Schering Aktiengesellschaft

Bayer Schering Pharma Ag

Univerzita Palackeho V Olomouci

Ustav Organicke Chemie a Biochemie Av Cr, V.v.i.

Helmholtz Zentrum Munchen

Ustav Molekularni Genetiky Akademie Ved Cr, V.v.i.

Gabriele Moeller

Jerzy Adamski

Walter Elger

Alexander Hillisch

Christian Gege

Birgitt Schneider

Olaf Peters

Wilko Regenhardt

Dominga Deluca

Ulrich Bothe

Marian Hajduch

Petr Dzubak

Petr Bartunek

David Sedlak

Martin Kotora

Eva Prchalova

Andrea Rosinus

Ondrej Stepanek

15&#x3b2;-substituted derivatives of estrone of general formula I wherein R, R, R, R, Rare independently selected from the group consisting of: C-Calkyl, C-Calkoxy, C-Chalogenalkyl, halogen, COORwherein Ris C-Calkyl; H, OH; optionally, R, Rand Rare each formed by a hydrogen atom, while Rand Rtogether form an aryl group, preferably naphthyl, in which the aromatic ring in position C-15 can be mono-, di-, tri-, tetra- and penta-substituted with substituents R-R. Compounds of the invention may be used for diagnosis and possibly also for the treatment of estrogen-dependent diseases.

15&#x3b2;-substituted estrone derivatives as selective inhibitors of 17&#x3b2;-hydroxysteroid-dehydrogenases, method of preparation and use thereof

The invention relates to new 2-substituted D-homo-estra-1,3,5(10)-trienes of general formula I in which

2-substituted D-homo-estra-1,3,5(10)-trienes as inhibitors of 17&#x3b2;-hydroxy steroid dehydrogenase type 1

The invention relates to new 2-substituted estra-1,3,5(10)-trien-17-ones of formula I as well as their pharmaceutically acceptable salts, their methods of manufacture and use as medicaments for prophylaxis and/or therapy of estrogen-dependent diseases that can be influenced by the inhibition of 17&#x3b2;-hydroxy steroid dehydrogenase type 1.

2-substituted estra-1,3,5(10)-trien-17-ones as inhibitors of 17&#x3b2;-hydroxy steroid dehydrogenase type 1

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Munich, Germany

Gabriele Moeller