Schering Aktiengesellschaft

Jenapharm Gmbh & Co. Kg

Bayer Schering Pharma Ag

Hans-Udo Schweikert

Walter Elger

Alexander Hillisch

Peter Droescher

Bernd Menzenbach

Ulf Tunn

Theodor Senge

Ulrich Bothe

Birgitt Schneider

Gudrun Reddersen

Friedmund Neumann

Gunter Kaufmann

Klaus Schoellkopf

Gerd Muller

Birgit Schneider

Friedmund Numann

New 17&#x3b1;-fluorosteroid compounds of formula (I) are disclosed: wherein Rdenotes H or methyl; Rand Reach denote H, Cl or methyl; and either a double bond or a single bond is present between C-6 and C-7 and also C-9 and C-10 of the steroid ring system respectively. These compounds have an activity profile with hybrid character so that they act as inhibitors for 5&#x3b1;-reductase and as high potency gestagens. Pharmaceutical compositions containing them are disclosed. They are suitable for treatment of conditions, which are caused by high levels of androgen in organs and tissues. These new compounds can be used in combination with other hormonal substances, such as estrogens, testosterone and other androgens, as contraceptives and for other applications.

17&#x3b1;-fluorosteroids, pharmaceutical compositions containing 17&#x3b1;-fluorosteroids and a method of making them

17-methylene-4-azasteroid compounds of formula I: wherein Rdenotes fluoro, chloro or bromo Rdenotes hydrogen, Rand Reach denote a hydrogen atom or a methyl group, and Rand Reach denote a hydrogen atom or together denote an additional bond, are useful for treating diseases or conditions caused by excessive androgen levels, such as acne, prostate diseases, alopecia and hirsutism, as well as gynecological conditions. Methods of synthesizing the new 17-methylene-4-azasteroid compounds are described.

Methylene-4-azasteroids

The invention relates to 17-methylene steroids, process for their production and pharmaceutical compositions that contain these compounds. The compounds according to the invention have a hybrid-type profile of action in the sense that they act as inhibitors of 5&#x3b1;-reductase and simultaneously as gestagens. They are therefore suitable for treating diseases that are the result of elevated androgen levels in certain organs and tissues in men and women. Together with other hormonal substances, such as an estrogen, testosterone or a strong androgen, the compounds according to the invention are suitable as contraceptive agents for women and for men.

17-Methylene steroids, process for their production and pharmaceutical compositions that contain these compounds

A combination of an aromatase-inhibitor and an antiandrogen in a weight ratio of aromatase-inhibitor to antiandrogen of 20:1 to 1:1 is useful in a method of prophylaxis and/or of treatment by therapy of prostatic hyperplasia. The aromatase-inhibitor is, for example, testolactone and the antiandrogen is, for example, cyproterone acetate.

Combinations of an aromatase-inhibitor and an antiandrogen for

Aromatase-inhibitors are used in a method of prophylaxis and/or treatment by therapy of prostatic hyperplasia. Pharmaceutical preparations suitable for such a use comprise an aromatase-inhibitor. A particularly preferred aromatase-inhibitor is, for example, testolactone.

Use of aromatase-inhibitors for prophylaxis and/or treatment of benign

Growing community of inventors

Bonn, Germany

Hans-Udo Schweikert