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1. 发明授权

US06753326B1 14, 15-.&agr;.-methylene equilenine derivatives, methods for producing the same and medicaments containing them 失效
标题翻译： 14,15- a-亚甲基平均衍生物，其制备方法和含有它们的药物
公开(公告)号：US06753326B1
公开(公告)日：2004-06-22
申请号：US09937723
申请日：2002-01-28
申请人： Sigfrid Schwarz , Ina Thieme , Bernd Undeutsch , Guenter Kaufmann , Wolfgang Roemer
发明人： Sigfrid Schwarz , Ina Thieme , Bernd Undeutsch , Guenter Kaufmann , Wolfgang Roemer
IPC分类号： C07J5300
CPC分类号： C07J71/001 , C07J53/004
摘要： Described are novel equilenin derivatives of general formula I methods for producing the same and medicaments containing these compounds. The new compounds have antioxidative activity and are usable for geroprophylaxis in women and men.
摘要翻译：描述的是通式的新型均聚物衍生物及其制备方法和含有这些化合物的药物。新化合物具有抗氧化活性，可用于男性和女性的预防性感染。

2. 发明授权

US06245756B1 Pharmaceutical preparations for treatment of estrogen deficiency in the central nervous system 失效
标题翻译：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。

3. 发明授权

US5705495A Sulfamate derivatives of 1,3,5(10)-estratriene derivatives, methods for their production and pharmaceuticals containing these compounds 失效
标题翻译： 1,3,5（10） - 三亚甲基衍生物的氨基磺酸酯衍生物，其制备方法和含有这些化合物的药物
公开(公告)号：US5705495A
公开(公告)日：1998-01-06
申请号：US732742
申请日：1996-10-18
申请人： Sigfrid Schwarz , Walter Elger , Gudrun Reddersen , Birgitt Schneider , Ina Thieme , Margit Richter
发明人： Sigfrid Schwarz , Walter Elger , Gudrun Reddersen , Birgitt Schneider , Ina Thieme , Margit Richter
IPC分类号： C07J41/00 , A61K31/56 , A61K31/58 , C07J1/00 , C07J53/00
CPC分类号： C07J41/0072
摘要： The invention relates to new sulfamate derivatives of 1,3,5(10)-estratriene derivatives of the general formula I ##STR1## wherein the 3-sulfamate moiety is acylated, sulfonated or amidosulfonated. Furthermore, methods for the production of the compound and pharmaceutical preparations containing this compound are described. The compounds according to the invention have an estrogenic effect.
摘要翻译：本发明涉及通式Ⅰ（I）的1,3,5（10） - 三亚甲基衍生物的新的氨基磺酸酯衍生物，其中3-氨基磺酸酯部分被酰化，磺化或酰氨基磺化。此外，还描述了制备化合物的方法和含有该化合物的药物制剂。根据本发明的化合物具有雌激素作用。

4. 发明申请

US20090029957A1 8-BETA-SUBSTITUTED ESTRATRIENES AS SELECTIVELY ACTIVE ESTROGENS 审中-公开
标题翻译： 8-BETA取代的ESTRATRIENES作为选择性活动的ESTROGENS
公开(公告)号：US20090029957A1
公开(公告)日：2009-01-29
申请号：US12171424
申请日：2008-07-11
申请人： Olaf Peters , Nico Braeuer , Ina Thieme , Katja Prelle , Peter Muhn , Karl Heinrich Fritzemeier
发明人： Olaf Peters , Nico Braeuer , Ina Thieme , Katja Prelle , Peter Muhn , Karl Heinrich Fritzemeier
IPC分类号： A61K31/56 , A61K31/565 , C07J1/00 , A61P37/00 , A61P35/00 , A61P17/00 , A61P17/14 , A61P9/00 , A61P1/00
CPC分类号： C07J1/007 , C07J1/0062
摘要： The invention refers to 8β-substituted estra-1,3,5(10)-triene derivatives of general formula I their use 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 in the ovary in comparison to the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds.
摘要翻译：本发明涉及通式I的8-取代的雌-1,3,5（10） - 三烯衍生物，其用作药物活性成分，其具有比雌激素受体制剂在体外对雌激素受体制剂更高的亲和力与子宫相比，子宫中的子宫，其产生，其治疗用途和含有新化合物的药物分配形式相比在体内具有优先的作用。

5. 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。

6. 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。

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