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31. 发明授权

US5994536A Process for mono- and 1,7-bis-N-.beta.-hydroxyalkylation of cyclene; N-.beta.-hydroxyalkyl-1,4,7,10-tetraazacyclododecane-lithium-salt complexes and the use of the complexes for the production of gadobutrol and analogs 失效
标题翻译：环烯的单和1,7-双-β-羟烷基化方法; N-β-羟基烷基-1,4,7,10-四氮杂环十二烷 - 锂盐络合物和复合物用于生产钆布醇和类似物
公开(公告)号：US5994536A
公开(公告)日：1999-11-30
申请号：US88700
申请日：1998-06-02
申请人： Orlin Petrov , Peter Blaszkiewicz
发明人： Orlin Petrov , Peter Blaszkiewicz
IPC分类号： C07D257/02 , C07D405/04 , C07D487/22
CPC分类号： C07D405/04 , C07D257/02
摘要： The invention relates to the process for mono- and 1,7-bis-N-.beta.-hydroxyalkylation of cyclene, the corresponding mono- and 1,7-bis-N-.beta.-hydroxyalkyl-1,4,7,10-tetraazacyclododecane-Li-salt complexes as intermediate products in the process and the use of the N-(6-hydroxy-2,3-dimethyl-1,3-dioxepan-5-yl)-1,4,7,10-tetraazacyclododecane-LiCl complex for the production of gadobutrol [Gd ocmplex of N-(1-hydroxy-methyl-2,3-dihydroxypropyl)-1,4,7-triscarboxymethyl-1,4,7,10-tetraazacyclododecane].
摘要翻译：本发明涉及环己烯的单和1,7-双-β-羟烷基化方法，相应的单 - 和1,1-双-β-羟烷基-1,4,7,10-四氮杂环十二烷 -L-盐络合物作为该方法中的中间产物，并使用N-（6-羟基-2,3-二甲基-1,3-二氧杂环庚烷-5-基）-1,4,7,10-四氮杂环十二烷 - 用于生产钆布醇[N-（1-羟基 - 甲基-2,3-二羟丙基）-1,4,7-三羧甲基-1,4,7,10-四氮杂环十二烷的Gd ocmplex]的LiCl络合物。

32. 发明授权

US07951790B2 Progesterone receptor antagonists 有权
公开(公告)号：US07951790B2
公开(公告)日：2011-05-31
申请号：US11984331
申请日：2007-11-15
申请人： Ulrike Fuhrmann , Anja Schmidt , Arwed Cleve , Orlin Petrov , Gunnar Garke , Stefan Pruehs , Margarete Brudny-Kloeppel , Antje Rottmann , Rainer Hasselmann , Marcus Schultze-Mosgau , Carsten Moeller
发明人： Ulrike Fuhrmann , Anja Schmidt , Arwed Cleve , Orlin Petrov , Gunnar Garke , Stefan Pruehs , Margarete Brudny-Kloeppel , Antje Rottmann , Rainer Hasselmann , Marcus Schultze-Mosgau , Carsten Moeller
IPC分类号： A61K31/565 , C07J1/00
摘要： The present invention relates to progesterone receptor antagonists of general formula I: in which R1 can be a hydrogen atom and R2 a hydroxyl group or R1 and R2 together can be an oxo group.

33. 发明授权

US07902178B2 Progesterone receptor antagonists 有权
公开(公告)号：US07902178B2
公开(公告)日：2011-03-08
申请号：US11984331
申请日：2007-11-15
申请人： Ulrike Fuhrmann , Anja Schmidt , Arwed Cleve , Orlin Petrov , Gunnar Garke , Stefan Pruehs , Margarete Brudny-Kloeppel , Antje Rottmann , Rainer Hasselmann , Marcus Schultze-Mosgau , Carsten Moeller
发明人： Ulrike Fuhrmann , Anja Schmidt , Arwed Cleve , Orlin Petrov , Gunnar Garke , Stefan Pruehs , Margarete Brudny-Kloeppel , Antje Rottmann , Rainer Hasselmann , Marcus Schultze-Mosgau , Carsten Moeller
IPC分类号： A61K31/565 , C07J1/00
摘要： The present invention relates to progesterone receptor antagonists of general formula I: in which R1 can be a hydrogen atom and R2 a hydroxyl group or R1 and R2 together can be an oxo group.

34. 发明授权

US07012081B2 Anthranyl amides and their use as medicaments 失效
标题翻译：氨基酰胺和它们作为药物的用途
公开(公告)号：US07012081B2
公开(公告)日：2006-03-14
申请号：US10275479
申请日：2001-05-07
申请人： Martin Krueger , Andreas Huth , Orlin Petrov , Dieter Seidelmann , Karl-Heinz Thierauch , Martin Haberey , Andreas Menrad , Alexander Ernst
发明人： Martin Krueger , Andreas Huth , Orlin Petrov , Dieter Seidelmann , Karl-Heinz Thierauch , Martin Haberey , Andreas Menrad , Alexander Ernst
IPC分类号： A61K31/47 , C07D215/00 , C07D217/00
CPC分类号： C07D213/80 , C07C237/40 , C07D211/26 , C07D211/32 , C07D211/62 , C07D217/22 , C07D265/26 , C07D309/04 , C07D309/06 , C07D317/72 , C07D401/12 , C07D405/12
摘要： Substituted anthranilamides and use thereof as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis as well as their intermediate products for the production of anthranilamides are described.
摘要翻译：描述了取代的邻氨基苯甲酰胺及其用作治疗由持续血管发生引起的疾病的药物及其用于制备邻氨基苯甲酰胺的中间产物。

35. 发明授权

US07538100B2 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
标题翻译： 17α-烷基-17β-氧 - 雌三烯及其制备的中间产物，使用17α-烷基-17β-氧 - 雌三烯来制备药剂以及药物制剂
公开(公告)号：US07538100B2
公开(公告)日：2009-05-26
申请号：US11188992
申请日：2005-07-26
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
IPC分类号： A61K31/56 , C07J1/00
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。

36. 发明申请

US20060116396A1 5-Substituted quinoline and isoquinoline derivatives, a process for their production and their use as anti-inflammatory agents 失效
标题翻译： 5-取代的喹啉和异喹啉衍生物，其制备方法及其作为抗炎剂的用途
公开(公告)号：US20060116396A1
公开(公告)日：2006-06-01
申请号：US11272009
申请日：2005-11-14
申请人： Stefan Jaroch , Hartmut Rehwinkel , Heike Schaecke , Norbert Schmees , Werner Skuballa , Jan Huebner , Orlin Petrov , Matthias Schneider , Christian Dinter
发明人： Stefan Jaroch , Hartmut Rehwinkel , Heike Schaecke , Norbert Schmees , Werner Skuballa , Jan Huebner , Orlin Petrov , Matthias Schneider , Christian Dinter
IPC分类号： A61K31/4709 , C07D405/02
CPC分类号： C07D405/12
摘要： Compounds of general formula (IIa) or (IIb) and their use as pharmaceutical agents.
摘要翻译：通式（IIa）或（IIb）的化合物及其作为药剂的用途。

37. 发明申请

US20050261343A1 Anthranilamides and their use as pharmaceutical agents 审中-公开
标题翻译：邻氨基苯甲酰胺及其作为药剂的用途
公开(公告)号：US20050261343A1
公开(公告)日：2005-11-24
申请号：US11193421
申请日：2005-08-01
申请人： Martin Krueger , Andreas Huth , Orlin Petrov , Dieter Seidelmann , Karl-Heinz Thierauch , Martin Haberey , Andreas Menrad , Alexander Ernst
发明人： Martin Krueger , Andreas Huth , Orlin Petrov , Dieter Seidelmann , Karl-Heinz Thierauch , Martin Haberey , Andreas Menrad , Alexander Ernst
IPC分类号： C07C237/28 , A61K31/166 , A61K31/351 , A61K31/416 , A61K31/472 , A61K31/4725 , A61P1/16 , A61P7/10 , A61P9/10 , A61P9/14 , A61P13/12 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/04 , A61P25/00 , A61P27/02 , A61P27/06 , A61P29/00 , A61P35/00 , A61P37/00 , A61P41/00 , A61P43/00 , C07C237/30 , C07C237/40 , C07D211/16 , C07D211/26 , C07D211/32 , C07D211/60 , C07D211/62 , C07D213/80 , C07D217/02 , C07D217/22 , C07D265/26 , C07D309/04 , C07D309/06 , C07D317/72 , C07D401/12 , C07D405/12 , A61K31/445 , C07D45/02
CPC分类号： C07D213/80 , C07C237/40 , C07D211/26 , C07D211/32 , C07D211/62 , C07D217/22 , C07D265/26 , C07D309/04 , C07D309/06 , C07D317/72 , C07D401/12 , C07D405/12
摘要： Substituted anthranilamides and use thereof as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis as well as their intermediate products for the production of anthranilamides are described.
摘要翻译：描述了取代的邻氨基苯甲酰胺及其用作治疗由持续血管发生引起的疾病的药物及其用于制备邻氨基苯甲酰胺的中间产物。

38. 发明授权

US06891041B2 Method for producing 4-(heteroaryl-methyl)-halogen-1(2H)-phthalazinones 失效
标题翻译： 4-（杂芳基 - 甲基） - 卤素-1（2H） - 酞嗪酮的制备方法
公开(公告)号：US06891041B2
公开(公告)日：2005-05-10
申请号：US10168794
申请日：2000-12-20
申请人： Orlin Petrov , Thomas Heiner , Herribert Neh , Martin Kruger
发明人： Orlin Petrov , Thomas Heiner , Herribert Neh , Martin Kruger
IPC分类号： C07D401/06 , C07D403/06
CPC分类号： C07D401/06
摘要： A process for the production of 4-(heteroaryl-methyl)-halogen-1(2H)-phthalazinones, especially 4-(4-pyridylmethyl)-1(2H)-phthalazinone, is described, which is characterized by the reaction of phthalidyl-3-triphenylphosphonium salt with 4-pyridine aldehyde in the presence of a basic adjuvant, subsequent reaction with hydrazine hydrate and subsequent acid treatment, whereby this process avoids the technical safety and environmental problems of the known processes.
摘要翻译：描述了制备4-（杂芳基 - 甲基） - 卤素-1（2H） - 酞嗪酮，特别是4-（4-吡啶基甲基）-1（2H） - 酞嗪酮的方法，其特征在于苯酞 -3-三苯基鏻盐与4-吡啶醛在碱性助剂的存在下反应，随后与水合肼反应并随后进行酸处理，由此该方法避免了已知方法的技术安全性和环境问题。

39. 发明申请

US20110009654A1 11B-FLUORO-3-ACETOXYESTRA-3,5-DIEN-17-ONE AND METHOD FOR THE PRODUCTION THEREOF 审中-公开
标题翻译： 11B-氟-3-乙酰氧基-3,5-二苯基-17-酮及其生产方法
公开(公告)号：US20110009654A1
公开(公告)日：2011-01-13
申请号：US12739195
申请日：2008-10-18
申请人： Orlin Petrov , Matthias Schneider , Rolf Bohlmann , Stephan Vettel
发明人： Orlin Petrov , Matthias Schneider , Rolf Bohlmann , Stephan Vettel
IPC分类号： C07J75/00 , C07J1/00
CPC分类号： C07J1/0059
摘要： The present invention relates to 11β-fluoro-3-acetoxyestra-3,5-dien-17-one as a suitable intermediate in the preparation of 11-fluoro-substituted steroids and to the process for preparation thereof. For this purpose, 11α-hydroxyestra-4-ene-3,17-dione is reacted with 1 to 3 equivalents of n-nonafluorobutanesulfonyl fluoride and 3 to 5 equivalents of diazabicycloundecene (DBU) at −40 to −20° C. in an organic aprotic solvent and, after an aqueous workup, reacted with 5 to 10 equivalents of acetic anhydride and 0.01 to 1 equivalent of a strong acid. The desired product precipitates spontaneously out of the reaction solution and is obtained in a very high purity by filtration. The process is notable for the very high yield, avoidance of a chromatographic purification of the product, a reduced proportion of wastes and significantly increased process throughput. The process according to the invention is therefore especially suitable for preparing 11β-fluoro-3-acetoxyestra-3,5-dien-17-one on a large industrial scale.
摘要翻译：本发明涉及11-氟-3-乙酰氧基雌-3,5-二烯-17-酮作为制备11-氟取代的类固醇的合适中间体及其制备方法。为此，将11α-羟基雌-4-烯-3,17-二酮与1至3当量的正 - 九氟丁磺酰氟和3至5当量的二氮杂双环十一碳烯（DBU）在-40至-20℃下反应，有机非质子溶剂，在水处理后，与5至10当量的乙酸酐和0.01至1当量的强酸反应。所需产物自发地从反应溶液中沉淀出来，通过过滤得到非常高的纯度。该方法是非常高的产量，避免产品的色谱纯化，减少的废物比例和显着增加的工艺生产量。因此，根据本发明的方法特别适用于大型工业规模的制备11-全氟-3-乙酰氧基雌-3,5-二烯-17-酮。

40. 发明申请

US20080242866A1 SYNTHESIS OF ANTHRANILAMIDES 审中-公开
标题翻译：苯磺酰胺的合成
公开(公告)号：US20080242866A1
公开(公告)日：2008-10-02
申请号：US12056572
申请日：2008-03-27
申请人： Norbert SCHMEES , Orlin Petrov
发明人： Norbert SCHMEES , Orlin Petrov
IPC分类号： C07D401/12 , C07D213/82
CPC分类号： C07D401/12
摘要： The present invention relates to a novel method of preparing anthranilamides of formula I: in which R1, R2, R3, A, E, Q, X, and W are defined in the claims, to a novel intermediate compound, and to the use of said novel intermediate compound for the preparation of said anthranilamides of formula I.
摘要翻译：本发明涉及制备式I的邻氨基苯甲酰胺的新方法：其中R 1，R 2，R 3，A，E Q，X和W在权利要求书中被定义为新的中间体化合物，以及所述新型中间体化合物用于制备式I的所述邻氨基苯甲酰胺的用途。

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