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81. 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。

82. 发明申请

US20100317632A1 17-(1'PROPENYL)-17-3'-OXIDOESTRA-4-EN-3-ONE DERIVATIVE, USE THEREOF, AND MEDICAMENT CONTAINING SAID DERIVATIVE 有权
标题翻译： 17-（1'PROPENYL）-17-3'-OXIDOESTRA-4-EN-3-ONE衍生物，其用途和含有衍生物的药物
公开(公告)号：US20100317632A1
公开(公告)日：2010-12-16
申请号：US12810858
申请日：2008-12-23
申请人： Ulrich Klar , Joachim Kuhnke , Rolf Bohlmann , Jan Hubner , Sven Ring , Thomas Frenzel , Frederik Menges , Steffen Borden , Hans Peter Muhn , Katja Prelle
发明人： Ulrich Klar , Joachim Kuhnke , Rolf Bohlmann , Jan Hubner , Sven Ring , Thomas Frenzel , Frederik Menges , Steffen Borden , Hans Peter Muhn , Katja Prelle
IPC分类号： A61K31/58 , C07J21/00 , A61P15/18
CPC分类号： C07J21/00 , C07J41/0016 , C07J53/001 , C07J53/007
摘要： The invention relates to 17-(1′-propenyl)-17-3′-oxidoestra-4-en-3-one derivatives with the general chemical formula I, where the residues Z, R4, R6a, R6b, R7, R15, R16a, R16b and R18 have the meanings stated in Claim 1, and their solvates, hydrates and salts, including all stereoisomers of these compounds. The invention further relates to the use of these derivatives for the production of a medicinal product for oral contraception and for the treatment of pre-, peri- and postmenopausal complaints and medicinal products that contain said derivatives, and in particular application in the aforementioned indications. The derivatives according to the invention have a progestational and in preferred cases additionally an antimineralocorticoid and neutral to slightly androgenic action.
摘要翻译：本发明涉及具有一般化学式I的17-（1'-丙烯基）-17-3'-氧代雌-4-烯-3-酮衍生物，其中残基Z，R4，R6a，R6b，R7，R15， R16a，R16b和R18具有权利要求1所述的含义，及其溶剂合物，水合物和盐，包括这些化合物的所有立体异构体。本发明还涉及这些衍生物用于生产口服避孕用药物和用于治疗绝经前，绝经期和绝经后的投诉和含有所述衍生物的药用产品的用途，特别是在上述适应症中的应用。根据本发明的衍生物具有促孕作用，在优选情况下另外具有抗皮质激素和中性至轻度雄激素作用。

83. 发明授权

US07846917B2 18-Methyl-19-norandrost-4-ene 17, 17-spiro ether (18-methyl-19-nor-20-spirox-4-en-3-one), and pharmaceutical products comprising the same 有权
标题翻译： 18-甲基-19-去雄甾-4-烯17,17-螺醚（18-甲基-19-去甲-20-螺-4-烯-3-酮）和包含它们的药物
公开(公告)号：US07846917B2
公开(公告)日：2010-12-07
申请号：US11769952
申请日：2007-06-28
申请人： Rolf Bohlmann , Joachim Kuhnke , Jan Huebner , Norbert Gallus , Frederik Menges , Steffen Borden , Hans-Peter Muhn , Katja Prelle
发明人： Rolf Bohlmann , Joachim Kuhnke , Jan Huebner , Norbert Gallus , Frederik Menges , Steffen Borden , Hans-Peter Muhn , Katja Prelle
IPC分类号： A61K31/58 , C07J21/00
CPC分类号： C07J53/008
摘要： The present invention describes the novel 18-methyl-19-norandrost-4-ene 17,17-spiro ethers of the general formula I in which Z is an oxygen atom, two hydrogen atoms, a group ═NOR or ═NNHSO2R, where R is a hydrogen atom or a straight- or branched-chain alkyl group having 1 to 4 or 3 to 4 carbon atoms, R4 is a hydrogen atom, a halogen atom or a trifluoromethyl group, and R6 and/or R7 may have α or β configuration, and R6 and R7 are independently of one another a hydrogen atom or a straight- or branched-chain alkyl group having 1 to 4 or 3 to 4 carbon atoms or a straight- or branched-chain alkenyl group having 2 to 4 or 3 to 4 carbon atoms or a saturated cycloalkyl group having 3 to 5 carbon atoms or together are a methylene group or a double bond. The novel compounds have progestational and antimineralocorticoid activity.
摘要翻译：本发明描述了通式I的新颖的18-甲基-19-壬二酰-4-烯17,17-螺醚，其中Z是氧原子，两个氢原子，一个= NOOR或= NONHSO 2 R，其中R 是氢原子或具有1-4个或3至4个碳原子的直链或支链烷基，R4是氢原子，卤素原子或三氟甲基，R 6和/或R 7可以具有α或> bgr ; 构型，R 6和R 7彼此独立地为氢原子或具有1至4或3至4个碳原子的直链或支链烷基或具有2至4或3个直链或支链的链烯基至4个碳原子或具有3至5个碳原子的饱和环烷基或一起是亚甲基或双键。新化合物具有促孕和抗皮质激素活性。

84. 发明申请

US20090099250A1 BENZOCYCLOHEPTENE DERIVATIVES AS ESTROGENS HAVING SELECTIVE ACTIVITY 审中-公开
标题翻译：作为具有选择性活性的雌激素的苄基胆碱衍生物
公开(公告)号：US20090099250A1
公开(公告)日：2009-04-16
申请号：US12249056
申请日：2008-10-10
申请人： Ralf WYRWA , Olaf Peters , Rolf Bohlmann , Peter Droescher , Katja Prelle , Karl Heinrich Fritzemeier , Hans Peter Muhn
发明人： Ralf WYRWA , Olaf Peters , Rolf Bohlmann , Peter Droescher , Katja Prelle , Karl Heinrich Fritzemeier , Hans Peter Muhn
IPC分类号： A61K31/381 , C07C39/17 , A61K31/122 , A61K31/05 , A61P5/00 , C07C49/747 , C07D333/16
CPC分类号： C07C39/23 , C07C39/17 , C07C43/23 , C07D333/16
摘要： The present invention describes non-steroidal compounds of the general formula (I) in which A is in which X1 means one or more groups on the phenyl ring and represents independently of one another a halogen, OH, (C1-C4)alkyl, (C1-C4)alkyl-O, (C3-C6)cycloalkyl-O, (C1-C14)acyl-O, (C1-C4)alkenyl, (C1-C4)alkynyl, perfluoro(C1-C4)alkyl radical, —CHO or CN, and X2 means one or more groups on the phenyl ring and represents independently of one another an H, halogen, OH, (C1-C4)alkyl, (C1-C4)alkyl-O, (C1-C4)alkenyl, (C1-C4)alkynyl, perfluoro-(C1-C4)alkyl radical, —CHO or CN, as Estrogens.
摘要翻译：本发明描述了通式（I）的非甾体化合物，其中A是其中X 1表示苯基上的一个或多个基团并且彼此独立地表示卤素，OH，（C 1 -C 4）烷基，（ C1-C4）烷基-O，（C3-C6）环烷基-O，（C1-C14）酰基-O，（C1-C4）烯基，（C1-C4）炔基，全氟（C1-C4）烷基， CHO或CN，X2表示苯基上的一个或多个基团，并且彼此独立地表示H，卤素，OH，（C1-C4）烷基，（C1-C4）烷基-O，（C1-C4）烯基，（C 1 -C 4）炔基，全氟 - （C 1 -C 4）烷基，-CHO或CN作为雌激素。

85. 发明申请

US20090029953A1 18-METHYL-19-NOR-17-PREGN-4-ENE-21,17-CARBOLACTONES, AS WELL AS PHARMACEUTICAL PREPARATIONS THAT CONTAIN THE LATTER 审中-公开
标题翻译： 18-METHYL-19-NOR-17-PREGN-4-ENE-21,17-CARBOLACTONES，作为包含LATTER的药物制剂
公开(公告)号：US20090029953A1
公开(公告)日：2009-01-29
申请号：US11813251
申请日：2005-12-30
申请人： Rolf Bohlmann , Dieter Bittler , Hermann Kuenzer , Peter Esperling , Hans Peter Muhn , Karl Heinrich Fritzemeier , Ulrike Fuhrmann , Katja Prelle , Steffen Borden
发明人： Rolf Bohlmann , Dieter Bittler , Hermann Kuenzer , Peter Esperling , Hans Peter Muhn , Karl Heinrich Fritzemeier , Ulrike Fuhrmann , Katja Prelle , Steffen Borden
IPC分类号： A61K31/585 , C07J21/00 , A61P15/00
CPC分类号： C07J21/00 , C07J53/008
摘要： The invention relates to novel 18-methyl-19-nor-17-pregn-4-en-21,17-carbolactones of general formula (I), where Z=O, H2, ═NOR or ═NNHSO2R, where R=H, a straight- or branched-chain 1-4 or 3-4 C alkyl group, R4=H, halogen, methyl or trifluoromethyl, R6 and/or R7 can be α- or β-positioned and independently=branched- or straight-chain 1-4 or 3-4 alkyl, or R6=H and R7=a- or β-positioned, straight- or branched-chain 1-4 or 3-4 C alkyl, or R6 and R7=H, or R6 and R7 together=a- or β-positioned methylene or an additional bond. The novel compounds have gestagenic and antimineralocorticoid activity and are suitable for the production of pharmaceutical preparations, for example, for oral contraception and the treatment of pre-, peri- and post-menopausal pain.
摘要翻译：本发明涉及通式（I）的新颖的18-甲基-19-去甲-17-孕-4-烯-21,17-碳内酯，其中Z = O，H 2，-NOR或-NNHSO 2 R，其中R = H 直链或支链1-4或3-4C烷基，R4 = H，卤素，甲基或三氟甲基，R6和/或R7可以是α-或β-位置，并且独立地为支链或直链，链1-4或3-4烷基，或R6 = H和R7 =α-或β-位置的直链或支链1-4或3-4C烷基，或R6和R7 = H或R6和 R7一起= a-或β-位置的亚甲基或另外的键。新化合物具有孕激素和抗皮质激素活性，并且适用于制备药物制剂，例如用于口服避孕和治疗绝经前，绝经期和绝经后疼痛。

86. 发明授权

US07375098B2 8β-vinyl-11β-(ω-substituted)alkyl-estra-1,3,5(10)-trienes 失效
标题翻译： 8beta-vinyl-11beta-（ω-取代的）烷基 - 雌-1,3,5（10） - 三烯
公开(公告)号：US07375098B2
公开(公告)日：2008-05-20
申请号：US10829390
申请日：2004-04-22
申请人： Nico Braeuer , Olaf Peters , Alexander Hillisch , Rolf Bohlmann , Margit Richter , Hans-Peter Muhn
发明人： Nico Braeuer , Olaf Peters , Alexander Hillisch , Rolf Bohlmann , Margit Richter , Hans-Peter Muhn
IPC分类号： A61K31/56 , A61K31/58 , C07J1/00
CPC分类号： C07J5/00 , C07J7/00 , C07J75/00
摘要： This invention relates to 8β-vinyl-11β-(ω-substituted)alkyl-estra-1,3,5(10)-trienes of general formula I with ERβ-antagonistic activity, process for their production, their intermediate products, pharmaceutical preparations that contain the compounds according to the invention, as well as their use for the production of pharmaceutical agents. The new compounds can be used for contraception in men and women without influencing other estrogen-sensitive organs such as the uterus or the liver.They are also suitable for treating benign or malignant proliferative diseases of the ovary, such as ovarian cancer and granulosa cell tumors.
摘要翻译：本发明涉及具有ERβ-拮抗活性的通式I的8-乙烯基-11β-（ω-取代的）烷基 - 雌-1,3,5（10） - 三烯，其生产方法，其中间产物，药物制剂其含有根据本发明的化合物，以及它们用于生产药剂的用途。新化合物可用于男性和女性避孕，而不影响其他雌激素敏感性器官如子宫或肝脏。它们也适用于治疗卵巢的良性或恶性增殖性疾病，如卵巢癌和颗粒细胞瘤。

87. 发明授权

US07145015B2 Benzocycloheptenes, process for their production, pharmaceutical preparations that contain that latter as well as their use for the production of pharmaceutical agents 失效
标题翻译：苯并环庚三烯，其生产方法，含有后者的药物制剂及其制备药剂的用途
公开(公告)号：US07145015B2
公开(公告)日：2006-12-05
申请号：US11102840
申请日：2005-04-11
申请人： Rolf Bohlmann , Jorg Kroll , Hermann Kuenzer , Christa Hegele-Hartung , Monika Lessl , Rosemarie Lichtner , Yukishige Nishino
发明人： Rolf Bohlmann , Jorg Kroll , Hermann Kuenzer , Christa Hegele-Hartung , Monika Lessl , Rosemarie Lichtner , Yukishige Nishino
IPC分类号： C07D213/28 , C07D307/02 , C07D309/04 , C07D333/16 , A61K31/34 , A61K31/35 , A61K31/38
CPC分类号： C07D307/38 , C07C217/20 , C07C317/18 , C07C317/28 , C07C317/44 , C07C323/12 , C07C323/25 , C07C323/60 , C07C327/28 , C07C2602/12 , C07D213/32 , C07D213/34 , C07D333/18
摘要： Benzocycloheptenes of formula (I), in which R1, R2 and Y have the meanings that indicated herein, exhibit selective estrogenic activity on bones and are suitable for the production of pharmaceutical agents, especially for prophylaxis and therapy of osteoporosis:
摘要翻译：其中R 1，R 2，R 2和Y具有本文所表示的含义的式（I）的苯并环庚烯在骨上显示出选择性雌激素活性，并且适用于生产药剂，特别是预防和治疗骨质疏松症：

88. 发明授权

US07074829B2 Antiestrogens, process for their production and their pharmaceutical use 失效
公开(公告)号：US07074829B2
公开(公告)日：2006-07-11
申请号：US10369577
申请日：2003-02-21
申请人： Ulrich Klar , Rolf Bohlmann , Karsten Parczyk , Karl-Heinrich Fritzemeier , Monika Lessl , Rosemarie Lichtner
发明人： Ulrich Klar , Rolf Bohlmann , Karsten Parczyk , Karl-Heinrich Fritzemeier , Monika Lessl , Rosemarie Lichtner
IPC分类号： A01N37/02
CPC分类号： C07D303/22 , C07C43/23 , C07C217/14 , C07C317/18 , C07C323/12 , C07C2602/24
摘要： This invention relates to new antiestrogens of the general formula in which the substituents have the meanings that are explained in more detail in the description. The new compounds are a) pure antiestrogens or b) antiestrogens with partial estrogenic action (tissue-selective estrogens).Based on these properties, the new compounds are suitable for the production of pharmaceutical agents: in the case of a), for example, for the treatment of breast cancer; in the case of b), for example, for hormone replacement therapy.

89. 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。

90. 发明申请

US20050090477A1 Microbiological process for the production of 7-substituted 11-hydroxy steroids, 7,17-substituted 11-halogen steroids that can be produced therefrom, their process for production and use as well as pharmaceutical prepartions that contain these compounds, as well as 7-substituted estra-1,3,5(10)-trienses that can be produced therefrom 失效
标题翻译：用于生产7-取代的11-羟基类固醇，可由其制备的7,17-取代的11-卤素类固醇，其生产和使用方法以及含有这些化合物的药物制剂的微生物过程，以及7- 取代的雌-1,3,5（10） - 三核苷酸
公开(公告)号：US20050090477A1
公开(公告)日：2005-04-28
申请号：US10625559
申请日：2003-07-24
申请人： Ludwig Zorn , Rolf Bohlmann , Norbert Gallus , Hermann Kuenzer , Hans-Peter Muhn , Reinhard Nubbemeyer
发明人： Ludwig Zorn , Rolf Bohlmann , Norbert Gallus , Hermann Kuenzer , Hans-Peter Muhn , Reinhard Nubbemeyer
IPC分类号： C07J1/00 , C07J3/00 , C07J5/00 , C07J7/00 , C07J9/00 , C07J11/00 , C07J31/00 , C07J41/00 , C12P33/10 , C12P33/16
CPC分类号： C07J1/00 , C07J1/0051 , C07J3/00 , C07J5/00 , C07J7/00 , C07J9/00 , C07J11/00 , C07J31/00 , C07J41/00 , C12P33/10 , C12P33/16
摘要： A novel method of synthesis for the manufacture of upstream products for the production of compounds with general formulas 8, 10, and 12 is described. In this synthesis, compounds with general formula 4,B are produced in a microbiological reaction. The meanings of R7, R10, R11, R13, R17 and R17′ as well as of the grouping U-V-W-X-Y-Z are indicated in the claims.
摘要翻译：描述了用于制备用于生产具有通式8,10和12的化合物的上游产物的合成新方法。在该合成中，通式4的化合物B在微生物反应中产生。 R 7，R 10，R 11，R 13，R 17，R 17，R 17， SUP＆gt;和R＆lt; 17＆gt;以及分组UVWXYZ在权利要求中表示。

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