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    COMPOUNDS WITH A SULPHONAMIDE GROUP AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS
    1.
    发明申请
    COMPOUNDS WITH A SULPHONAMIDE GROUP AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS 审中-公开
    具有磺酰胺基团的化合物和含有这些化合物的药物组合物

    公开(公告)号：US20090023896A1

    公开(公告)日：2009-01-22

    申请号：US12142332

    申请日：2008-06-19

    申请人： Walter Elger ,  Alexander Hillisch ,  Annemarie Hedden ,  Sigfrid Schwarz ,  Klaus Schollkopf

    发明人： Walter Elger ,  Alexander Hillisch ,  Annemarie Hedden ,  Sigfrid Schwarz ,  Klaus Schollkopf

    IPC分类号： C07K7/06 ,  C07J1/00

    CPC分类号： C07J41/0044 ,  C07J41/0038 ,  C07J41/005

    摘要： This invention relates to compounds that as prodrugs and/or vehicles make it possible for an active ingredient to be taken up into erythrocytes and/or an active ingredient to bind to erythrocytes, whereby the uptake of the compounds into erythrocytes and/or the binding of the compounds to erythrocytes is made possible by a group —SO2NR1R2, whereby R1 and R2, independently of one another, mean a hydrogen atom, an acyl group, an alkyl group, a cycloalkyl group, an aryl group, a cyano group or a hydroxy group. By the prodrugs according to the invention, active ingredients, such as endogenous substances, natural substances and synthetic substances with therapeutically valuable properties with a high “first pass” effect are made available orally to a reasonable extent or are decisively improved relative to oral activity.

    摘要翻译： 本发明涉及作为前药和/或载体的化合物，使活性成分能够摄入红细胞和/或活性成分以结合红细胞，由此将化合物摄入红细胞和/或结合 对于红细胞的化合物可以通过基团-SO 2 NR 1 R 2来实现，其中R 1和R 2彼此独立地表示氢原子，酰基，烷基，环烷基，芳基，氰基或羟基 组。 通过根据本发明的前药，可以以合理的方式口服提供活性成分，例如内源物质，天然物质和具有高“第一道”效果的治疗有价值的性质的合成物质，或者相对于口服活性而言是有显着改善的。

    8Beta-Hydrocarbyl-Substituted Estratrienes As Selectively Active Estrogens
    2.
    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。

    SUBSTITUTED ESTRATRIENES AS SELECTIVELY ACTIVE ESTROGENS
    3.
    发明申请
    SUBSTITUTED ESTRATRIENES AS SELECTIVELY ACTIVE ESTROGENS 审中-公开
    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。

    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。

    17alpha-fluorosteroids, pharmaceutical compositions containing 17alpha-fluorosteroids and a method of making them
    9.
    发明申请
    17alpha-fluorosteroids, pharmaceutical compositions containing 17alpha-fluorosteroids and a method of making them 失效
    17α-含氟类固醇，含有17α-荧光素的药物组合物及其制备方法

    公开(公告)号：US20050234027A1

    公开(公告)日：2005-10-20

    申请号：US11104736

    申请日：2005-04-13

    申请人： Ulrich Bothe ,  Peter Droescher ,  Walter Elger ,  Gudrun Reddersen ,  Bernd Menzenbach ,  Hans-Udo Schweikert ,  Alexander Hillisch ,  Birgett Schneider

    发明人： Ulrich Bothe ,  Peter Droescher ,  Walter Elger ,  Gudrun Reddersen ,  Bernd Menzenbach ,  Hans-Udo Schweikert ,  Alexander Hillisch ,  Birgett Schneider

    IPC分类号： A61K31/57 ,  C07J3/00

    CPC分类号： C07J3/00

    摘要： New 17α-fluorosteroid compounds of formula (I) are disclosed: wherein R1 denotes H or methyl; R2 and R3 each denote H, Cl or methyl; and either a double bond or a single bond is present between C-6 and C-7 and also C-9 and C-10 of the steroid ring system respectively. These compounds have an activity profile with hybrid character so that they act as inhibitors for 5α-reductase and as high potency gestagens. Pharmaceutical compositions containing them are disclosed. They are suitable for treatment of conditions, which are caused by high levels of androgen in organs and tissues. These new compounds can be used in combination with other hormonal substances, such as estrogens, testosterone and other androgens, as contraceptives and for other applications.

    摘要翻译： 公开了式（I）的新的17α-荧光素类化合物：其中R 1表示H或甲基; R 2和R 3各自表示H，Cl或甲基; 并且分别存在于类固醇环体系的C-6和C-7之间以及C-9和C-10之间的双键或单键。 这些化合物具有混合特征的活性谱，因此它们作为5α-还原酶的抑制剂和作为高效力的孕激素。 公开了含有它们的药物组合物。 它们适用于治疗由器官和组织中高水平雄激素引起的病症。 这些新化合物可以与其他荷尔蒙物质（如雌激素，睾酮和其他雄激素）一起使用，作为避孕药具和其他应用。

    11β-Substituted 19-nor-17-α-pregna-1,3,5(10)-trien-17β-ols with a 21,16α-lactone ring
    10.
    发明授权
    11β-Substituted 19-nor-17-α-pregna-1,3,5(10)-trien-17β-ols with a 21,16α-lactone ring 失效
    11beta取代的19-nor-17-α-前 - 1,3,5（10） - 三烯-17β-酯与21,16α-内酯环

    公开(公告)号：US06956031B2

    公开(公告)日：2005-10-18

    申请号：US10397855

    申请日：2003-03-27

    申请人： Alexander Hillisch ,  Walter Elger ,  Rolf Bohlmann ,  Jens Hoffmann

    发明人： Alexander Hillisch ,  Walter Elger ,  Rolf Bohlmann ,  Jens Hoffmann

    IPC分类号： A61K31/58 ,  A61K31/585 ,  C07J17/00 ,  C07J71/00

    CPC分类号： C07J17/00

    摘要： This invention relates to new 19-nor-17α-pregna-1,3,5(10)-trien-17β-ols with a 21,16α-lactone ring with a long-chain substituent in 11β-position of general formula II in which R11 is a long-chain alkyl radical that has a nitrogen atom that can be substituted in terminal position with a perfluoroalkyl group. The compounds act in a tissue-selective manner as pure antiestrogens and are suitable for the production of pharmaceutical agents because of these properties.

    摘要翻译： 本发明涉及具有21,16α-内酯环的新的19-nor-17α-前 - 1,3,5（10） - 三烯-17β-环，其通式II在11b位具有长链取代基 其中R 11是具有可以在末端被全氟烷基取代的氮原子的长链烷基。 化合物以组织选择性的方式作为纯抗雌激素起作用，并且由于这些性质而适用于制药。