Schering Aktiengesellschaft

Shering Ag

Martin Schneider

Rolf Bohlmann

Yukishige Nishino

Arwed Cleve

Wolfgang Schwede

Karsten Parczyk

Gerhard Sauer

Gunter Neef

Rosemarie Lichtner

Hermann Kunzer

Ulrich Klar

Kristof Chwalisz

Nikolaus Heinrich

Ulrike Fuhrmann

Helmut Hofmeister

Dieter Bittler

David A Henderson

Peter Strehlke

Holger Heb-Stumpp

Walter Elger

Eckhard Ottow

Josef Heindl

Christa Hegele-Hartung

Erwin Von Angerer

Krzysztof Chwalisz

Jens Hoffmann

Jorg Kroll

Hans-Peter Muhn-Seipoldy

Christian Biberger

Rudolf Wiechert

Gerhard Siemeister

Ludwig Zorn

Karl-Heinrich Fritzemeier

Ekkehard Schillinger

Monika Lessl

Christoph Huwe

Karl Heinrich Fritzemeier

Joseph Heindl

Hermann K&uuml;nzer

Eckhardt Ottow

Sebastian Erber

Christa Hegelehartung

The present invention relates to methods and uses for preventing or treating hormone-dependent disease, in particular breast cancer, in a mammal by antiprogestins, in particular antiprogestin 11&#x3b2;-(4-acetylphenyl)-17&#x3b2;-hydroxy-17&#x3b1;-(1,1,2,2,2-pentafluoroethyl)-estra-4,9-dien-3-one or a pharmaceutically acceptable derivative or analogue thereof. The invention further relates to pharmaceutical compositions comprising said antiprogestin.

Use of antiprogestins for prophylaxis and treatment of hormone-dependent diseases

This invention describes the new 17&#x3b1;-fluoroalkyl steroids of general formula I as well as their physiologically compatible salts with bases. The new compounds have an extraordinary strong antigestagenic action and are suitable for the production of pharmaceutical preparations.

Antigestagenically active steroids with a fluorinated 17&#x3b1;-alkyl chain

Antigestagenically active steroids with a fluorinated 17-alpha-alkyl chain

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

2-phenylindoles are described, as well as a process for making them, pharmaceutical preparations that contain them, methods of using them as pharmaceutical agents.

2-phenylindoles as antiestrogenic pharmaceutical agents

Antigestagenically active steroids with a fluorinated 17&agr;-alkyl chain

This invention describes the new 17&agr;-fluoroalkyl steroids of general formula I

Antigestagenically active steroids with a flourinated 17 &agr;-alkyl chain

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

Steroid esters of formula I ##STR1## are described, wherein m, n and x are as defined by the specification. The compounds are distinguished from the basic hydroxy compounds by considerably improved solubility as well by increased biological activity and selectivity. The compounds are suitable for the production of pharmaceutical agents.

Steroid esters, process for their production and their pharmaceutical use

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,

6,7-modified 11.beta.-aryl-4-oestrenes

Growing community of inventors

Berlin, Germany

Martin Schneider