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1. 发明授权

US08445469B2 18-methyl-19-nor-17-pregn-4-ene-21,17-carbolactones, as well as pharmaceutical preparations that contain the latter 失效
标题翻译： 18-甲基-19-去甲-17-孕甾-4-烯-21,17-碳内酯，以及含有后者的药物制剂
公开(公告)号：US08445469B2
公开(公告)日：2013-05-21
申请号：US11321449
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： A61K31/58 , C07J21/00
CPC分类号： C07J19/00
摘要： A 18-Methyl-19-nor-17-pregn-4-ene-21,17-carbolactone of general formula I in which Z, R4, R6, R7 are as defined below with the proviso that the compound is not 18-Methyl-15β,16β-methylene-3-oxo-19-nor-17-pregn-4-ene-21,17-carbolactone.
摘要翻译：其中Z，R4，R6，R7如下所定义的通式I的18-甲基-19-降-17-孕-4-烯-21,17-碳内酯，条件是该化合物不是18-甲基 -15β，16β-亚甲基-3-氧代-19-去甲-17-孕-4-烯-21,17-碳内酯。

2. 发明申请

US20060252737A1 18-Methyl-19-nor-17-pregn-4-ene-21,17-carbolactones, as well as pharmaceutical preparations that contain the latter 失效
标题翻译： 18-甲基-19-去甲-17-孕-4-烯-21,17-碳内酯，以及含有后者的药物制剂
公开(公告)号：US20060252737A1
公开(公告)日：2006-11-09
申请号：US11321449
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： A61K31/58 , C07J19/00
CPC分类号： C07J19/00
摘要： This invention describes the new 18-methyl-19-nor-17-pregn-4-ene-21,17-carbolactones of general formula I in which Z means an oxygen atom, two hydrogen atoms, a grouping ═NOR or ═NNHSO2R, whereby R is a hydrogen atom or a straight-chain or branched-chain alkyl group with 1 to 4 or 3 to 4 carbon atoms, R4 is a hydrogen atom, a halogen atom, a methyl group, or a trifluoromethyl group, R6 and/or R7 can be in α- or β-position, and, independently of one another, mean a straight-chain or branched-chain alkyl group with 1 to 4 or 3 to 4 carbon atoms, or R6 means a hydrogen atom, and R7 means an α- or β-position, straight-chain or branched-chain alkyl group with 1 to 4 or 3 to 4 carbon atoms, or R6 and R7 each mean a hydrogen atom, or R6 and R7 together mean an α- or β-position methylene group or an additional bond. The new compounds have gestagenic and anti-mineralocorticoid action and are suitable for the production of pharmaceutical preparations, for example for oral contraception and the treatment of pre-, peri- and post-menopausal symptoms.
摘要翻译：本发明描述了通式I的新的18-甲基-19-去甲-17-孕甾-4-烯-21,17-碳内酯，其中Z表示氧原子，两个氢原子，-NOR或-NNHSO- R 2是氢原子或具有1至4或3至4个碳原子的直链或支链烷基，R 4是氢原子，卤素原子，甲基或三氟甲基，R 6和/或R 7可以是α-或β-位，并且独立地为一个另一个是指具有1至4或3至4个碳原子的直链或支链烷基，或R 6表示氢原子，R 7表示具有1至4或3至4个碳原子的α-或β-位的直链或支链烷基，或R 6和R 7各自表示氢原子或R 6和R 7一起是指α-或β-位亚甲基或另外的键。新化合物具有孕激素和抗盐皮质激素的作用，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，绝经期和绝经后症状。

3. 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。

4. 发明申请

US20110015162A1 15,16-Methylene-17-hydroxy-19-nor-21-carboxylic acid-steroid Y-lactone derivative, use thereof and medicinal products containing the derivative 审中-公开
标题翻译： 15,16-亚甲基-17-羟基-19-去甲-21-羧酸类固醇Y-内酯衍生物及其衍生物的用途
公开(公告)号：US20110015162A1
公开(公告)日：2011-01-20
申请号：US12811002
申请日：2008-12-23
申请人： Ulrich Klar , Joachim Kuhnke , Rolf Bohlmann , Jan Huebner , Sven Ring , Thomas Frenzel , Frederik Menges , Steffen Borden , Hans Peter Muhn , Katja Prelle
发明人： Ulrich Klar , Joachim Kuhnke , Rolf Bohlmann , Jan Huebner , Sven Ring , Thomas Frenzel , Frederik Menges , Steffen Borden , Hans Peter Muhn , Katja Prelle
IPC分类号： A61K31/58 , C07J53/00 , A61K31/56
CPC分类号： C07J53/008
摘要： The invention relates to 15,16-methylene-17-hydroxy-19-nor-21-carboxylic acid-steroid γ-lactone derivatives with the general chemical formula I, and R4, R6a, R6b, R7 and Z have the meanings stated in claim 1, and their solvates, hydrates, stereoisomers and salts. 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. 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15,16-亚甲基-17-羟基-19-去甲-21-羧酸 - 类固醇γ-内酯衍生物，且R4，R6a，R6b，R7和Z具有以下含义：权利要求1及其溶剂合物，水合物，立体异构体和盐。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前，绝经前和绝经后的投诉和含有所述衍生物的药用产品的用途。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。

5. 发明授权

US08623850B2 15, 16-methylene-17-(1′-propenyl)-17,3′-oxidoestra-4-en-3-one derivative, use thereof, and medicament containing said derivative 失效
标题翻译： 15，16-亚甲基-17-（1'-丙烯基）-17,3'-氧代雌-4-烯-3-酮衍生物及其用途，以及含有所述衍生物
公开(公告)号：US08623850B2
公开(公告)日：2014-01-07
申请号：US12810857
申请日：2008-12-23
申请人： Ulrich Klar , Joachim Kuhnke , Rolf Bohlmann , Jan Hübner , Sven Ring , Thomas Frenzel , Frederik Menges , Steffen Borden , Hans-Peter Muhn , Katja Prelle
发明人： Ulrich Klar , Joachim Kuhnke , Rolf Bohlmann , Jan Hübner , Sven Ring , Thomas Frenzel , Frederik Menges , Steffen Borden , Hans-Peter Muhn , Katja Prelle
IPC分类号： A61K31/56 , A61K31/58
CPC分类号： C07J53/008
摘要： The invention relates to 15,16-methylene-17-(1′-propenyl)-17-3′-oxidoestra-4-en-3-one derivatives with the general chemical formula I, where the Z, R4, R6a, R6b, R7 and R18 have the meanings stated in claim 1, and solvates, hydrates and salts thereof, including all crystal modifications and all stereoisomers of these compounds. The invention also relates to the use of these derivatives for the production of a drug for oral contraception and for the treatment of pre-, peri- and postmenopausal problems and drugs which contain such derivatives, in particular use in the aforesaid indications. The derivatives according to the invention have a progestational and in preferable cases also an antimineralcorticoid and neutral to slight androgenic activity.
摘要翻译：本发明涉及具有一般化学式I的15,16-亚甲基-17-（1'-丙烯基）-17-3'-氧代雌-4-烯-3-酮衍生物，其中Z，R4，R6a，R6b R 7和R 18具有权利要求1所述的含义，并溶剂合物，其水合物和盐，包括这些化合物的所有晶体改性和所有立体异构体。本发明还涉及这些衍生物用于生产口服避孕药物和用于治疗绝经前，绝经期和绝经后问题的药物以及含有此类衍生物的药物，特别是在上述适应症中使用。根据本发明的衍生物具有促孕作用，并且在优选情况下还具有抗铁皮质激素和中性至轻度雄激素活性。

6. 发明授权

US08207150B2 17β-cyano-19-nor-androst-4-ene derivative, its use and medicaments comprising the derivative 失效
标题翻译： 17-氰基-19-去甲 - 雄甾-4-烯衍生物，其用途和药物包含衍生物
公开(公告)号：US08207150B2
公开(公告)日：2012-06-26
申请号：US12137111
申请日：2008-06-11
申请人： Joachim Kuhnke , Jan Huebner , Rolf Bohlmann , Thomas Frenzel , Ulrich Klar , Frederik Menges , Sven Ring , Steffen Borden , Hans-Peter Muhn , Katja Prelle
发明人： Joachim Kuhnke , Jan Huebner , Rolf Bohlmann , Thomas Frenzel , Ulrich Klar , Frederik Menges , Sven Ring , Steffen Borden , Hans-Peter Muhn , Katja Prelle
IPC分类号： A61K31/56 , C07J3/00
CPC分类号： C07J53/008 , C07J41/0094 , C07J53/007
摘要： The 17β-cyano-19-nor-androst-4-ene derivatives of the present invention possess gestagenic activity. They have the general chemical formula 1, in which Z is selected from the group comprising O, two hydrogen atoms, NOR and NNHSO2R, in which R is hydrogen or C1-C4-alkyl, R4 is hydrogen or halogen, furthermore either: R6a, R6b together form methylene or 1,2-ethanediyl or R6a is hydrogen and R6b is selected from the group comprising hydrogen, methyl and hydroxymethylene, and R7 is selected from the group comprising hydrogen, C1-C4-alkyl, C2-C3-alkenyl and cyclopropyl, or: R6a is hydrogen and R6b and R7 together form methylene or are omitted with formation of a double bond between C6 and C7, R9, R10 are hydrogen or are omitted with formation of a double bond between C9 and C10, R15, R16 are hydrogen or together form methylene, R17 is selected from the group comprising hydrogen, C1-C4-alkyl and allyl, where at least one of the substituents R4, R6a, R6b, R7, R15, R16 and R17 is unequal to hydrogen or R6b and R7 are omitted with formation of a double bond between C6 and C7, and moreover comprise their solvates, hydrates, stereoisomers, diastereomers, enantiomers and salts.
摘要翻译：本发明的17α-氰基-19-去雄甾-4-烯衍生物具有孕激活作用。它们具有一般化学式1，其中Z选自O，两个氢原子，NOR和NNHSO 2 R，其中R是氢或C 1 -C 4 - 烷基，R 4是氢或卤素，此外：R 6a， R6b一起形成亚甲基或1,2-乙二基或R6a为氢，R6b选自氢，甲基和羟基亚甲基，R7选自氢，C1-C4-烷基，C2-C3-烯基和环丙基，或者：R6a是氢，R6b和R7一起形成亚甲基，或者在C6和C7之间形成双键被省略，R9，R10是氢或在C9与C10之间形成R15，R16 是氢或一起形成亚甲基，R 17选自氢，C 1 -C 4 - 烷基和烯丙基，其中至少一个取代基R4，R6a，R6b，R7，R15，R16和R17不等于氢或R6b 并且在C6和C7之间形成双键而省略R7，此外，上升它们的溶剂合物，水合物，立体异构体，非对映异构体，对映体和盐。

7. 发明申请

US20100292184A1 17BETA-CYANO-19-ANDROST-4-ENE DERIVATIVE, ITS USE AND MEDICAMENTS COMPRISING THE DERIVATIVE 审中-公开
标题翻译： 17BETA-CYANO-19-ANDROST-4-ENE DERIVATIVE，其使用和药物包含衍生物
公开(公告)号：US20100292184A1
公开(公告)日：2010-11-18
申请号：US12664099
申请日：2008-06-12
申请人： Joachim Kuhnke , Jan Huebner , Rolf Bohlmann , Thomas Frenzel , Ulrich Klar , Frederik Menges , Sven Ring , Steffen Borden , Hans Peter Muhn , Katja Prelle
发明人： Joachim Kuhnke , Jan Huebner , Rolf Bohlmann , Thomas Frenzel , Ulrich Klar , Frederik Menges , Sven Ring , Steffen Borden , Hans Peter Muhn , Katja Prelle
IPC分类号： A61K31/56 , C07J53/00 , C07J41/00 , A61K31/695 , A61K31/565 , A61P15/18 , A61P5/24 , A61P5/34 , A61P5/42
CPC分类号： C07J41/0094 , C07J53/007 , C07J53/008
摘要： The 17β-cyano-19-androst-4-ene derivatives of the present invention possess gestagenic activity. They have the general chemical formula 1, in which Z is selected from the group comprising O, two hydrogen atoms, NOR and NNHSO2R, in which R is hydrogen or C1-C4-alkyl, R1, R2 are each independently hydrogen or methyl, or R1 and R2 together form methylene or are omitted with formation of a double bond between C1 and C2, R4 is hydrogen or halogen, furthermore either: R6a, R6b together form methylene or 1,2-ethanediyl or R6a is hydrogen and R6b is selected from the group comprising hydrogen, methyl and hydroxymethylene, and R7 is selected from the group comprising hydrogen, C1-C4-alkyl, C2-C3-alkenyl and cyclopropyl, or: R6a hydrogen and R6b and R7 together form methylene or are omitted with formation of a double bond between C6 and C7 or: R6a is methyl and R6b and R7 are omitted with formation of a double bond between C6 and C7, R15, R16 are hydrogen or together form methylene, R17 is selected from the group comprising hydrogen, C1-C4-alkyl and allyl, and moreover comprise their solvates, hydrates, stereoisomers, diastereomers, enantiomers and salts, with the proviso that particular compounds are excluded.
摘要翻译：本发明的17α-氰基-19-雄甾-4-烯衍生物具有孕激活作用。它们具有一般化学式1，其中Z选自O，两个氢原子，NOR和NNHSO 2 R，其中R是氢或C 1 -C 4烷基，R 1，R 2各自独立地是氢或甲基，或 R1和R2一起形成亚甲基或被省略，在C1和C2之间形成双键，R4是氢或卤素，此外：R6a，R6b一起形成亚甲基或1,2-乙二基或R6a是氢，R6b选自包括氢，甲基和羟基亚甲基的基团，并且R 7选自氢，C 1 -C 4 - 烷基，C 2 -C 3 - 烯基和环丙基，或者：R 6a氢和R 6b和R 7一起形成亚甲基或被形成 C6和C7之间的双键或：R6a是甲基，R6和C7之间形成双键，R6b和R7被省略，R15，R16是氢或一起形成亚甲基，R17选自氢，C1- C4-烷基和烯丙基，并且还包含它们的溶剂化物 es，水合物，立体异构体，非对映体，对映异构体和盐，条件是排除特定的化合物。

8. 发明申请

US20100311702A1 19-NOR-STEROID DERIVATIVES WITH A 15ALPHA, 16ALPHA-METHYLENE GROUP AND A SATURATED 17, 17-SPIRO-LACTONE RING, USE THEREOF, AND MEDICAMENTS CONTAINING SAID DERIVATIVES 审中-公开
标题翻译：具有15ALPHA，16ALPHA-甲基组的饱和甾体衍生物和饱和的17,17-螺旋体环，其使用和含有所述衍生物的药物
公开(公告)号：US20100311702A1
公开(公告)日：2010-12-09
申请号：US12810860
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： A61K31/585 , C07J21/00 , A61P15/18 , A61P5/24 , A61P5/42 , A61P5/26
CPC分类号： C07J21/003 , C07J53/008
摘要： The 15α,16α-methylene-17-hydroxy-19-nor-17-pregna-4-en-3-one-21-carboxylic acid γ-lactone derivatives of the present invention possess progestational efficacy. They have the general chemical formula I, in which Z is selected from the group comprising an oxygen atom, two hydrogen atoms, NOR and NNHSO2R, where R is hydrogen, C1-C10-alkyl, aryl or C7-C20-aralkyl, R4 is hydrogen or halogen, and moreover either: R6a, R6b together form methylene or 1,2-ethanediyl or R6a is hydrogen and R6b is selected from the group comprising hydrogen, C1-C10-alkyl, C2-C10-alkenyl or C2-C10-alkynyl, and R7 is selected from the group comprising hydrogen, C1-C10-alkyl, C3-C6-cycloalkyl, C2-C10-alkenyl or C2-C10-alkynyl, or: R6a is hydrogen and R6b and R7, together, denote a bond, an oxygen or form methylene, R18 represents hydrogen or C1-C3-alkyl and in addition include their solvates, hydrates, stereoisomers and salts.
摘要翻译：本发明的15α，16α-亚甲基-17-羟基-19-去甲-17-前 - 孕-4-烯-3-酮-21-羧酸γ-内酯衍生物具有促进功效。它们具有一般化学式I，其中Z选自氧原子，两个氢原子，NOR和NNHSO 2 R，其中R是氢，C 1 -C 10 - 烷基，芳基或C 7 -C 20 - 芳烷基，R 4是氢或卤素，此外：R6a，R6b一起形成亚甲基或1,2-乙二基或R6a为氢，R6b选自氢，C1-C10-烷基，C2-C10-烯基或C2-C10-烯基，炔基，R 7选自氢，C 1 -C 10 - 烷基，C 3 -C 6 - 环烷基，C 2 -C 10 - 烯基或C 2 -C 10 - 炔基，或者：R 6a是氢，R 6b和R 7一起表示键，氧或亚甲基，R 18表示氢或C 1 -C 3 - 烷基，并且还包括它们的溶剂合物，水合物，立体异构体和盐。

9. 发明申请

US20080153787A1 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：US20080153787A1
公开(公告)日：2008-06-26
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 , C07J71/00
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 a or a 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-壬二酸-4-烯17,17-螺醚，其中Z是氧原子，两个氢原子，-NOR或-NNHSO - 2 R，其中R是氢原子或具有1至4或3至4个碳原子的直链或支链烷基，R 4是氢原子，卤素原子或三氟甲基，R 6和/或R 7可以具有或其结构，并且R 6和R 6可以是 7个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至4个碳原子的直链或支链烯基 4个碳原子或3〜5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。

10. 发明申请

US20110021472A1 17-HYDROXY-19-NOR-21-CARBOXYLIC ACID-STEROID Y-LACTONE DERIVATIVE, USE THEREOF, AND MEDICAMENT CONTAINING THE DERIVATIVE 有权
标题翻译： 17-羟基-19-异-21-羧酸 - 甾体Y-LACTONE衍生物，其用途和含有衍生物的药物
公开(公告)号：US20110021472A1
公开(公告)日：2011-01-27
申请号：US12810991
申请日：2008-12-23
申请人： Ulrich Klar , Jooachim Kuhnke , Rolf Bohlmann , Jan Huebner , Sven Ring , Thomas Frenzel , Frederik Menges , Steffen Borden , Hans Peter Muhn , Katja Prelle
发明人： Ulrich Klar , Jooachim Kuhnke , Rolf Bohlmann , Jan Huebner , Sven Ring , Thomas Frenzel , Frederik Menges , Steffen Borden , Hans Peter Muhn , Katja Prelle
IPC分类号： A61K31/585 , C07J21/00 , A61P15/18
CPC分类号： C07J53/00 , C07J19/00
摘要： The invention relates to 17-hydroxy-19-nor-21-carboxylic acid-steroid γ-lactone derivatives with the chemical formula I, where R4, R6a, R6b, R7, R15, R16a, R16b, R18 and Z have the meanings stated in claim 1, and their solvates, hydrates, stereoisomers and salts. 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. 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：本发明涉及具有化学式I的17-羟基-19-去甲-21-羧酸 - 类固醇γ-内酯衍生物，其中R4，R6a，R6b，R7，R15，R16a，R16b，R18和Z具有以下含义：权利要求1及其溶剂合物，水合物，立体异构体和盐。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前，绝经前和绝经后的投诉和含有所述衍生物的药用产品的用途。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。

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