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1. 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

2. 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。

3. 发明授权

US06670347B2 19-nor-17&agr;-pregna-1,3,5(10)-trien-17&bgr;-ols with a 21,16&agr;-lactone ring 失效
标题翻译：具有21,16α-内酯环的19-nor-17α-前 - 1,3,5（10） - 三烯-17β-
公开(公告)号：US06670347B2
公开(公告)日：2003-12-30
申请号：US09963685
申请日：2001-09-27
申请人： Gerd Müller , Uwe Kollenkirchen , Dirk Kosemund , Karl-Heinrich Fritzemeier , Walter Elger
发明人： Gerd Müller , Uwe Kollenkirchen , Dirk Kosemund , Karl-Heinrich Fritzemeier , Walter Elger
IPC分类号： A61K31585
CPC分类号： C07J71/0005 , Y10S514/825
摘要： This invention relates to new 19-nor-17&agr;-pregna-1,3,5(10)-trien-17&bgr;-ols with a 21,16&agr;-lactone ring of formula II, process for their production and pharmaceutical preparations that contain these compounds as well as 17&agr;-cyanomethylated estra-1,3,5(10)-trienes, which produce intermediate products on the way to the 19-nor-17&agr;-pregna-1,3,5(10)-trien-17&bgr;-ols. The 19-nor-17&agr;-pregna-1,3,5(10)-trien-17&bgr;-ols produce novel selective estrogens, which contrast to standard estrogens, such as estradiol, show a preference for one of the two known estrogen receptors, estrogen receptor alpha.
摘要翻译：本发明涉及具有式II的21,16α-内酯环的新的19-去甲-17α-前 - 1,3,5（10） - 三烯-17β-环，其制备方法和含有这些化合物的药物制剂以及17α-氰基甲基化的雌-1,3,5（10） - 三烯，其在通过19-nor-17α-前 - 1,3,5（10） - 三烯-17β-氧化物的途中产生中间产物 19-nor-17alpha-pregna-1,3,5（10） - 三烯-17β-ols产生新的选择性雌激素，其与标准雌激素（例如雌二醇）形成对照，显示出对两种已知雌激素受体之一的偏好，雌激素受体α。

4. 发明申请

US20080182829A1 8Beta-Hydrocarbyl-Substituted Estratrienes As Selectively Active Estrogens 审中-公开
标题翻译： 8Beta-Hydrocarbyl-Substituted Estratrienes As Selective Active Estrogens
公开(公告)号：US20080182829A1
公开(公告)日：2008-07-31
申请号：US12045979
申请日：2008-03-11
申请人： Olaf Peters , Alexander Hillisch , Ina Thieme , Walter Elger , Christa Hegele-Hartung , Uwe Kollenkirchen , Karl-Heinrich Fritzemeier , Vladimir Patchev
发明人： Olaf Peters , Alexander Hillisch , Ina Thieme , Walter Elger , Christa Hegele-Hartung , Uwe Kollenkirchen , Karl-Heinrich Fritzemeier , Vladimir Patchev
IPC分类号： A61K31/58 , A61K31/565 , A61P25/28 , A61P19/02 , A61P1/00 , A61P15/00
CPC分类号： C07J1/007 , C07J1/0059 , C07J1/0062 , C07J1/0074 , C07J41/0072
摘要： This invention describes the new 8β-substituted estratrienes of general formula I in which R2, R3, R6, R6′, R7, R7′, R9, R11, R11′, R12, R14, R15, R15′, R16, R16′, R17, R17′ have the meanings that are indicated in the description, and R8 means a straight-chain or branched-chain, optionally partially or completely halogenated alkyl or alkenyl radical with up to 5 carbon atoms, an ethinyl- or prop-1-inyl radical, 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 preferably a preferential action on bone rather than the uterus and/or a pronounced action with respect to stimulation of the expression of 5HT2a-receptors and 5HT2a-transporters, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention also describes the use of these compounds for treatment of estrogen-deficiency-induced diseases and conditions as well as the use of an 8β-substituted estratriene structural part in the total structures of compounds that have a dissociation in favor of their estrogenic action on bones rather than the uterus.
摘要翻译：本发明描述了通式I的新的8-取代的雌三烯，其中R 2，R 3，R 6，R 6， R 7，R 7，R 9，R 11，R 11， > 11'，R 12，R 14，R 15，R 15'，R 15， R 16，R 16，R 17，R 17，R 17具有在说明书中指出的含义， R 8是指具有至多5个碳原子的直链或支链，任选部分或完全卤代的烷基或烯基，乙炔基或丙-1-基基团作为药物活性物质具有体外对大鼠前列腺的雌激素受体制剂的亲和力高于大鼠子宫雌激素受体制剂的体内成分，并且在体内优选对骨骼而不是子宫的优先作用和/或对刺激表达的显着作用 5HT2a受体和5HT2a转运蛋白，它们的产物 n，其治疗用途和含有新化合物的药物分配形式。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，以及在具有有利于其雌激素作用的解离的化合物的总体结构中使用8-取代的雌三醇结构部分骨头而不是子宫。

5. 发明授权

US07378404B2 8β-hydrocarbyl-substituted estratrienes for use as selective estrogens 失效
标题翻译：用作选择性雌激素的8-烃基取代的雌三烯
公开(公告)号：US07378404B2
公开(公告)日：2008-05-27
申请号：US10257288
申请日：2001-04-12
申请人： Olaf Peters , Alexander Hillisch , Ina Thieme , Walter Elger , Christa Hegele-Hartung , Uwe Kollenkirchen , Karl-Heinrich Fritzemeier , Vladimir Patchev
发明人： Olaf Peters , Alexander Hillisch , Ina Thieme , Walter Elger , Christa Hegele-Hartung , Uwe Kollenkirchen , Karl-Heinrich Fritzemeier , Vladimir Patchev
IPC分类号： A61K31/56 , C07J1/00
CPC分类号： C07J1/007 , C07J1/0059 , C07J1/0062 , C07J1/0074 , C07J41/0072
摘要： This invention describes the new 8β-substituted estratrienes of general formula I in which R2, R3, R6, R6′, R7, R7′, R9, R11, R11′, R12, R14, R15, R15′, R16, R16′, R17 and R17′ have the meanings that are indicated in the description, and R8 means a straight-chain or branched-chain, optionally partially or completely halogenated alkyl or alkenyl radical with up to 5 carbon atoms, an ethinyl- or prop-1-inyl radical, 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 preferably a preferential action on bone rather than the uterus and/or a pronounced action with respect to stimulation of the expression of 5HT2a-receptors and 5HT2a-transporters, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention also describes the use of these compounds for treatment of estrogen-deficiency-induced diseases and conditions as well as the use of an 8β-substituted estratriene structural part in the total structures of compounds that have a dissociation in favor of their estrogenic action on bones rather than the uterus.
摘要翻译：本发明描述了通式I的新的8-取代的雌三烯，其中R 2，R 3，R 6，R 6， R 7，R 7，R 9，R 11，R 11， > 11'，R 12，R 14，R 15，R 15'，R 15， R 16，R 17，R 17和R 17'具有在说明书中指出的含义， R 8是指具有至多5个碳原子的直链或支链，任选部分或完全卤代的烷基或烯基，乙炔基或丙-1-基基团作为药物活性物质具有体外对大鼠前列腺的雌激素受体制剂的亲和力高于大鼠子宫雌激素受体制剂的体内成分，并且在体内优选对骨骼而不是子宫的优先作用和/或对刺激表达的显着作用 5HT2a受体和5HT2a转运蛋白，其产品其治疗用途和含有新化合物的药物分配形式。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，以及在具有有利于其雌激素作用的解离的化合物的总体结构中使用8-取代的雌三醇结构部分骨头而不是子宫。

6. 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。

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