Schering Aktiengesellschaft

Bayer Schering Pharma Ag

Schring Aktiengesellschaft

Karsten Parczyk

Rolf Bohlmann

Rosemarie Lichtner

Martin Schneider

Gerhard Sauer

Yukishige Nishino

Nikolaus Heinrich

Helmut Hofmeister

Dieter Bittler

Karl-Heinrich Fritzemeier

Monika Lessl

Hermann Kunzer

Ulrich Klar

Arwed Cleve

Josef Heindl

Christa Hegele-Hartung

Jens Hoffmann

Volker Schulze

Dieter Zopf

Jorg Kroll

Andreas Reichel

Ludwig Zorn

Christoph Huwe

Joseph Heindl

Christa Hegelehartung

Hermann K&uuml;nzer

This invention relates to anti-androgenic N-[&#x3c9;-[3-[4-cyano-3-(trifluoromethyl)-phenyl]-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl]alkyl]-substituted pyrrolidines of general formula I, with a strongly pronounced antiproliferative profile of action; process for the production of the compounds of general formula I, pharmaceutical preparations and the use for the production of pharmaceutical agents.

Anti-androgenic pyrrolidines with tumor-inhibiting action

This invention relates to new antiestrogens of the general formulain which the substituents have the meanings that are explained in more detail in the description. The new compounds are a) pure antiestrogens or b) antiestrogens with partial estrogenic action (tissue-selective estrogens). Based on these properties, the new compounds are suitable for the production of pharmaceutical agents: in the case of a), for example, for the treatment of breast cancer; in the case of b), for example, for hormone replacement therapy.

Antiestrogens, process for their production and their pharmaceutical use

11&bgr;-HALOGEN-7&agr;-SUBSTITUTED ESTRATRIENES, PROCESS FOR THE PRODUCTION OF PHARMACEUTICAL PREPARATIONS THAT CONTAIN THESE 11&bgr;-HALOGEN-7&agr;-SUBSTITUTED ESTRATRIENES AS WELL AS THEIR USE FOR THE PRODUCTION OF PHARMACEUTICAL AGENTS

The invention relates to new 7&agr;, 17&agr;, 17&bgr;-substituted testosterone derivatives of general formula (I) and their use as pure antiandrogens for the long-term therapy of androgen-dependent diseases, notably for the long-term antiandrogen therapy of prostate carcinoma. In the general formula (I) A is an unbranched C -C -alkylene group; B is an oxygen atom, &mdash;S(O) &mdash; group, in which p is 0, 1 or 2, an iminocarbonyl group &mdash;C(O)N(Y)&mdash;, an imino group &mdash;N(Y)&mdash;, a carbonylimino group &mdash;N(Y)C(O)&mdash;, a sulfonylimino group &mdash;NN(Y)S(O) &mdash;, where Y is a hydrogen atom or a C -C -alkyl group, a sulfonyloxy group &mdash;OS(O) &mdash;, a dimethylsilyloxy group &mdash;O&mdash;Si(CH ) &mdash; or a carbonylsulfanyl group &mdash;SC(O)&mdash; or a bond between A and C or, together with C, a bond between A and D; C is a bond between B and D or, together with B, a bond between A and D or an unbranched C -C -alkylene group, a phenylene group, a substituted phenylene group, a five-membered ring or six-membered ring heteroarylene group, a substituted five-membered ring or six-membered ring heteroarylene group or a five-membered ring or six-membered ring heteroarylene group fused with a phenyl ring; and D is a hydrogen atom, a C -C -alkyl group, a vinyl group, a C -C -alkoxy group, a C -C -alkoxycarbonyl group, a bis(C -C -alkoxycarbonyl)methyl group, an acetyl(C -C -alkoxybonyl)methyl group, a cyan group, a carboxy group, an azide group, a hydroxy group, a halogen atom or a rest of the formula C F H , in which n is 1, 2, 3 or 4, m>1 and m&plus;o&equals;2n&plus;1.

New7&agr;, 17&agr;-bis-alkylated testosterone derivatives and their use in long-term therapy of androgen-dependent diseases

Antiestrogens, process for their protection and their pharmaceutical use

This invention describes the new 7&agr;-(5-methylaminopentyl)-estratrienes of general formula I

7 &agr;-(5-methylaminopentyl)-estratrienes, process for their production, pharmaceutical preparations that contain these 7 &agr;(5-methylaminopentyl)-estratrienes as well as their use for the production of pharmaceutical agents

This invention describes new, substituted 7&agr;-(&egr;-aminoalkyl)-estratrienes of general formula I

7&agr;-(xi-aminoalkyl)-estratrienes, process for their production, pharmaceutical preparations which contain these 7&agr;-(xi-aminoalkyl-estratrienes as well as their use for the production of pharmaceutical agents

This invention relates to new antiestrogens of the general formula ##STR1## in which the substituents have the meanings that are explained in more detail in the description. The new compounds are a) pure antiestrogens or b) antiestrogens with partial estrogenic action (tissue-selective estrogens). Based on these properties, the new compounds are suitable for the production of pharmaceutical agents: in the case of a), for example, for the treatment of breast cancer; in the case of b), for example, for hormone replacement therapy.

This invention describes new, substituted 7.alpha.-(.xi.-aminoalkyl)-estratrienes of general formula I ##STR1## in which side chain SK is a radical of partial formula ##STR2## as well as their physiologically compatible addition salts with organic and inorganic acids. The new compounds represent compounds with very strong antiestrogenic action. The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.

7.alpha.-(.xi.-aminoalkyl)-estratrienes, process for their production,

This invention describes the new triphenylethylenes of general formula I ##STR1## in which n means an integer from 1 to 10,

Triphenylethylenes, process for their production, pharmaceutical

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Berlin, Germany

Karsten Parczyk