Schering Aktiengesellschaft

Jenapharm Gmbh & Co. Kg

Bayer Schering Pharma Ag

Entec Gesellschaft Fuer Endokrinologische Technologie M.b.h.

Sterix Limited

Birgitt Schneider

Walter Elger

Gudrun Reddersen

Sigfrid Schwarz

Alexander Hillisch

Sven Ring

Olaf Peters

Christian Gege

Gerd Schubert

Peter Droescher

Guenter Kaufmann

Wilko Regenhardt

Jerzy Adamski

Gabriele Moeller

Ulrich Bothe

Bernd Menzenbach

Ralf Wyrwa

Lothar Sobek

Margit Richter

Dominga Deluca

G&uuml;nter Kaufmann

Dirk Kosemund

Michael Oettel

Michael Dittgen

Hans-Udo Schweikert

Ina Thieme

Thomas Michel

Ingo Tornus

Wolfgang Roemer

Doris Hubler

Ina Scherlitz-Hofmann

Gerd M&uuml;ller

Andrea Rosinus

Michael Ernst

By Frank Siemann, Heir

Hans-Joachim Siemann, Deceased

By Margit Lucas, Heir

Hans-Joachim Siemann

Christel Siemann

Elger Walter

Reddersen Gudrun

Sigfried Schwarz

Gabriele Möller

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 compounds of general formula I, their production and pharmaceutical preparations that contain these compounds. The compounds according to the invention are preferably used for female birth control and for HRT.

Progesterone receptor modulators with increased antigonadotropic activity for female birth control and hormone replacement therapy

The invention relates to estradiol prodrugs of general formula (I), in which group Z is bonded to the steroid, process for their production, pharmaceutical compositions that contain these compounds, as well as their use for the production of pharmaceutical agents with estrogenic action.

Estradiol prodrugs

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

The invention relates to &#x394;-D-homosteroids of general formula (I) process for their production and pharmaceutical compositions that contain these compounds. The compounds of general formula I according to the invention have androgenic activity.

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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

The invention concerns pharmaceutical preparations containing estra-1,3,5(10)-triene derivatives as active ingredients which carry a group of the general formulaR&#x2014;SO&#x2014;O&#x2014; The preparations according to the invention can be used for hormonal contraception and for hormon replacement therapy (HRT). They exhibit a low hepatic estrogenity.

Pharmaceutical preparations containing estra-1,3,5(10)-triene derivatives

Compounds of general formula I as well as their pharmaceutically compatible salts are described, in which R stands for hydrogen, C - to C -alkyl, COR , COOR , COSR or CONHR , in which R is C - to C -alkyl or unsubstituted or substituted aryl and in which R is hydrogen, C - to C -alkyl or unsubstituted or substituted aryl, in which R also stands for hydrogen, C - to C -alkyl or C - to C -acyl, and R stands for a C F group, in which n&equals;1, 2 or 3, or a CH O(CH ) C F group, in which m&equals;0 or 1 and n&equals;1, 2 or 3. In addition, a process for the production of the compounds with general formula I is indicated. The compounds can be used for the production of pharmaceutical agents.

17&agr;-fluoroalkyl-11&bgr;-benzaldoxime steroids, process for their production, pharmaceutical preparations that contain these steroids as well as their use for the production of pharmaceutical agents

C13-substituted estra-1,3,5,(10)-trien-3-yl sulfamates, methods of preparing same, and pharmaceutical compositions containing these compounds

Described are new, unsaturated 14,15-cyclopropano-androstanes of general formula (I) and their pharmaceutically acceptable salts, a process for their production and pharmaceutical preparations that contain these compounds. The compounds are characterized by hormonal (gestagenic and/or androgenic) activity and may be used for hormone replacement therapy.

Unsaturated 14, 15-cyclopropanoandrostanes, method for the production thereof and pharmaceutical preparations containing said compounds

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

Described are new 14,15-cyclopropano steroids of the 19-norandrostane series of general formula (I) and their pharmaceutically acceptable salts, a process for their production and pharmaceutical preparations that contain these compounds. The compounds are distinguished by hormonal (gestagenic and/or androgenic) activity.

14,15-cyclopropano steroids of the 19-norandrostane series, method for the production thereof and pharmaceutical preparations containing said compounds

Estra-1,3,5(10)-trien derivatives, processes for their preparation and

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Jena, Germany

Birgitt Schneider