Schering Aktiengesellschaft

Uwe Kollenkirchen

Karl-Heinrich Fritzemeier

Christa Hegele-Hartung

Walter Elger

Alexander Hillisch

Gerhard Sauer

Dirk Kosemund

Wolfgang Schwede

Ludwig Zorn

Rolf Jautelat

Olaf Peters

Peter Esperling

Hermann Kuenzer

Werner Boidol

Vladimir Patchev

Ina Thieme

Gerd M&uuml;ller

This invention describes the new 8&#x3b2;-substituted estratrienes of general formula I in which R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, Rand Rhave the meanings that are indicated in the description, and Rmeans 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 8&#x3b2;-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.

8&#x3b2;-hydrocarbyl-substituted estratrienes for use as selective estrogens

The invention relates to novel 18-norsteroids (gonatrienes) of general formula (I), wherein R, R, R, R, R, R, R, R, R, R, R, R, R, Rand Rhave 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

18 Norsteroids as selectively active estrogens

This invention describes the new 4-fluoroalkyl-2H-benzopyrans of general formula I,in which The new compounds have at their disposal strong antiestrogenic action. In addition, they can have at their disposal estrogenic action that occurs in a tissue-selective manner. They can be used for the production of pharmaceutical agents, especially for the treatment of estrogen-dependent diseases and tumors and pharmaceutical agents for hormone replacement therapy (HRT) as well as for the prevention and treatment of osteoporosis.

4-fluoroalkyl-2h-benzopyrans with anti-estogenic activity

19-nor-17&agr;-pregna-1,3,5(10)-trien-17&bgr;-ols with a 21,16&agr;-lactone ring

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Berlin, Germany

Uwe Kollenkirchen