Schering Aktiengesellschaft

Sybille Beier

Walter Elger

Rudolf Wiechert

Gunter Neef

Eckhard Ottow

David A Henderson

Henry Laurent

Krzysztof Chwalisz

Guenter Neef

Klaus Annen

Ralph Rohde

Stefan Scholz

Helmut Hofmeister

Dieter Bittler

Cornelius Scheidges

Gerhard Sauer

Arwed Cleve

Yukishige Nishino

Gerald Kirsch

Marianne Fahnrich

James R Bull

Syed Hamiduddin Hasan

Beate Kosub

Klaus Nickisch

Ulrich Kerb

Karl-Heinrich Fritzemeier

Wolfgang Losert

Peter Esperling

Harald Von Keyserlingk

Frank Dahlke

Klaus Nickish

Krzsysztof Chwalisz

Juergen Bardenhagen

Angelika Esch

Eckard Otto

Marianne Faehnrich

Gordon Oliver Potts

Krsysztof Chwalisz

The invention relates to the use of esters of estriol, for example, an estriol 3,17-dipropionate or an estriol 3,17-dihexanoate, for the treatment of autoimmune diseases, such as multiple sclerosis (MS).

Use of biogenic estriol diester prodrugs for the treatment of autoimmune diseases

Compounds of formula I ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the meanings indicated in the description, are described, as well as processes for their production, pharmaceutical preparations containing these compounds as well as their use for treatment of diseases. The compounds have antigestagenic, antiglucocorticoid, antimineralocorticoid and antiandrogenic properties.

11.beta.-aryl-4-estrenes, process for their production as well as their

A pharmaceutical agent contains a progesterone synthesis inhibitor (ProI) of the trilostane or epostane type and an antigestagen (AG). It can be used for inducing delivery at term in humans and animals, for terminating normal or pathological pregnancies therein or for treatment of hormone-dependent tumors, endometriosis or dysmenorrhea.

Combined use of an antigestagen and a progesterone synthesis inhibitor

Antigestagens inhibit prostaglandin synthesis by the uterus and thus can be used to treat symptoms of dysmennhorea.

Antigestagens for the inhibition of uterine synthesis of prostaglandin

A method of inducing an antigestagenic effect by the administration of compounds of formula I: ##STR1## wherein, substituents are as defined in the specification.

Dihydrospirorenone, ##STR1## preferably together with an estrogen, can be used for the production of a pharmaceutical agent suitable for treatment of hormonal irregularities during premenopause (menstruation stabilization), for hormonal substitution therapy during menopause, for treatment of androgen-induced disorders and/or for contraception.

Dihydrospirorenone as an antiandrogen

A 14.alpha.,17.alpha.-bridged estratriene of formula I ##STR1## wherein (a) OR.sup.3 is in .alpha.-position

14.alpha., 17.alpha.-ethano-16.alpha.-hydroxy-estratrienes

There are provided 13-alkyl-11beta-phenyl-gonanes of formula I ##STR1## wherein Z is an oxygen atom or N--OH;

13-alkyl-11beta-phenylgonanes

A process of cyclizing compounds of formula II ##STR1## wherein K, V', R.sup.1 and 1 are as herein defined, is described whereby a compound of formula IVa is produced ##STR2## wherein K, V', R.sup.1, Q, S and 1 are as herein defined. The compounds of formula IVa are useful intermediates in the production of compounds of formula I ##STR3## wherein ring A, B, G, V, Z, R.sup.1 and R.sup.2 are as herein defined.

Process for preparing 19,11.beta.-bridged steroids

13-alkyl-11.beta.-phenylgonanes

11.beta.-phenyl-14.beta.H steroids

9.alpha.-hydroxy-19,11.beta.-bridged steroids, their production and

##STR1## New 14.alpha.,17.alpha.-ethano-estratrienes of general formula (I) wherein R.sup.1 is a hydrogen atom, an alkyl or acyl group with 1 to 12 carbon atoms, R.sup.2 is a hydrogen atom or a methyl group, R.sup.3 is a hydrogen atom or an acyl group with 1 to 12 carbon atoms and (a) is either (II) or (III), where R.sup.4 is an alkyl residue in the .alpha. or .beta. position with 1 to 8 carbon atoms or an .alpha.,.beta.-alkenyl residue which may contain several double bonds or an .alpha.,.beta.-alkinyl residue, both with 2 to 8 carbon atoms, are described. Also described is a process for producing them. These new compounds have a marked oestrogenic activity.

14.alpha.,17.alpha.-ethanoestratrienes

11.beta.-phenyl-4,9,15-estratrienes, their manufacture and

New 19,11.beta.-bridged steroids of the general formula I ##STR1## where R.sup.1 stands for a methyl or ethyl radical,

19,11 .beta.-bridged steroids, their manufacture and pharmaceutical

Growing community of inventors

Berlin, Germany

Sybille Beier