Jenapharm Gmbh & Co. Kg

Wolfgang Roemer

Sigfrid Schwarz

Guenter Kaufmann

Ina Thieme

Walter Elger

Michael Oettel

Birgitt Schneider

Peter Droescher

Bernd Menzenbach

Bernd Undeutsch

Vladimir Patchev

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

New non-estrogenic derivative compounds of estradiol, which have no estrogenic activity and comparatively high anti-oxidative activity, are disclosed. These new non-estrogenic derivative compounds are potentially useful as non-estrogenic antioxidants, especially for administration in post-menopausal women and in men. The compounds of the invention can also inhibit aromatase and sulfatase.

Non-estrogenic estradiol derivative compounds with anti-oxidative activity

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

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Jena, Germany

Wolfgang Roemer