Schering Aktiengesellschaft

James R Bull

Walter Elger

Rudolf Wiechert

Henry Laurent

Karl-Heinrich Fritzemeier

Gunter Neef

Sybille Beier

Gerald Kirsch

Christa Hegele-Hartung

Krzysztof Chwalisz

Peter Esperling

Rolf Krattenmacher

Karl-Heinrich Fritzmeier

Helmut Schroeder

Russell I Thomson

New 15,15-dialkyl-substituted derivatives of the estradiol of general formula I ##STR1## in which R.sup.1 and R.sup.2, independently of one another, are each a hydrogen atom or a straight-chain alkanoyl group with 1 to 10 carbon atoms, a branched-chain alkanoyl group with 3-10 carbon atoms, an alkanoyl group of 3-10 carbon atoms containing a cycloaliphatic structure of 3-6 carbon ring atoms or a benzoyl group, and R.sup.3 and R.sup.4, independently of one another, are each a straight-chain alkyl group with 1 to 10 carbon atoms or a branched-chain alkyl group with 3 to 10 carbon atoms, are described, a process for their production and initial products for this process. The new compounds have--also after oral administration--high estrogenic effectiveness and are suitable for the production of pharmaceutical agents.

15,15-dialkyl-substituted derivatives of estradiol

New 15,15-dialkyl-substituted derivatives of the estradiol of general formula I ##STR1## in which R.sup.1 and R.sup.2, independently of one another, are each a hydrogen atom or a straight-chain alkanoyl group with 1 to 10 carbon atoms, a branched-chain alkanoyl group with 3-10 carbon atoms, an alkanoyl group of 3-10 carbon atoms containing a cycloaliphatic structure of 3-6 carbon ring atoms or a benzoyl group, and

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

14.alpha.17.alpha.-(Propano-and 17.sup.2 propeno) -estratrienes

14,16.beta.-ethano-15.beta., 16(1)-cyclo-14.beta.-estra-1,3,5(10)-trienes

##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

14,17.beta.-ethano-14.beta.-estratriene and estratetraene of Formula I ##STR1## wherein R.sup.1 is a hydrogen atom, a methyl or an acyl group of a monocarboxyclic acid of 1-12 carbon atoms,

14,17.beta.-ethano-14.beta.-estratrienes and estratetraenes, process for

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Cape Town, South Africa

James R Bull