Schering Aktiengesellschaft

Bayer Schering Pharma Ag

Novo Nordisk D/s

Christa Hegele-Hartung

Rolf Bohlmann

Karl-Heinrich Fritzemeier

Rosemarie Lichtner

Yukishige Nishino

Gerhard Sauer

Hermann Kuenzer

Nikolaus Heinrich

Monika Lessl

Jorg Kroll

Helmut Hofmeister

Dieter Bittler

Martin Schneider

Josef Heindl

Karsten Parczyk

Uwe Kollenkirchen

Rudolf Knauthe

Dirk Kosemund

Alexander Hillisch

Ludwig Zorn

Olaf Peters

Peter Esperling

James R Bull

Hermann Kunzer

Gerd Mueller

Walter Elger

Wolfgang Schwede

Rolf Jautelat

Norbert Schmees

Sven Ring

Jens Hoffmann

Gerd Schubert

Ulrike Fuhrmann

Manfred Lehmann

Thorsten Blume

Werner Boidol

Ulf Boemer

Peter Muhn

Vladimir Patchev

Ina Thieme

Ingo Tornus

Karl Heinrich Fritzemeier

Hiroshi Yamanouchi

Hermann K&uuml;nzer

Karsten Parzcyk

Karl-Heinrich Fritzmeier

Michael Klotzbuecher

The present invention relates to non-steroidal progestins of the general formula (I) wherein or a pharmaceutically acceptable derivative or analogue thereof. These progestins are suitable for selectively modulating progesterone receptor mediated effects in different target tissues, particularly in uterine tissue versus breast tissue. Therefore, the progestins of the present invention, optionally in combination with estrogens, may be used for contraception (in particular in estrogen-free oral contraceptives), hormone replacement therapy and the treatment of gynecological disorders. The present invention furthermore relates to methods for selectively modulating progesterone receptor mediated effects in different target tissues or organs.

Non-steroidal progesting

This invention describes the new 8&#x3b2;-substituted estratrienes of general formula I in which R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, Rand Rhave the meanings that are indicated in the description, and Rmeans a straight-chain or branched-chain, optionally partially or completely halogenated alkyl or alkenyl radical with up to 5 carbon atoms, an ethinyl- or prop-1-inyl radical, as pharmaceutical active ingredients that have in vitro a higher affinity to estrogen receptor preparations of rat prostates than to estrogen receptor preparations of rat uteri and in vivo preferably a preferential action on bone rather than the uterus and/or a pronounced action with respect to stimulation of the expression of 5HT2a-receptors and 5HT2a-transporters, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention also describes the use of these compounds for treatment of estrogen-deficiency-induced diseases and conditions as well as the use of an 8&#x3b2;-substituted estratriene structural part in the total structures of compounds that have a dissociation in favor of their estrogenic action on bones rather than the uterus.

8&#x3b2;-hydrocarbyl-substituted estratrienes for use as selective estrogens

Benzocycloheptenes of formula (I), in which R, Rand Y have the meanings that indicated herein, exhibit selective estrogenic activity on bones and are suitable for the production of pharmaceutical agents, especially for prophylaxis and therapy of osteoporosis: 

Benzocycloheptenes, process for their production, pharmaceutical preparations that contain that latter as well as their use for the production of pharmaceutical agents

The invention describes new compounds as pharmaceutical active ingredients, which have in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo a preferential action on bone rather than the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The new compounds are 16&#x3b1;- and 16&#x3b2;-hydroxy-estra-1,3,5(10)-estratrienes, which carry additional substituents on the steroid skeleton and can have one or more additional double bonds in the B-, C- and/or D-rings.

16-hydroxyestratrienes as selectively active estrogens

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

The present invention relates to steroid compounds of general formula X, which may advantageously be employed to stimulate meiosis in human oocytes, the steroid being specifically characterized by amino nitrogen bonded to Cof the steroid skeleton via a spacer A.

Steroid compounds, use of these compounds for the preparation of meiosis-regulating medicaments and method for the preparation of these compounds

This invention describes the new benzocycloheptenes of general formula Iin which

Benzocycloheptenes, process for their production, pharmaceutical preparations that contain the latter as well as their use for the production of pharmaceutical agents

This invention describes the new 4-fluoroalkyl-2H-benzopyrans of general formula I,in which The new compounds have at their disposal strong antiestrogenic action. In addition, they can have at their disposal estrogenic action that occurs in a tissue-selective manner. They can be used for the production of pharmaceutical agents, especially for the treatment of estrogen-dependent diseases and tumors and pharmaceutical agents for hormone replacement therapy (HRT) as well as for the prevention and treatment of osteoporosis.

4-fluoroalkyl-2h-benzopyrans with anti-estogenic activity

Use of ER&bgr;-selective ligands for regulating fertility and compounds useful therefor

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

Combination preparation of estrogen and anti-estrogen

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 11&bgr;-aryl-substituted 14,17-ethanoestratrienes of general formula (I). The new compounds are selective estrogens whose action occurs in a tissue-selective manner. The estrogenic action occurs in particular on bone, in the cardiovascular system and in the CNS (central nervous system). Only a slight estrogenic action or no estrogenic action occurs in the uterus and in the liver, however. The compounds are suitable for the production of pharmaceutical agents for use in numerous indications (for example for hormone replacement therapy, prevention and treatment of osteoporosis).

11&bgr;-aryl substituted 14,17-ethanoestratriens, method for the production of these compounds and their use in the production of medicaments

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,

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Muelheim a.d. Ruhr, Germany

Christa Hegele-Hartung