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1. 发明授权

US06956031B2 11β-Substituted 19-nor-17-α-pregna-1,3,5(10)-trien-17β-ols with a 21,16α-lactone ring 失效
标题翻译： 11beta取代的19-nor-17-α-前 - 1,3,5（10） - 三烯-17β-酯与21,16α-内酯环
公开(公告)号：US06956031B2
公开(公告)日：2005-10-18
申请号：US10397855
申请日：2003-03-27
申请人： Alexander Hillisch , Walter Elger , Rolf Bohlmann , Jens Hoffmann
发明人： Alexander Hillisch , Walter Elger , Rolf Bohlmann , Jens Hoffmann
IPC分类号： A61K31/58 , A61K31/585 , C07J17/00 , C07J71/00
CPC分类号： C07J17/00
摘要： This invention relates to new 19-nor-17α-pregna-1,3,5(10)-trien-17β-ols with a 21,16α-lactone ring with a long-chain substituent in 11β-position of general formula II in which R11 is a long-chain alkyl radical that has a nitrogen atom that can be substituted in terminal position with a perfluoroalkyl group. The compounds act in a tissue-selective manner as pure antiestrogens and are suitable for the production of pharmaceutical agents because of these properties.
摘要翻译：本发明涉及具有21,16α-内酯环的新的19-nor-17α-前 - 1,3,5（10） - 三烯-17β-环，其通式II在11b位具有长链取代基其中R 11是具有可以在末端被全氟烷基取代的氮原子的长链烷基。化合物以组织选择性的方式作为纯抗雌激素起作用，并且由于这些性质而适用于制药。

2. 发明授权

US06790842B1 11&bgr; LONG-CHAIN SUBSTITUTED ESTRATRIENES, METHOD FOR THEIR PRODUCTION, PHARMACEUTICAL PREPARATIONS CONTAINING SAID 11&bgr; LONG-CHAIN SUBSTITUTED ESTATRIENES, AND THEIR USE FOR PRODUCING MEDICAMENTS 失效
标题翻译： 11β长链取代的ESTRATRIENES，其生产方法，含有11β长链取代的ESTATRIRIES的药物制剂及其用于生产药物的用途
公开(公告)号：US06790842B1
公开(公告)日：2004-09-14
申请号：US10018429
申请日：2002-05-07
申请人： Rolf Bohlmann , Nikolaus Heinrich , Jorg Kroll , Gerhard Sauer , Karl-Heinrich Fritzemeier , Christa Hegele-Hartung , Jens Hoffmann , Rosemarie Lichtner , Ludwig Zorn
发明人： Rolf Bohlmann , Nikolaus Heinrich , Jorg Kroll , Gerhard Sauer , Karl-Heinrich Fritzemeier , Christa Hegele-Hartung , Jens Hoffmann , Rosemarie Lichtner , Ludwig Zorn
IPC分类号： A61K3158
CPC分类号： C07J1/00
摘要： This invention describes a 11&bgr;-long-chain-substituted estratriene of general formula (I), in which R11 is a long-chain radical that has a nitrogen atom and optionally a sulfur atom, which in addition can be functionalized in the terminal position with a perfluoroalkyl group or an optionally substituted arly radical. The compound can have antiestrogenic or tissue-selective estrogenic properties and be suitable for the production of pharmaceutical agents.
摘要翻译：本发明描述了通式（I）的11b-长链取代的雌三烯，其中R 11是具有氮原子和任选的硫原子的长链基团，其还可以在具有全氟烷基或任选取代的芳基的末端位置。该化合物可以具有抗雌激素或组织选择性雌激素特性，并且适用于生产药剂。

3. 发明申请

US20120157421A1 17Beta-Alkyl-17Alpha-oxy-estratrienes 审中-公开
标题翻译： 17β-烷基-17α-氧 - 雌三烯
公开(公告)号：US20120157421A1
公开(公告)日：2012-06-21
申请号：US13376194
申请日：2010-05-26
申请人： Rolf Bohlmann , Nikolaus Heinrich , Jan Hübner , Georg Kettschau , Hermann Künzer , Philip Lienau , Michael Gerisch , Silke Köhr , Dieter Lang , Karsten Denner , Michael Sander , Jens Hoffmann , Tim Wintermantel
发明人： Rolf Bohlmann , Nikolaus Heinrich , Jan Hübner , Georg Kettschau , Hermann Künzer , Philip Lienau , Michael Gerisch , Silke Köhr , Dieter Lang , Karsten Denner , Michael Sander , Jens Hoffmann , Tim Wintermantel
IPC分类号： A61K31/58 , A61K31/56 , C07J3/00 , A61P5/30 , C07J31/00 , C07J41/00 , C07J43/00
CPC分类号： A61K31/56 , C07J41/0072 , C07J43/003
摘要： The invention relates to 17β-alkyl-17α-oxy-oestratrienes of the formula (I), to processes for their preparation, to the use of the 17β-alkyl-17α-oxy-oestratrienes for preparing pharmaceuticals and to pharmaceutical preparations comprising these compounds.
摘要翻译：本发明涉及式（I）的17α-烷基-17α-氧 - 三亚甲基三醇，其制备方法，17α-烷基-17α-氧 - 二亚甲基三唑在制备药物中的用途以及药物制剂，其包含这些化合物。

4. 发明申请

US20060009436A1 17alpha-alkyl-17beta-oxy-estratrienes and intermediate products for their production, use of the 17alpha-alkyl-17beta-oxy-estratrienes for the production of pharmaceutical agents as well as pharmaceutical preparations 失效
公开(公告)号：US20060009436A1
公开(公告)日：2006-01-12
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： A61K31/57
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.

5. 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。

6. 发明授权

US07018994B2 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-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
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。

7. 发明授权

US07119082B2 11β-long-chain-substituted 19-nor-17α-pregna-1,3,5(10)-trien-17β-ols with a 21,16α-lactone ring 失效
标题翻译：具有21,16α-内酯环的11β-长链取代的19-去甲-17α-前 - 1,3,5（10） - 三烯-17β-
公开(公告)号：US07119082B2
公开(公告)日：2006-10-10
申请号：US10397854
申请日：2003-03-27
申请人： Gerd Mueller , Jens Hoffmann , Karl-Heinrich Fritzemeier , Alexander Hillisch
发明人： Gerd Mueller , Jens Hoffmann , Karl-Heinrich Fritzemeier , Alexander Hillisch
IPC分类号： A61K31/58 , C07J71/00
CPC分类号： C07J17/00
摘要： This invention relates to new 19-nor-17α-pregna-1,3,5(10)-trien-17β-ols with a 21,16α-lactone ring with a long-chain substituent in 11β-position of general formula II in which R11 means a straight-chain alkyl radical with 6 to 17 carbon atoms, and R3 and R13 have the meanings that are explained in more detail in the description. The compounds act in a tissue-selective manner as pure antiestrogens and are suitable for the production of pharmaceutical agents because of these properties.
摘要翻译：本发明涉及具有21,16α-内酯环的新的19-nor-17α-前 - 1,3,5（10） - 三烯-17β-环，其通式II在11b位具有长链取代基其中R 11表示具有6至17个碳原子的直链烷基，R 3和R 13和R 13具有所述的含义在描述中更详细。化合物以组织选择性的方式作为纯抗雌激素起作用，并且由于这些性质而适用于制药。

8. 发明授权

US08026229B2 Antitumor-active 2-alkoxyestradiol sulfamates 失效
标题翻译：抗肿瘤活性2-烷氧基雌二醇亚磺酸盐
公开(公告)号：US08026229B2
公开(公告)日：2011-09-27
申请号：US10217165
申请日：2002-08-13
申请人： Ina Scherlitz-Hofmann , Jens Hoffmann , Alexander Hillisch , Eberhard Unger , Tobias Neumann , Sigfrid Schwarz , Olaf Peters , Thomas Michel
发明人： Ina Scherlitz-Hofmann , Jens Hoffmann , Alexander Hillisch , Eberhard Unger , Tobias Neumann , Sigfrid Schwarz , Olaf Peters , Thomas Michel
IPC分类号： A61K31/56 , C07J1/00
CPC分类号： A61K31/565 , A61K31/56
摘要： The present invention relates to the use of 2-alkoxyestrogen sulfamates of general formula I wherein R1 and R2 independently represent H, methyl, C1-C4 acyl, benzoyl R3 represents C1-C4 alkyl or a group of formula CnFmHo, wherein n=1, 2, 3, 4, 5 or 6, m>1, and m+o=2n+1, R4 and R5 in each case represent H or, together, a methylene group or an additional double bond, R6 represents H, R7 represents OH, OC1-C4-alkyl, OC1-C11-acyl or OSO2NR1R2, the dashed lines in the B and C rings of the steroid skeleton additionally representing up to two double bonds, for the production of a medical drug for the treatment of tumor diseases which can be affected positively by inhibiting the tubulin polymerization. The inventive compounds are distinguished by the 2-alkoxy substitution in conjunction with the 17-hydroxy substitution. They have a special effect with regard to inhibiting tubulin polymerization and can be used, for example, for the treatment of prostate cancers.
摘要翻译：本发明涉及通式Ⅰ的2-烷氧基雌激素亚磺酸盐的用途，其中R 1和R 2独立地表示H，甲基，C 1 -C 4酰基，苯甲酰基，R 3表示C 1 -C 4烷基或式C n F m H 0基团，其中n = 2，3，4，5或6，m≥1，m + o = 2n + 1，R4和R5各自表示H或一起为亚甲基或另外的双键，R6表示H，R7表示 OH，OC1-C4-烷基，OC1-C11-酰基或OSO2NR1R2，类固醇骨架的B和C环中的虚线另外代表多达两个双键，用于生产用于治疗肿瘤疾病的药物这可以通过抑制微管蛋白聚合而受到积极的影响。本发明化合物通过2-烷氧基取代与17-羟基取代相结合来区分。它们在抑制微管蛋白聚合方面具有特殊的效果，并且可以用于例如前列腺癌的治疗。

9. 发明授权

US09175737B2 Drum brake module which can be operated by electric motor 有权
标题翻译：可由电动机操作的鼓式制动模块
公开(公告)号：US09175737B2
公开(公告)日：2015-11-03
申请号：US13976704
申请日：2012-02-02
申请人： Uwe Bach , Holger von Hayn , Ralf Sundheim , Wolfgang Ritter , Ahmed Sefo , Jürgen Balz , Jens Hoffmann , Martin Semsch , Götz Mehner , Dirk Sundheim
发明人： Uwe Bach , Holger von Hayn , Ralf Sundheim , Wolfgang Ritter , Ahmed Sefo , Jürgen Balz , Jens Hoffmann , Martin Semsch , Götz Mehner
IPC分类号： F16D65/10 , F16D51/10 , F16D51/16 , F16D51/46 , F16D65/16 , F16D65/22 , F16D51/18 , F16D51/12 , F16D121/24 , F16D125/24 , F16D125/40 , F16D125/60
CPC分类号： F16D51/10 , F16D51/12 , F16D51/16 , F16D51/18 , F16D51/46 , F16D65/16 , F16D65/22 , F16D2121/24 , F16D2125/24 , F16D2125/40 , F16D2125/60
摘要： A drum brake module for motor vehicles operable by electric motor and performs at least one parking brake function, having an electromechanical actuator mounted on one side of the armature plate and a rotational-translational movement converter converting a rotational drive rotational movement into a translational activation movement of brake shoes arranged on a side of the armature plate facing away from the actuator in a brake drum, and including at least one supporting device between the brake shoes such that the latter can carry out an activation movement in the direction of the brake drum. A drive nut is supported by the rotational-translational movement converter in an axially secure and rotatable fashion on the armature plate to assist the braking force. The drive nut drives a spindle arrangement mounted in a rotationally fixed and axially displaceable fashion and engages with an activation cable on at least one brake shoe.
摘要翻译：一种用于机动车辆的鼓式制动器模块，其可由电动机操作并且执行至少一个驻车制动功能，其具有安装在所述衔铁板的一侧上的机电致动器和将旋转驱动旋转运动转换成平移激活运动的旋转平移运动转换器在制动鼓中布置在衔铁板背离驱动器的一侧的制动蹄，并且在制动蹄之间包括至少一个支撑装置，使得后者可以在制动鼓的方向上进行启动运动。驱动螺母由旋转平移运动转换器以轴向固定和可旋转的方式支撑在衔铁板上以辅助制动力。驱动螺母驱动以旋转固定和可轴向移动的方式安装的主轴装置，并与至少一个制动蹄上的启动电缆接合。

10. 发明申请

US20080268041A1 COMBINATION OF PROGESTERONE-RECEPTOR ANTAGONIST TOGETHER WITH NONE-STEROIDAL ANTIESTROGEN FOR USE IN BRCA MEDIATED DISEASES 审中-公开
标题翻译：孕激素受体拮抗剂与无症状性静脉注射用于BRCA介导的疾病的组合
公开(公告)号：US20080268041A1
公开(公告)日：2008-10-30
申请号：US12105357
申请日：2008-04-18
申请人： Jens Hoffmann , Daniel Korr
发明人： Jens Hoffmann , Daniel Korr
IPC分类号： A61K9/48 , A61K31/575 , A61P35/00
CPC分类号： A61K31/138 , A61K31/00 , A61K31/567 , A61K45/06 , A61K2300/00
摘要： The present invention relates to the combination of the progesterone-receptor antagonist 11β-(4-acetylphenyl)-17β-hydroxy-17α-(1,1,2,2,2-pentafluoroethyl)-estra-4,9-dien-3-one or a pharmaceutically acceptable derivative or analogue thereof, together with at least one none-steroidal antiestrogen and to the use of said combination for the prophylaxis and treatment of BRCA1- or BRCA2-mediated diseases. None-steroidal antiestrogens which can be combined together with the progesterone-receptor antagonist 11β-(4-acetylphenyl)-17β-hydroxy-17α-(1,1,2,2,2-pentafluoroethyl)-estra-4,9-dien-3-one are for example is tamoxifen, raloxifene, droloxifen, toremifen, lasofoxifen, arzoxifen, GW5638, EM-800, idoxifen and basedoxifene.
摘要翻译：本发明涉及孕酮受体拮抗剂11beta-（4-乙酰基苯基）-17β-羟基-17α-（1,1,2,2,2-五氟乙基） - 雌-4,9-二烯-3 一种或其药学上可接受的衍生物或类似物，以及至少一种非甾体抗雌激素，以及所述组合用于预防和治疗BRCA1或BRCA2介导的疾病的用途。无甾体抗雌激素可与孕酮受体拮抗剂11beta-（4-乙酰基苯基）-17β-羟基-17α-（1,1,2,2,2-五氟乙基） - 雌-4,9-二烯例如，他莫昔芬，雷洛昔芬，屈昔洛芬，托瑞米芬，拉索福昔芬，阿唑西芬，GW5638，EM-800，艾多昔芬和依诺昔芬。

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