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1. 发明申请

US20060270845A1 16-Hydroxyestratrienes as selectively active estrogens 审中-公开
标题翻译： 16羟基三烯作为选择性活性雌激素
公开(公告)号：US20060270845A1
公开(公告)日：2006-11-30
申请号：US11498109
申请日：2006-08-03
申请人： Hermann Kuenzer , Rudolf Knauthe , Monika Lessl , Karl-Heinrich Fritzemeier , Christa Hegele-Hartung , Ulf Boemer , Gerd Mueller , Dirk Kosemund
发明人： Hermann Kuenzer , Rudolf Knauthe , Monika Lessl , Karl-Heinrich Fritzemeier , Christa Hegele-Hartung , Ulf Boemer , Gerd Mueller , Dirk Kosemund
IPC分类号： C07J41/00 , C07J1/00
CPC分类号： A61K31/565 , C07J1/00 , C07J9/00 , C07J41/00
摘要： The invention describes new compounds as pharmaceutical active ingredients, which have in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo a preferential action on bone rather than the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The new compounds are 16α- and 16β-hydroxy-estra-1,3,5(10)-estratrienes, which carry additional substituents on the steroid skeleton and can have one or more additional double bonds in the B-, C- and/or D-rings.
摘要翻译：本发明描述了作为药物活性成分的新化合物，其具有体外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的雌激素受体制剂，并且在体内对骨骼而不是子宫的优先作用，其产生，其治疗使用和含有新化合物的药物分配形式。新化合物是16α-和16beta-羟基 - 雌-1,3,5（10） - 三亚甲基，其在类固醇骨架上携带另外的取代基，并且可以在B-，C-和/ 或D形环。

2. 发明授权

US07109360B1 16-hydroxyestratrienes as selectively active estrogens 失效
标题翻译： 16-羟基三烯作为选择性活性雌激素
公开(公告)号：US07109360B1
公开(公告)日：2006-09-19
申请号：US09497891
申请日：2000-02-04
申请人： Hermann Kuenzer , Rudolf Knauthe , Monika Lessl , Karl-Heinrich Fritzemeier , Christa Hegele-Hartung , Ulf Boemer , Gerd Mueller , Dirk Kosemund
发明人： Hermann Kuenzer , Rudolf Knauthe , Monika Lessl , Karl-Heinrich Fritzemeier , Christa Hegele-Hartung , Ulf Boemer , Gerd Mueller , Dirk Kosemund
IPC分类号： C07J9/00 , C07J41/00
CPC分类号： A61K31/565 , C07J1/00 , C07J9/00 , C07J41/00
摘要： The invention describes new compounds as pharmaceutical active ingredients, which have in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo a preferential action on bone rather than the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds.The new compounds are 16α- and 16β-hydroxy-estra-1,3,5(10)-estratrienes, which carry additional substituents on the steroid skeleton and can have one or more additional double bonds in the B-, C- and/or D-rings.
摘要翻译：本发明描述了作为药物活性成分的新化合物，其具有体外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的雌激素受体制剂，并且在体内对骨骼而不是子宫的优先作用，其产生，其治疗使用和含有新化合物的药物分配形式。新化合物是16α-和16beta-羟基 - 雌-1,3,5（10） - 三亚甲基，其在类固醇骨架上携带另外的取代基，并且可以在B-，C-和/ 或D形环。

3. 发明申请

US20050020695A1 Use of ERbeta-selective ligands for regulating fertility and compounds useful therefor 审中-公开
标题翻译：使用ERbeta选择性配体调节生育力和有用的化合物
公开(公告)号：US20050020695A1
公开(公告)日：2005-01-27
申请号：US10909540
申请日：2004-08-03
申请人： Christa Hegele-Hartung , Karl-Heinrich Fritzemeier , Hiroshi Yamanouchi , Olaf Peters , Dirk Kosemund , Gerd Mueller , Ingo Tornus , Gerd Schubert , Sven Ring
发明人： Christa Hegele-Hartung , Karl-Heinrich Fritzemeier , Hiroshi Yamanouchi , Olaf Peters , Dirk Kosemund , Gerd Mueller , Ingo Tornus , Gerd Schubert , Sven Ring
IPC分类号： A61K31/00 , A61K31/05 , A61K31/122 , A61K45/06 , A61K31/075 , C07C39/12
CPC分类号： A61K45/06 , A61K31/00 , A61K31/05 , A61K31/122
摘要： The present invention discloses the use of ERβ-selective ligands for production of medicaments for regulating fertility without additional use of a progestin. ERβ-agonists are used for treatment of infertility and ERβ-antagonists for contraception.
摘要翻译：本发明公开了ERbeta选择性配体用于生产用于调节生育力而不需要额外使用孕激素的药物。 ERbeta激动剂用于治疗不育症和ERbeta拮抗剂用于避孕。

4. 发明授权

US06794409B2 Use of ER&bgr;-selective ligands for regulating fertility and compounds useful therefor 失效
标题翻译：使用ERbeta选择性配体调节生育力和有用的化合物
公开(公告)号：US06794409B2
公开(公告)日：2004-09-21
申请号：US10083685
申请日：2002-02-27
申请人： Christa Hegele-Hartung , Karl-Heinrich Fritzemeier , Hiroshi Yamanouchi , Olaf Peters , Dirk Kosemund , Gerd Mueller , Ingo Tornus , Gerd Schubert , Sven Ring
发明人： Christa Hegele-Hartung , Karl-Heinrich Fritzemeier , Hiroshi Yamanouchi , Olaf Peters , Dirk Kosemund , Gerd Mueller , Ingo Tornus , Gerd Schubert , Sven Ring
IPC分类号： A61K31215
CPC分类号： A61K45/06 , A61K31/00 , A61K31/05 , A61K31/122
摘要： The present invention discloses the use of ER&bgr;-selective ligands for production of medicaments for regulating fertility without additional use of a progestin. ER&bgr;-agonists are used for treatment of infertility and ER&bgr;-antagonists for contraception.
摘要翻译：本发明公开了ERbeta选择性配体用于生产用于调节生育力的药物的用途，而不需要额外使用孕激素.Ebeta激动剂用于治疗不育症和用于避孕的ERbeta拮抗剂。

5. 发明授权

US06844336B2 4-fluoroalkyl-2h-benzopyrans with anti-estogenic activity 失效
标题翻译：具有抗雌激素活性的4-氟烷基-2H-苯并吡喃酮
公开(公告)号：US06844336B2
公开(公告)日：2005-01-18
申请号：US10221553
申请日：2001-03-15
申请人： Hermann Kuenzer , Rolf Jautelat , Ludwig Zorn , Christa Hegele-Hartung , Uwe Kollenkirchen , Karl-Heinrich Fritzemeier
发明人： Hermann Kuenzer , Rolf Jautelat , Ludwig Zorn , Christa Hegele-Hartung , Uwe Kollenkirchen , Karl-Heinrich Fritzemeier
IPC分类号： A61K31/453 , A61P3/06 , A61P5/00 , A61P5/32 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/08 , A61P15/00 , A61P15/12 , A61P15/16 , A61P15/18 , A61P17/14 , A61P19/02 , A61P19/10 , A61P25/28 , A61P29/00 , A61P35/00 , C07D311/60 , A61K31/35 , A61K31/445 , C07D311/64 , C07D405/12 , C07D413/12
CPC分类号： C07D311/60
摘要： This invention describes the new 4-fluoroalkyl-2H-benzopyrans of general formula I, in which Z is a straight-chain or branched-chain alkyl group with up to 5 carbon atoms that is fluorinated in at least one place, preferably a trifluoromethyl group, and R1, R2, X, Y and n have the meanings that are indicated in the description. The new compounds have at their disposal strong antiestrogenic action. In addition, they can have at their disposal estrogenic action that occurs in a tissue-selective manner. They can be used for the production of pharmaceutical agents, especially for the treatment of estrogen-dependent diseases and tumors and pharmaceutical agents for hormone replacement therapy (HRT) as well as for the prevention and treatment of osteoporosis.
摘要翻译：本发明描述了通式I的新的4-氟烷基-2H-苯并吡喃，其中Z是至少在一个位置，优选三氟甲基氟化的具有至多5个碳原子的直链或支链烷基， R 1，R 2，X，Y和n具有说明书中所示的含义。新化合物具有强的抗雌激素作用。此外，它们可以具有以组织选择性方式发生的雌激素作用。它们可用于生产药剂，特别是用于治疗雌激素依赖性疾病和肿瘤以及用于激素替代疗法（HRT）的药剂以及用于预防和治疗骨质疏松症。

6. 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。

7. 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。

8. 发明授权

US06958327B1 18 Norsteroids as selectively active estrogens 失效
标题翻译： 18只小鼠作为选择性活性雌激素
公开(公告)号：US06958327B1
公开(公告)日：2005-10-25
申请号：US10111933
申请日：2000-11-02
申请人： Alexander Hillisch , Werner Boidol , Wolfgang Schwede , Peter Esperling , Gerhard Sauer , Christa Hegele-Hartung , Uwe Kollenkirchen , Karl-Heinrich Fritzemeier
发明人： Alexander Hillisch , Werner Boidol , Wolfgang Schwede , Peter Esperling , Gerhard Sauer , Christa Hegele-Hartung , Uwe Kollenkirchen , Karl-Heinrich Fritzemeier
IPC分类号： A61K31/56 , C07J1/00
CPC分类号： C07J1/00
摘要： The invention relates to novel 18-norsteroids (gonatrienes) of general formula (I), wherein R1, R2, R3, R6, R7, R8, R9, R11, R11′, R14, R15, R15′, R16, R17 and R17′ have the meaning cited in the description, and to the use of said compounds as pharmaceutical active ingredients. Said compounds exhibit a high affinity in vitro for estrogen receptor preparations of rat prostate and in an estrogen receptor preparation of rat uterus. Said compounds exhibit in vivo preferential activity on bones as compared to the uterus and/or significant activity with regard to stimulating the expression of 5HT2a-receptors and transporter molecules. The invention also relates to the production of said compounds, therapeutic use and galenic form of said compounds contained in the novel compounds of invention. The invention also relates to utilization of steroids based on the gonatriene molecular skeleton in order to treat estrogen deficiency-induced diseases and disorders, in addition to the use of said gonatriene structural component in the total structure of compounds which dissociate to produce enhanced estrogen activity in bone as compared to the uterus
摘要翻译：本发明涉及通式（I）的新颖的18-降胆固醇（高三烯），其中R 1，R 2，R 3，R 3， R 6，R 7，R 8，R 9，R 11，R 11，R 11， R 11，R 14，R 15，R 15'，R 16， R 17和R 17'具有说明书中引用的含义，以及所述化合物作为药物活性成分的用途。所述化合物在体外对大鼠前列腺的雌激素受体制剂和大鼠子宫的雌激素受体制剂中表现出高亲和力。与刺激5HT2a受体和转运蛋白分子表达相关的子宫和/或显着活性相比，所述化合物在骨骼上表现出体内优先活性。本发明还涉及所述化合物的生产，本发明新化合物中所含化合物的治疗用途和盖仑型形式。本发明还涉及除了在分解以产生增强的雌激素活性的化合物的总体结构中使用所述三氢结构组分之外，还可以利用基于分子量分子骨架的类固醇来治疗雌激素缺乏诱导的疾病和病症骨与子宫相比

9. 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。

10. 发明申请

US20050282791A1 18-nor steroids as selectively active estrogens 审中-公开
标题翻译： 18-或类固醇作为选择性活性雌激素
公开(公告)号：US20050282791A1
公开(公告)日：2005-12-22
申请号：US11184784
申请日：2005-07-20
申请人： Alexander Hillisch , Werner Boidol , Wolfgang Schwede , Peter Esperling , Gerhard Sauer , Christa Hegele-Hartung , Uwe Kollenkirchen , Karl-Heinrich Fritzemeier
发明人： Alexander Hillisch , Werner Boidol , Wolfgang Schwede , Peter Esperling , Gerhard Sauer , Christa Hegele-Hartung , Uwe Kollenkirchen , Karl-Heinrich Fritzemeier
IPC分类号： A61K31/56 , A61K31/58
CPC分类号： C07J1/0051
摘要： This invention describes the new 18-nor steroids (gonatrienes) of general formula (I), in which R1, R2, R3, R6, R7, R8, R9, R11, R11′, R14, R15, R15, R16, R17 and R17′ have the meanings that are indicated in the description, as pharmaceutical active ingredients that have in vitro a higher affinity to estrogen receptor preparations of rat prostates than to estrogen receptor preparations of rat uteri and in vivo a preferential action on bone in comparison to the uterus, and/or pronounced action relative to the stimulation of the expression of 5HT2a-receptors and transporters, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention further describes the use of steroids, on which the gonatriene skeleton is based, for treatment of estrogen-deficiency-induced diseases and conditions as well as the use of the gonatriene structural part in the total structures of compounds that have a dissociation in favor of their estrogenic action on bone in comparison to the uterus.
摘要翻译：本发明描述了通式（I）的新的18-或类固醇（高碳二烯），其中R 1，R 2，R 3，R 3， R 6，R 7，R 8，R 9，R 11，，R 11，R 14，R 15，R 15，R 16， R 17和R 17具有在说明书中指出的含义，作为具有体外对大鼠前列腺的雌激素受体制剂具有更高亲和力的药物活性成分而不是雌激素受体制剂的大鼠子宫和体内与子宫相比优于骨骼的优势，和/或相对于刺激5HT2a受体和转运蛋白表达的显着作用，其生产，其治疗用途和药物分配包含新化合物的形式。本发明进一步描述了用于治疗雌激素缺乏诱导的疾病和病症以及在有兴趣解离的化合物的总体结构中使用三烯结构部分的用途，与子宫相比，它们对骨骼的雌激素作用。

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