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    18-Methyl-19-nor-17-pregn-4-ene-21,17-carbolactones, as well as pharmaceutical preparations that contain the latter
    2.
    发明申请
    18-Methyl-19-nor-17-pregn-4-ene-21,17-carbolactones, as well as pharmaceutical preparations that contain the latter 失效
    18-甲基-19-去甲-17-孕-4-烯-21,17-碳内酯，以及含有后者的药物制剂

    公开(公告)号：US20060252737A1

    公开(公告)日：2006-11-09

    申请号：US11321449

    申请日：2005-12-30

    申请人： Rolf Bohlmann ,  Dieter Bittler ,  Hermann Kuenzer ,  Peter Esperling ,  Hans-Peter Muhn ,  Karl-Heinrich Fritzemeier ,  Ulrike Fuhrmann ,  Katja Prelle ,  Steffen Borden

    发明人： Rolf Bohlmann ,  Dieter Bittler ,  Hermann Kuenzer ,  Peter Esperling ,  Hans-Peter Muhn ,  Karl-Heinrich Fritzemeier ,  Ulrike Fuhrmann ,  Katja Prelle ,  Steffen Borden

    IPC分类号： A61K31/58 ,  C07J19/00

    CPC分类号： C07J19/00

    摘要： This invention describes the new 18-methyl-19-nor-17-pregn-4-ene-21,17-carbolactones of general formula I in which Z means an oxygen atom, two hydrogen atoms, a grouping ═NOR or ═NNHSO2R, whereby R is a hydrogen atom or a straight-chain or branched-chain alkyl group with 1 to 4 or 3 to 4 carbon atoms, R4 is a hydrogen atom, a halogen atom, a methyl group, or a trifluoromethyl group, R6 and/or R7 can be in α- or β-position, and, independently of one another, mean a straight-chain or branched-chain alkyl group with 1 to 4 or 3 to 4 carbon atoms, or R6 means a hydrogen atom, and R7 means an α- or β-position, straight-chain or branched-chain alkyl group with 1 to 4 or 3 to 4 carbon atoms, or R6 and R7 each mean a hydrogen atom, or R6 and R7 together mean an α- or β-position methylene group or an additional bond. The new compounds have gestagenic and anti-mineralocorticoid action and are suitable for the production of pharmaceutical preparations, for example for oral contraception and the treatment of pre-, peri- and post-menopausal symptoms.

    摘要翻译： 本发明描述了通式I的新的18-甲基-19-去甲-17-孕甾-4-烯-21,17-碳内酯，其中Z表示氧原子，两个氢原子，-NOR或-NNHSO- R 2是氢原子或具有1至4或3至4个碳原子的直链或支链烷基，R 4是氢原子 ，卤素原子，甲基或三氟甲基，R 6和/或R 7可以是α-或β-位，并且独立地为一个 另一个是指具有1至4或3至4个碳原子的直链或支链烷基，或R 6表示氢原子，R 7表示 具有1至4或3至4个碳原子的α-或β-位的直链或支链烷基，或R 6和R 7各自表示 氢原子或R 6和R 7一起是指α-或β-位亚甲基或另外的键。 新化合物具有孕激素和抗盐皮质激素的作用，并且适用于制备药物制剂，例如用于口服避孕和治疗绝经前，绝经期和绝经后症状。

    18-nor steroids as selectively active estrogens
    4.
    发明申请
    18-nor steroids as selectively active estrogens 审中-公开
    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。

    18 Norsteroids as selectively active estrogens
    5.
    发明授权
    18 Norsteroids as selectively active estrogens 失效
    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

    Glucocorticoids
    8.
    发明授权
    Glucocorticoids 失效
    糖皮质激素

    公开(公告)号：US5616573A

    公开(公告)日：1997-04-01

    申请号：US530352

    申请日：1995-10-06

    申请人： Hans J. Zentel ,  Michael Topert ,  Henry Laurent ,  Thomas Brumby ,  Peter Esperling

    发明人： Hans J. Zentel ,  Michael Topert ,  Henry Laurent ,  Thomas Brumby ,  Peter Esperling

    IPC分类号： A61K31/57 ,  A61K31/58 ,  A61P29/00 ,  C07J41/00 ,  C07J43/00 ,  C07J5/00

    CPC分类号： C07J41/005 ,  C07J43/003

    摘要： Glucocorticoids of general formula IR--Val--O--GC (II),are described,in whichO-GC is the radical of a 21-hydroxycorticoid that has an antiinflammatory action,Val represents a valine radical in the 21-position of the corticoid andR means a hydrogen atom or a hydrocarbon radical with up to 32 carbon atoms that is optionally substituted by hydroxy groups, amino groups, oxo groups and/or halogen atoms and/or interrupted by oxygen atoms, SO.sub.2 groups and/or NH groups and their salts.

    摘要翻译： PCT No.PCT / EP94 / 00937 371日期1995年10月6日 102（e）日期1995年10月6日PCT 1994年3月24日PCT公布。 出版物WO94 / 22898 日期：1994年10月13日描述了通式IR-Val-O-GC（II）的糖皮质激素，其中O-GC是具有抗炎作用的21-羟基皮质激素的基团，Val表示21位的缬氨酸基团 皮质激素和R表示氢原子或具有多至32个碳原子的烃基，其任选被羟基，氨基，氧代基和/或卤素原子取代和/或被氧原子，SO2基团和 /或NH基及其盐。