Jenapharm Gmbh & Co. Kg

Schering Aktiengesellschaft

Ina Thieme

Sigfrid Schwarz

Walter Elger

Vladimir Patchev

Wolfgang Roemer

Alexander Hillisch

Karl-Heinrich Fritzemeier

Michael Oettel

Christa Hegele-Hartung

Birgitt Schneider

Olaf Peters

Guenter Kaufmann

Gudrun Reddersen

Bernd Undeutsch

Uwe Kollenkirchen

Margit Richter

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

14, 15-.&agr;.-methylene equilenine derivatives, methods for producing the same and medicaments containing them

Pharmaceutical preparations containing selected steroid compounds and methods of treating estrogen deficiency in the central nervous system (CNS) without influencing other organs or systems are described. These steroids have selective neurotropic estrogen-like transcription action in contrast to the systemically acting natural and synthetic estrogen compounds, such as 17&agr;-estradiol. The selected steroids surprisingly have a selective influence on the transcription estrogen-dependent gene in the CNS and cause changes of physiological parameters as well as CNS-specific transcription effects in the dosages used with no biological effects in reproductive system tissues. They have CNS specific transcription effects at those dosages at which neither 17 &bgr;-estradiol nor 17&agr;-estradiol had any action and the transcription estrogen-dependent gene in the CNS is not influenced by secondarily formed 17&bgr;-estradiol.

Pharmaceutical preparations for treatment of estrogen deficiency in the central nervous system

The invention relates to new sulfamate derivatives of 1,3,5(10)-estratriene derivatives of the general formula I ##STR1## wherein the 3-sulfamate moiety is acylated, sulfonated or amidosulfonated. Furthermore, methods for the production of the compound and pharmaceutical preparations containing this compound are described. The compounds according to the invention have an estrogenic effect.

Sulfamate derivatives of 1,3,5(10)-estratriene derivatives, methods for

Growing community of inventors

Graitschen, Germany

Ina Thieme