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    8Beta-Hydrocarbyl-Substituted Estratrienes As Selectively Active Estrogens
    3.
    发明申请
    8Beta-Hydrocarbyl-Substituted Estratrienes As Selectively Active Estrogens 审中-公开
    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。

    8β-hydrocarbyl-substituted estratrienes for use as selective estrogens
    4.
    发明授权
    8β-hydrocarbyl-substituted estratrienes for use as selective estrogens 失效
    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。

    Pharmaceutical preparations for treatment of estrogen deficiency in the central nervous system
    5.
    发明授权
    Pharmaceutical preparations for treatment of estrogen deficiency in the central nervous system 失效
    用于治疗中枢神经系统雌激素缺乏症的药物制剂

    公开(公告)号：US06245756B1

    公开(公告)日：2001-06-12

    申请号：US09252726

    申请日：1999-02-19

    申请人： Vladimir Patchev ,  Michael Oettel ,  Sigfrid Schwarz ,  Ina Thieme ,  Wolfgang Roemer

    发明人： Vladimir Patchev ,  Michael Oettel ,  Sigfrid Schwarz ,  Ina Thieme ,  Wolfgang Roemer

    IPC分类号： A61K31566

    CPC分类号： A61K31/567 ,  A61K31/565

    摘要： Pharmaceutical preparations containing selected steroid compounds and methods of treating estrogen deficiency in the central nervous system (CNS) without influencing other organs or systems are described. These steroids have selective neurotropic estrogen-like transcription action in contrast to the systemically acting natural and synthetic estrogen compounds, such as 17&agr;-estradiol. The selected steroids surprisingly have a selective influence on the transcription estrogen-dependent gene in the CNS and cause changes of physiological parameters as well as CNS-specific transcription effects in the dosages used with no biological effects in reproductive system tissues. They have CNS specific transcription effects at those dosages at which neither 17 &bgr;-estradiol nor 17&agr;-estradiol had any action and the transcription estrogen-dependent gene in the CNS is not influenced by secondarily formed 17&bgr;-estradiol.

    摘要翻译： 描述了含有选择的类固醇化合物的药物制剂和治疗中枢神经系统（CNS）中雌激素缺乏症的方法，而不影响其他器官或系统。 与系统作用的天然和合成雌激素化合物（如17α-雌二醇）相比，这些类固醇具有选择性神经营养因子雌激素样转录作用。 所选择的类固醇令人惊奇地对CNS中的转录雌激素依赖性基因具有选择性影响，并且在生殖系统组织中没有生物效应的剂量中引起生理参数的变化以及CNS特异性转录效应。 它们在17β-雌二醇和17α-雌二醇都不具有任何作用的那些剂量下具有CNS特异性转录效应，并且CNS中的转录雌激素依赖性基因不受二次形成的17β-雌二醇的影响。

    In Vitro screening for ligands of the estrogen receptor
    7.
    发明授权
    In Vitro screening for ligands of the estrogen receptor 失效
    体外筛选雌激素受体配体

    公开(公告)号：US07166438B2

    公开(公告)日：2007-01-23

    申请号：US09989952

    申请日：2001-11-20

    申请人： Vladimir Patchev ,  Youriy Mitev ,  Siegmund Wolf ,  Gernot Langer

    发明人： Vladimir Patchev ,  Youriy Mitev ,  Siegmund Wolf ,  Gernot Langer

    IPC分类号： G01N33/53

    CPC分类号： G01N33/743 ,  G01N2500/02 ,  G01N2500/04 ,  G01N2500/10 ,  G01N2500/20

    摘要： A method for in vitro screening a group of test substances for a ligand using two assay systems, i.e. a cellular or tissue assay system and an enzymatic assay system, is described. First, those test substances are selected which have transcriptional ER-mediated activity measured by an ER-driven reporter gene in the cellular or tissue assay system with an EC50(ER)(half-maximally effective ligand concentration) lower than or equal to 10 nmol/l. Then in an enzymatic assay system the selected test substances having the required transcriptional ER-mediated activity are tested by measuring a physical-chemical interaction (recruitment) of SRC-1 and the ER in the presence of the test substances. The selected ligand activates the ER and induces interaction with the co-present SRC-1 with an E50(ER+SRC) higher than or equal to 100 nmol/l. The ligands found by the inventive screening method are useful for treatment and prevention of neuro-degeneration in the cerebral cortex, especially of age-related cognitive disorders, affective disorders, Alzheimer's diseases and cerebral ischemia/stroke.

    摘要翻译： 描述了使用两个测定系统（即细胞或组织测定系统和酶测定系统）体外筛选配体的一组测试物质的方法。 首先，选择在细胞或组织测定系统中通过ER驱动的报告基因测量的具有转录ER介导活性的测试物质，其具有EC 50（ER）（半最大有效配体浓度 ）低于或等于10nmol / l。 然后在酶分析系统中，通过测量在存在测试物质的情况下测量SRC-1和ER的物理 - 化学相互作用（招募）来测试所选择的具有所需转录ER介导活性的测试物质。 选择的配体激活ER并诱导与共同存在的SRC-1与高于或等于100nmol / l的E 50（ER + SRC）的相互作用。 通过本发明筛选方法发现的配体可用于治疗和预防大脑皮质中的神经变性，特别是与年龄相关的认知障碍，情感障碍，阿尔茨海默病和脑缺血/卒中。