Schering Aktiengesellschaft

Jenapharm Gmbh & Co. Kg

Zentaris Ag

Jenapharm Gmbh

Bayer Schering Pharma Ag

Schering Aktiengesellschaft Patents

Peter Droescher

Bernd Menzenbach

Walter Elger

Norbert Schmees

Gunter Kaufmann

Alexander Hillisch

Michael Oettel

Werner Skuballa

Bernd Buchmann

Stefan Jaroch

Birgitt Schneider

Heike Schaecke

Konrad Krolikiewicz

Manfred Lehmann

Kurt Ponsold

Bernd Undeutsch

Hartwig Hennekes

Hans-Udo Schweikert

Wolfgang Romer

Jens Schroder

Harmur Rehwinkel

Emmanuel Polymeropoulos

Eckhard Guenther

Peter Strehlke

Holger Hess-Stumpp

Gudrun Reddersen

Peter Muhn

Arndr Schottelius

Antonius M Ter Laak

Ulrich Buehmann

Sven Ring

Ulrich Bothe

Sigfrid Schwarz

Guenter Kaufmann

Ralf Wyrwa

Klaus Schoellkopf

Wolfgang Roemer

Gerd Muller

Jens Schroeder

Rolf-Dieter Hesch

Roland K&uuml;hne

Arndt Schottelius

Birgit Schneider

Wolfgang R&ouml;mer

Roland Kühne

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 quinoline, isoquinoline and phthalazine derivatives as antagonists of the gonadotropin-releasing hormone.

Quinoline, isoquinoline and phthalazine derivatives as antagonists of the gonadotropin-releasing hormone

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

Compounds of Formula 1 are useful in the treatment of inflammation.

Nonsteroidal antiinflammatory agents

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

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

The method of prophylaxis and therapy of radical-mediated cell damage includes administering an effective amount of at least one steroid and at least one pharmaceutical adjuvant to a human being. The at least one steroid is selected from the group consisting of ent-estradiol, 17&agr;-estradiol, 8-dehydro-estradiol, 8-dehydro-17&agr;-estradiol, 8(14)-dehydroestradiol, 6,8-didehydro-17&agr;-estradiol, 6-dehydroestriol, 9(11)-dehydroestriol, 20-hydroxymethyl-3-hydroxy-19-norpregna-1,3,5(10)-triene, 14&agr;, 15&agr;-methylene-8-dehydroestradiol, 14&agr;, 15&agr;-methylene-estradiol, 2-hydroxy-estradiol-3-methyl ether, 3-hydroxy-1,3,5(10)-estratriene-17S-spirooxirane, 3-hydroxy-1,3,5(10),9(11)-estratetraene-17S-spirooxirane, and 14&bgr;,15&bgr;-methylene-8-dehydroestradiol. This method strongly inhibits changes in cells and tissues, such as lipid peroxidation and oxidation of low-density lipoprotein (LDL) cholesterol, triggered by reaction oxygen species, free oxygen radicals and other forms of radicals and thus reduces attendant irreversible membrane and endothelial damage.

Pharmaceutical compositions and method for prophylaxis and therapy of radical-mediated cell damage

Novel substituted steroid compounds are disclosed which are more effective than known radical-trapping agents in methods of prophylaxis and therapy of radical-mediated cell damage and of treatment of diseases due to radical-mediated cell damage. The novel substituted steroid compounds can be made from steroids having an estrane, androstane, pregnane or cholestane basic skeleton and have a radical-attracting aromatic substituent of the general formula --(CH.sub.2).sub.n X, or .dbd.CH--(CH.sub.2).sub.m X at the 17 or 6 position of the steroid nucleus, wherein X=Y, OY, SY, SeY or NHY; n=0 to 5; m=n-1 and Y is a phenyl group having five substituents A, B, C, D and E, wherein A to E is independently H, alkyl, Oalkyl, Oacyl, OH, or one of the substituents B, C or D is NR.sub.2 wherein R=alkyl and each of the other substituents is hydrogen. Pharmaceutical compositions containing the novel substituted steroid compounds and methods of making them are also part of the invention.

Steroids with radical-attracting aromatic substituents, process for the

Androgens and anabolic agents

Growing community of inventors

Weimar, Germany

Peter Droescher