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1. 发明申请

US20090075987A1 ALKYLACETYLENE SUBSTITUTED ACYLTRYPTOPHANOLS 审中-公开
标题翻译：烷基乙烯取代的乙酰胆碱
公开(公告)号：US20090075987A1
公开(公告)日：2009-03-19
申请号：US12178325
申请日：2008-07-23
申请人： Lars Wortmann , Marcus Koppitz , Hans Peter Muhn , Thomas Frenzel , Florian Peter Liesener , Anna Schrey , Ronald Kuehne
发明人： Lars Wortmann , Marcus Koppitz , Hans Peter Muhn , Thomas Frenzel , Florian Peter Liesener , Anna Schrey , Ronald Kuehne
IPC分类号： A61K31/541 , C07D209/18 , A61K31/404 , A61P15/08 , A61P19/10 , C07D417/02
CPC分类号： C07D209/14 , C07D405/12
摘要： The present invention relates to acyltryptophanols of the general formula I, in which R1, R2, R3, Q and X have the meaning as defined in the description.The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
摘要翻译：本发明涉及通式Ⅰ的酰基色氨酸，其中R1，R2，R3，Q和X具有说明书中定义的含义。根据本发明的化合物是有效的FSH拮抗剂，可用于例如男性或女性的生育控制，或用于预防和/或治疗骨质疏松症。

2. 发明申请

US20080207728A1 BICYCLIC ACYLTRYPTOPHANOLS 审中-公开
标题翻译：双相ACYLTRYPTOPHANOLS
公开(公告)号：US20080207728A1
公开(公告)日：2008-08-28
申请号：US11956824
申请日：2007-12-14
申请人： Lars Wortmann , Bernd Menzenbach , Marcus Koppitz , Dirk Kosemund , Hans-Peter Muhn , Anna Schrey , Ronald Kuehne , Thomas Frenzel , Florian Peter Liesener
发明人： Lars Wortmann , Bernd Menzenbach , Marcus Koppitz , Dirk Kosemund , Hans-Peter Muhn , Anna Schrey , Ronald Kuehne , Thomas Frenzel , Florian Peter Liesener
IPC分类号： A61K31/404 , C07D405/12 , C07D311/02 , C07D307/77 , C07D209/14 , A61P15/18 , A61P15/16
CPC分类号： C07D417/14 , C07D405/12 , C07D405/14 , C07D409/14
摘要： The present invention relates to acyltryptophanols of the general formula I, in which Q, V, X, W, R1, R2, R3, R4, R5, R6, R7 and R8 have the meaning as defined in the description.The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
摘要翻译：本发明涉及通式I的酰基色氨酸，其中Q，V，X，W，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8具有如说明书中所定义的含义。根据本发明的化合物是有效的FSH拮抗剂，可用于例如男性或女性的生育控制，或用于预防和/或治疗骨质疏松症。

3. 发明申请

US20080255117A1 SULFONYLTRYPTOPHANOLS 审中-公开
标题翻译：磺酰亚胺
公开(公告)号：US20080255117A1
公开(公告)日：2008-10-16
申请号：US12040369
申请日：2008-02-29
申请人： Lars WORTMANN , Bernd Menzenbach , Marcus Koppitz , Dirk Kosemund , Hans Peter Muhn , Anna Schrey , Ronald Kuehne , Thomas Frenzel , Florian Peter Liesener
发明人： Lars WORTMANN , Bernd Menzenbach , Marcus Koppitz , Dirk Kosemund , Hans Peter Muhn , Anna Schrey , Ronald Kuehne , Thomas Frenzel , Florian Peter Liesener
IPC分类号： A61K31/4035 , C07D209/14 , A61K31/5377 , C07D413/02 , C07D403/12 , A61K31/454 , A61K31/4155 , C07D405/12 , A61K31/4709 , C07D215/36
CPC分类号： A61K31/4035 , A61K31/4155 , A61K31/454 , A61K31/4709 , A61K31/5377 , C07D209/14 , C07D215/36 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12
摘要： The present invention relates to sulfonyltryptophanols of the general formula I, in which Q, X, W, R1, R2, R3, R4, R5, R6, R7 and R8 have the meaning as defined in the description.The compounds according to the invention are effective FSH receptor antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
摘要翻译：本发明涉及通式I的磺酰基色氨酸，其中Q，X，W，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8具有说明书中定义的含义。根据本发明的化合物是有效的FSH受体拮抗剂，可用于例如男性或女性的生育控制，或用于预防和/或治疗骨质疏松症。

4. 发明申请

US20090069321A1 CYANOMETHYL SUBSTITUTED N-ACYL TRYPTAMINES 审中-公开
标题翻译：氰基取代的N-亚乙基三羟甲基纤维素
公开(公告)号：US20090069321A1
公开(公告)日：2009-03-12
申请号：US12181654
申请日：2008-07-29
申请人： Lars WORTMANN , Marcus Koppitz , Florian Peter Liesener , Thomas Frenzel , Hans-Peter Muhn , Anna Schrey , Ronald Kuehne
发明人： Lars WORTMANN , Marcus Koppitz , Florian Peter Liesener , Thomas Frenzel , Hans-Peter Muhn , Anna Schrey , Ronald Kuehne
IPC分类号： C07D209/18 , A61K31/404 , A61K31/5377 , C07D413/12 , C07D401/12 , A61K31/454 , A61K31/4709 , A61P19/10 , A61P15/16 , A61P15/18
CPC分类号： C07D209/16 , C07D209/14 , C07D401/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to cyanomethyl substituted N-acyl tryptamines of the formula I in whichR1, R2, R3, R4, R5, Q, X and W have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
摘要翻译：本发明涉及式I的氰基甲基取代的N-酰基色胺，其中R1，R2，R3，R4，R5，Q，X和W具有如说明书中所定义的含义。根据本发明的化合物是有效的FSH拮抗剂，可用于例如男性或女性的生育控制，或用于预防和/或治疗骨质疏松症。

5. 发明申请

US20090082372A1 Arylmethylene Substituted N-Acyl-Beta-Amino Alcohols 审中-公开
标题翻译：芳基亚甲基取代的N-酰基-β-氨基醇
公开(公告)号：US20090082372A1
公开(公告)日：2009-03-26
申请号：US12179037
申请日：2008-07-24
申请人： Lars WORTMANN , Marcus Koppitz , Bernd Menzenbach , Dirk Kosemund , Norbert Schmees , Hans-Peter Muhn , Thomas Frenzel , Florian Peter Liesener , Anna Schrey , Ronald Kuehne
发明人： Lars WORTMANN , Marcus Koppitz , Bernd Menzenbach , Dirk Kosemund , Norbert Schmees , Hans-Peter Muhn , Thomas Frenzel , Florian Peter Liesener , Anna Schrey , Ronald Kuehne
IPC分类号： A61K31/437 , C07D471/04 , C07D409/12 , A61K31/416 , A61K31/4709 , A61P19/10 , A61P15/00 , A61K31/47 , C07D231/56 , A61K31/517
CPC分类号： C07D215/20 , C07D215/52 , C07D333/58 , C07D409/12 , C07D471/04
摘要： The present invention relates to arylmethylene substituted N-Acyl-β-amino alcohols of the formula I in which Y is selected from the aryl or heteroaryl groups: and R1, R2, R3, R4, R5, Q, X and W have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
摘要翻译：本发明涉及式I的芳基亚甲基取代的N-酰基-β-氨基醇，其中Y选自芳基或杂芳基：并且R 1，R 2，R 3，R 4，R 5，Q，X和W具有如说明书中所定义。根据本发明的化合物是有效的FSH拮抗剂，可用于例如男性或女性的生育控制，或用于预防和/或治疗骨质疏松症。

6. 发明申请

US20080275083A1 2,3,4,9-TETRAHYDRO-1H-CARBAZOLES 审中-公开
标题翻译： 2,3,4,9-四氢-1H-咪唑
公开(公告)号：US20080275083A1
公开(公告)日：2008-11-06
申请号：US12055524
申请日：2008-03-26
申请人： Lars Wortmann , Marcus Koppitz , Hans Peter Muhn , Thomas Frenzel , Florian Peter Liesener , Anna Schrey , Ronald Kuehne
发明人： Lars Wortmann , Marcus Koppitz , Hans Peter Muhn , Thomas Frenzel , Florian Peter Liesener , Anna Schrey , Ronald Kuehne
IPC分类号： C07D209/82 , C07D401/12 , A61K31/4709 , A61K31/403 , A61P15/08
CPC分类号： C07D401/12 , C07D209/88 , C07D405/12
摘要： The present invention relates to 2,3,4,9-tetrahydro-1H-carbazoles of the general formula I, in which Q, X, W, R1, R2, R3, R4 and R5 have the meaning as defined in the description.The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
摘要翻译：本发明涉及通式I的2,3,4,9-四氢-1H-咔唑，其中Q，X，W，R 1，R 2，R 3，R 4和R 5具有如说明书中所定义的含义。根据本发明的化合物是有效的FSH拮抗剂，可用于例如男性或女性的生育控制，或用于预防和/或治疗骨质疏松症。

7. 发明申请

US20080287493A1 ARYLMETHYLEN SUBSTITUTED N-ACYL-Y-AMINOALCOHOLS 审中-公开
标题翻译：芳基取代的N-亚氨基 - 氨基醇
公开(公告)号：US20080287493A1
公开(公告)日：2008-11-20
申请号：US12108541
申请日：2008-04-24
申请人： Lars Wortmann , Bernd Menzenbach , Marcus Koppitz , Dirk Kosemund , Hans-Peter Muhn , Anna Schrey , Ronald Kuhne , Thomas Frenzel , Florian Peter Liesener
发明人： Lars Wortmann , Bernd Menzenbach , Marcus Koppitz , Dirk Kosemund , Hans-Peter Muhn , Anna Schrey , Ronald Kuhne , Thomas Frenzel , Florian Peter Liesener
IPC分类号： A61K31/4709 , C07D215/38 , C07D209/04 , A61K31/404 , C07C233/64 , A61K31/164 , A61K31/47 , A61P15/08
CPC分类号： C07D401/12 , C07C235/60 , C07D209/16 , C07D215/52 , C07D405/12 , C07D409/12
摘要： The present invention relates to arylmethylen substituted N-acyl-Y-aminoalcohols of the general formula I in which Q, X, W, R1, R2, R3, R4 and R5 have the meaning as defined in the description.The compounds according to the invention are effective FSH modulators and can be used for example for fertility regulation in men or in women.
摘要翻译：本发明涉及通式I的芳基亚甲基取代的N-酰基-Y-氨基醇，其中Q，X，W，R 1，R 2，R 3，R 4和R 5具有如说明书中所定义的含义。根据本发明的化合物是有效的FSH调节剂，并且可以用于例如男性或女性的生殖调节。

8. 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。

9. 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。

10. 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。

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