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1. 发明专利

HRP980289A2 NON-STEROIDAL GESTAGENS 未知
公开(公告)号：HRP980289A2
公开(公告)日：1999-02-28
申请号：HRP980289
申请日：1998-05-29
申请人： HANS-PETER MUHN
发明人： MUHN HANS-PETER
IPC分类号： A61K31/136 , A61K31/16 , A61K31/167 , A61K31/343 , A61K31/365 , A61K31/366 , A61K31/38 , A61K31/381 , A61K31/41 , A61K31/4245 , A61K31/50 , A61K31/535 , A61K31/536 , A61P5/26 , A61P5/34 , A61P15/00 , A61P15/12 , A61P15/18 , C07C225/22 , C07C235/26 , C07C235/32 , C07C235/38 , C07C235/84 , C07C255/57 , C07D237/28 , C07D237/32 , C07D249/18 , C07D265/02 , C07D271/08 , C07D271/12 , C07D285/10 , C07D285/14 , C07D307/88 , C07D307/94 , C07D311/76 , C07D333/72 , C07D409/12
摘要： The invention relates to non-steroidal gestagens of general formula (I), wherein R and R are the same or different and stand for a hydrogen atom, a C1-C5 alkyl group or a halogen atom, or together with the C atom of the chain stand for a ring with 3-7 units, R means a C1-C5 alkyl group or a partially or fully fluorinated C1-C5 alkyl group, A stands for an optionally substituted mono or bi-cyclic aromatic ring, an ester group -COOR , an alkenyl group -CR =CR R , an alkinyl group -CCR or for a partially or fully fluorinated C1-C5 alkyl group, B means a carbonyl group or a CH2 group and Ar is a ring system selected from the group of general partial formulae (2-11). When B represents a CH2 group in general formula (I), Ar additionally means a phenyl radical of partial general formula (12). The novel compounds display a very strong affinity to the gestagen receptor. They can be used on their own or in combination with oestrogen's in contraceptive preparations. They can also be used in the treatment of endometriosis. They can be used with oestrogen's in preparations for the treatment of gynaecological disorders. They can also be used to treat pre-menstrual complaints and in substitution therapy. Their androgen activity enables them to be used for male fertility control, male HRT and to treat andrological syndromes.

2. 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。

3. 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。

4. 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。

5. 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。

6. 发明申请

US20080132476A1 SUBSTITUTED ESTRATRIENES AS SELECTIVELY ACTIVE ESTROGENS 审中-公开
标题翻译：取代的ESTRATRIRIES作为选择性活动的ESTROGENS
公开(公告)号：US20080132476A1
公开(公告)日：2008-06-05
申请号：US12027618
申请日：2008-02-07
申请人： Dirk KOSEMUND , Gerd Mueller , Alexander Hillisch , Karl-Heinrich Fritzemeier , Peter Muhn
发明人： Dirk KOSEMUND , Gerd Mueller , Alexander Hillisch , Karl-Heinrich Fritzemeier , Peter Muhn
IPC分类号： A61K31/56 , A61P19/08 , A61P15/08 , A61P5/24 , A61P15/02 , A61P19/02 , A61P17/06 , A61P9/00 , A61P9/12 , A61P25/28
CPC分类号： C07J41/00 , Y10S514/825 , Y10S514/843
摘要： This invention describes the new 9α-substituted estratrienes of general formula I in which R3, R7, R7′, R13, R16 as well as R17 and R17′ have the meanings that are indicated in the description and R9 means a straight-chain or branched-chain, optionally partially or completely halogenated alkenyl radical with 2 to 6 carbon atoms, an ethinyl or prop-1-inyl radical, as pharmaceutical active ingredients that exhibit in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo preferably a preferential action on the ovary in comparison to the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds.The invention also describes the use of these compounds for treating estrogen-deficiency-induced diseases and conditions.
摘要翻译：本发明描述了通式I的新的9α-取代的雌三烯，其中R 3，R 7，R 7'，R“ 13，R 16以及R 17和R 17'具有在说明书中指出的含义，是指直链或支链，任选部分或完全卤化的具有2-6个碳原子的烯基，乙炔基或丙-1-炔基，作为在体外表现出的药物活性成分对来自大鼠前列腺的雌激素受体制剂的亲和力高于来自大鼠子宫内和体内的雌激素受体制剂的亲和力，优选与子宫相比优于子宫，其生产，其治疗用途和含有新化合物的药物分配形式的优选作用。本发明还描述了这些化合物用于治疗雌激素缺乏诱导的疾病和病症的用途。

7. 发明授权

US07309691B2 Combined pharmaceutical preparation containing LHRH-analogous substances and anti estrogens for treating gynaecological disorders 失效
标题翻译：含有LHRH类似物质和抗雌激素用于治疗妇科疾病的组合药物制剂
公开(公告)号：US07309691B2
公开(公告)日：2007-12-18
申请号：US09117357
申请日：1997-01-29
申请人： Klaus Stöckemann , Peter Muhn
发明人： Klaus Stöckemann , Peter Muhn
IPC分类号： A61K38/00 , A61K31/445
CPC分类号： A61K38/09 , A61K31/445 , A61K31/40 , A61K31/135 , A61K2300/00
摘要： The invention relates to a pharmaceutical combined preparation of LHRH analogues and anti-oestrogens having tissue-selective oestrogen activity and also to its use for the treatment of gynaecological disorders, especially for the treatment of endometrioses and myomas.
摘要翻译：本发明涉及具有组织选择性雌激素活性的LHRH类似物和抗雌激素的药物组合制剂，以及其用于治疗妇科疾病，特别是用于治疗子宫内膜异位症和肌瘤的用途。

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。

10. 发明授权

US07414043B2 9-α-substituted estratrienes as selectively active estrogens 失效
标题翻译： 9-α-取代的雌三醇作为选择性活性雌激素
公开(公告)号：US07414043B2
公开(公告)日：2008-08-19
申请号：US10458735
申请日：2003-06-11
申请人： Dirk Kosemund , Gerd Mueller , Alexander Hillisch , Karl-Heinrich Fritzemeier , Peter Muhn
发明人： Dirk Kosemund , Gerd Mueller , Alexander Hillisch , Karl-Heinrich Fritzemeier , Peter Muhn
IPC分类号： A61K31/56 , C07J1/00
CPC分类号： C07J41/00 , Y10S514/825 , Y10S514/843
摘要： This invention describes the new 9α-substituted estratrienes of general formula I in which R3, R7, R7′, R13, R16 as well as R17 and R17′ have the meanings that are indicated in the description and R9 means a straight-chain or branched-chain, optionally partially or completely halogenated alkenyl radical with 2 to 6 carbon atoms, an ethinyl or prop-1-inyl radical, as pharmaceutical active ingredients that exhibit in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo preferably a preferential action on the ovary in comparison to the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention also describes the use of these compounds for treating estrogen-deficiency-induced diseases and conditions.
摘要翻译：本发明描述了通式I的新的9α-取代的雌三烯，其中R 3，R 7，R 7'，R“ 13，R 16以及R 17和R 17'具有在说明书中指出的含义，是指具有2-6个碳原子的直链或支链，任选部分或完全卤化的烯基，乙炔基或丙-1-茚基，作为在体外表现出的药物活性成分对来自大鼠前列腺的雌激素受体制剂的亲和力高于来自大鼠子宫内和体内的雌激素受体制剂的亲和力，优选与子宫相比优于子宫，其生产，其治疗用途和含有新化合物的药物分配形式的优选作用。本发明还描述了这些化合物用于治疗雌激素缺乏诱导的疾病和病症的用途。

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