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公开(公告)号：US07235561B2
公开(公告)日：2007-06-26
申请号：US10156759
申请日：2002-05-29
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 , A61P35/00
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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2.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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3.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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4.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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![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)
5.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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![Substituted imidazo[1,2b]pyridazines as kinase inhibitors, their preparation and use as medicaments](/abs-image/US/2007/04/26/US20070093490A1/abs.jpg.150x150.jpg)
6.发明申请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：US20070093490A1
公开(公告)日：2007-04-26
申请号：US11514308
申请日：2006-09-01
申请人： Olaf Prien , Stuart Ince , Knut Eis , Christoph Huwe , Ulrich Lucking , Rolf Jautelat , Ulrich Zugel , Judith Gunther , Benjamin Bader , Manfred Husemann , Karina Schuck
发明人： Olaf Prien , Stuart Ince , Knut Eis , Christoph Huwe , Ulrich Lucking , Rolf Jautelat , Ulrich Zugel , Judith Gunther , Benjamin Bader , Manfred Husemann , Karina Schuck
IPC分类号： A61K31/503 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to novel inhibitors of kinases, methods for preparing such inhibitors, intermediates for the preparation of such inhibitors and uses of such inhibitors.
摘要翻译： 本发明涉及新型的激酶抑制剂，制备这种抑制剂的方法，制备这种抑制剂的中间体和这种抑制剂的用途。
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7.发明申请Quinoline derivatives, their preparation, their use, and medicaments comprising them 审中-公开喹啉衍生物，其制备方法，用途以及包含它们的药物公开(公告)号：US20080056987A1
公开(公告)日：2008-03-06
申请号：US11765683
申请日：2007-06-20
申请人： Olaf Prien , Knut Eis , Duy Nguyen , Christoph Huwe , Wolfgang Schwede , Judith Guenther , Dieter Zopf
发明人： Olaf Prien , Knut Eis , Duy Nguyen , Christoph Huwe , Wolfgang Schwede , Judith Guenther , Dieter Zopf
IPC分类号： A61K51/00 , A61K31/47 , A61P25/00 , A61P9/00 , C07D295/00 , C12Q1/00 , C12N9/99 , C07D215/00 , A61P43/00 , A61K31/5377
CPC分类号： C07D513/04 , C07D495/04
摘要： The present invention relates to a quinoline derivative having the general formula (A) in which R1, R2, W, X, Y and Z are indicated in the description and the claims, the use of the compounds of the general formula (A) for the treatment of various disorders, and the preparation of compounds of the general formula (A).
摘要翻译： 本发明涉及具有通式（A）的喹啉衍生物，其中R 1，R 2，W，X，Y和Z在说明书中表示， 权利要求书，通式（A）的化合物用于各种病症的治疗，以及制备通式（A）的化合物。
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8.发明申请SUBSTITUTED ISOXAZOLINES, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME, METHODS OF PREPARING SAME, AND USES OF SAME 审中-公开取代的ISOXAZOLINES，含有其的药物组合物，其制备方法及其用途公开(公告)号：US20080027059A1
公开(公告)日：2008-01-31
申请号：US11776232
申请日：2007-07-11
申请人： Dominic Brittain , Benjamin Bader , Philip Lienau , Gerhard Siemeister , Takayuki Tatamiya , Hilmar Weinmann , Christoph Huwe
发明人： Dominic Brittain , Benjamin Bader , Philip Lienau , Gerhard Siemeister , Takayuki Tatamiya , Hilmar Weinmann , Christoph Huwe
IPC分类号： A61K31/42 , A61K31/443 , A61K31/47 , A61K31/498 , A61K31/5377 , A61P27/06 , A61P33/02 , A61P33/06 , A61P37/00 , A61P37/08 , A61P7/00 , C07D215/06 , C07D241/38 , C07D261/04 , C07D413/10
CPC分类号： C07D261/04 , C07D261/08 , C07D261/10 , C07D261/14 , C07D261/18 , C07D413/12
摘要： The invention relates to substituted isoxazolines according to the general formula (I): in which A, R1, R2, R3, R4, Z, X, m, n, and p, are given in the claims, and salts thereof, to pharmaceutical compositions comprising said substituted isoxazolines, to methods of preparing said substituted isoxazolines as well as the use thereof for manufacturing a pharmaceutical composition for the treatment of diseases known to be at least in part mediated by HDAC activity or whose symptoms are known to be alleviated by HDAC inhibitors.
摘要翻译： 本发明涉及根据通式（I）的取代的异恶唑啉：其中A，R 1，R 2，R 3，R 4，Z，X，m，n和p及其盐在权利要求书中给出， 包含所述取代的异恶唑啉的组合物，制备所述取代的异恶唑啉的方法及其制备用于治疗已知至少部分由HDAC活性介导的疾病或其症状已被HDAC缓解的疾病的药物组合物的用途 抑制剂。
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公开(公告)号：US09085603B2
公开(公告)日：2015-07-21
申请号：US13577799
申请日：2011-02-08
申请人： Wolfgang Schwede , Ulrich Klar , Carsten Möller , Andrea Rotgeri , Wilhelm Bone , Christoph Huwe
发明人： Wolfgang Schwede , Ulrich Klar , Carsten Möller , Andrea Rotgeri , Wilhelm Bone , Christoph Huwe
IPC分类号： A61K31/58 , A61K31/567 , C07J1/00 , C07J43/00 , C07J41/00 , A61K31/573
CPC分类号： C07J43/003 , A61K31/573 , A61K31/58 , C07J41/0083
摘要： The invention relates to 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of the formula I with a progesterone antagonizing effect and processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and also their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular of uterus fibroids (myomas, uterine leiomyomas), endometriosis, heavy menstrual bleeding, meningiomas, hormone-dependent breast cancers and troubles associated with the menopause or for monitoring fertility and emergency contraception.
摘要翻译： 本发明涉及具有孕酮拮抗作用的式I的17-羟基-17-五氟乙基 - 雌-4,9（10） - 二烯-11-芳基衍生物及其制备方法及其用于治疗和/或 疾病的预防及其用于治疗和/或预防疾病，特别是子宫肌瘤（肌瘤，子宫平滑肌瘤），子宫内膜异位症，重度月经出血，脑膜瘤，激素依赖性乳腺癌和与 更年期或监测生育和紧急避孕。
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公开(公告)号：US09109004B2
公开(公告)日：2015-08-18
申请号：US13578500
申请日：2011-02-08
申请人： Wolfgang Schwede , Ulrich Klar , Carsten Möller , Andrea Rotgeri , Wilhelm Bone , Christoph Huwe
发明人： Wolfgang Schwede , Ulrich Klar , Carsten Möller , Andrea Rotgeri , Wilhelm Bone , Christoph Huwe
CPC分类号： C07J43/003 , A61K31/57 , A61K31/58 , C07J41/0083
摘要： The invention relates to 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of formula I with progesterone-antagonizing action and methods of production thereof, use thereof for the treatment and/or prevention of diseases and use thereof for producing medicinal products for the treatment and/or prevention of diseases, in particular uterine fibroids (myomata, uterine leiomyomata), endometriosis, heavy menstrual bleeding, meningiomata, hormone-dependent breast cancers and menopause-associated complaints or for fertility control and emergency contraception.
摘要翻译： 本发明涉及式I的17-羟基-17-五氟乙基 - 雌-4,9（10） - 二烯-11-芳基衍生物与孕酮拮抗作用及其生产方法，其用于治疗和/或预防 的疾病及其用于生产用于治疗和/或预防疾病的药物的用途，特别是子宫肌瘤（肌瘤，子宫平滑肌瘤），子宫内膜异位症，重度月经出血，脑膜炎，激素依赖性乳腺癌和绝经相关的投诉或用于 生育控制和紧急避孕。
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