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    17alpha-fluorosteroids, pharmaceutical compositions containing 17alpha-fluorosteroids and a method of making them
    3.
    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。

    18-nor steroids as selectively active estrogens
    8.
    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。