Schering Aktiengesellschaft

Gerhard Sauer

Gregor Haffer

Ulrich Eder

Rudolf Wiechert

Helmut Wachtel

Jurgen Ruppert

Gunter Neef

Yukishige Nishino

Josef Heindl

Rolf Bohlmann

Helmut Hofmeister

Herbert H Schneider

Martin Schneider

Thomas Brumby

Rosemarie Lichtner

Nikolaus Heinrich

Karsten Parczyk

Andreas Huth

Christa Hegele-Hartung

Jonathan Turner

Dieter Bittler

Helmut Hauser

Karl-Heinrich Fritzemeier

Wolfgang Kehr

Jorg Kroll

Hermann Kunzer

Peter-Andreas Loschmann

Peter A Loschmann

Juergen Ruppert

Henry Laurent

Sybille Beier

Ludwig Zorn

Helmut Biere

David A Henderson

Jens Hoffmann

Reinhard Horowski

Guenter Neef

Gertrud Schroeder

Hans Peter Lorenz

Gerhard Kuhne

Walter Elger

Alexander Hillisch

Wolfgang Schwede

Klaus Annen

Ulrich Kerb

Karl Petzoldt

Alfred Weber

Arwed Cleve

Wolfgang Losert

Mario Kennecke

Peter Esperling

Hermann Steinbeck

Ralph Rohde

Christoph Huwe

Paul-Eberhard Schulze

Monika Lessl

Werner Boidol

Rudolf Muller

Helmut Borner

Jean-Claude Hilscher

Uwe Kollenkirchen

Rainer Dorow

Bernard Acksteiner

Christa Hegelehartung

Alfred Popper

Hermann K&uuml;nzer

Bernd Schroter

The invention relates to novel 18-norsteroids (gonatrienes) of general formula (I), wherein R, R, R, R, R, R, R, R, R, R, R, R, R, Rand Rhave the meaning cited in the description, and to the use of said compounds as pharmaceutical active ingredients. Said compounds exhibit a high affinity in vitro for estrogen receptor preparations of rat prostate and in an estrogen receptor preparation of rat uterus. Said compounds exhibit in vivo preferential activity on bones as compared to the uterus and/or significant activity with regard to stimulating the expression of 5HT2a-receptors and transporter molecules. The invention also relates to the production of said compounds, therapeutic use and galenic form of said compounds contained in the novel compounds of invention. The invention also relates to utilization of steroids based on the gonatriene molecular skeleton in order to treat estrogen deficiency-induced diseases and disorders, in addition to the use of said gonatriene structural component in the total structure of compounds which dissociate to produce enhanced estrogen activity in bone as compared to the uterus

18 Norsteroids as selectively active estrogens

This invention describes a 11&bgr;-long-chain-substituted estratriene of general formula (I), in which R is a long-chain radical that has a nitrogen atom and optionally a sulfur atom, which in addition can be functionalized in the terminal position with a perfluoroalkyl group or an optionally substituted arly radical. The compound can have antiestrogenic or tissue-selective estrogenic properties and be suitable for the production of pharmaceutical agents.

11&bgr; LONG-CHAIN SUBSTITUTED ESTRATRIENES, METHOD FOR THEIR PRODUCTION, PHARMACEUTICAL PREPARATIONS CONTAINING SAID 11&bgr; LONG-CHAIN SUBSTITUTED ESTATRIENES, AND THEIR USE FOR PRODUCING MEDICAMENTS

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

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 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,

8.alpha.-acylamino ergolines are useful dopamine agonists.

N-(8.alpha.-ergolinyl)-amides

Compounds of formula I and their acid addition salts ##STR1## in which R.sup.2 R.sup.6 R.sup.13 and X have the meanings defined herein are described as well as a process and intermediates for their production, and pharmaceutical agents containing these compounds.

2, 13-disubstituted ergolines, their production and use in

2,14-disubstituted ergolines, their production and use in pharmaceutical

8 beta-substituted ergolines, process for their production and their use

8.alpha.-acylamino ergolines and use as pharmaceutical agents

2-Substituted ergolines ##STR1## wherein C.sub.2  C.sub.3 and C.sub.9  C.sub.10 represent a single of double bond;

2-substituted ergolines

2-Substituted ergolines ##STR1## wherein C.sub.2  C.sub.3 and C.sub.9  C.sub.10 represent a single or double bond;

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Berlin, Germany

Gerhard Sauer