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发明授权
US06958327B1 18 Norsteroids as selectively active estrogens 失效
18只小鼠作为选择性活性雌激素

18 Norsteroids as selectively active estrogens
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（中）：

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

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