烯以及17β-羟基 - 雌-1,3,5（10） - 三烯作为生产根据本发明的雌三醇的中间产物。 本发明还涉及17α-烷基-17β-氧 - 雌三烯在制备药剂中的用途以及含有至少一种17α-烷基-17β-氧 - 雌三醇的药物制剂以及至少一种药物相容性 车辆。
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![Substituted imidazo[1,2-a]pyrazines as MPS-1 inhibitors](/abs-image/US/2016/03/15/US09284317B2/abs.jpg.150x150.jpg)
公开(公告)号：US09284317B2
公开(公告)日：2016-03-15
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： A61K31/4985 , C07D241/36 , C07D487/04 , C07D403/02
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，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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18.发明申请6-THIO-SUBSTITUTED 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6-THIO替代的咪达唑仑公开(公告)号：US20130281460A1
公开(公告)日：2013-10-24
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： 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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![SUBSTITUTED 6-FLUORO-1H-PYRAZOLO[4,3-B]PYRIDINES AND USE THEREOF](/abs-image/US/2013/10/10/US20130267548A1/abs.jpg.150x150.jpg)
19.发明申请公开(公告)号：US20130267548A1
公开(公告)日：2013-10-10
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 , A61K45/06 , A61K31/506
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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20.发明申请SULFOXIMINE-SUBSTITUTED ANILINOPYRIMIDINE DERIVATIVES AS CDK INHIBITORS, THE PRODUCTION THEREOF, AND USE AS MEDICINE 有权作为CDK抑制剂的SULFOXIMINE取代的抗胰蛋白胨衍生物，其生产和用作医药公开(公告)号：US20110294838A1
公开(公告)日：2011-12-01
申请号：US13125066
申请日：2009-10-09
IPC分类号： A61K31/505 , C07D239/48 , A61P35/00 , C07D239/47
CPC分类号： C07D239/47
摘要： The invention relates to sulfoximine-substituted anilino-pyrimidine derivatives of formula (I). methods of production thereof, and use thereof as medication for the treatment of various diseases.
摘要翻译： 本发明涉及式（I）的磺酰亚胺取代的苯胺基 - 嘧啶衍生物。 其生产方法及其用作治疗各种疾病的药物。
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