11.beta.-arylestradienes, their production, and pharmaceutical preparations containing same
AssigneeSchering Corporation
InventorsRalph Rohde, Klaus Annen, Gunter Neef, Rudolf Wiechert, Sybille Beier, Walter Elger, David Henderson
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Abstract
11.beta.-Arylestradienes of general Formula I are disclosed ##STR1## wherein R.sup.2 is a hydrogen atom, a methyl group, or an ethyl group, R.sup.3 is a hydrogen atom or an acyl group, R.sup.1 and A-B have various meanings, which possess antigestagen and antimineralocorticoid activity.
Claims40
An 11.beta.-arylestradiene of the formula ##STR25## wherein R.sup.1 is hydrogen, ##STR26## wherein R.sup.I and R.sup.II each independently is hydrogen, alkyl of 1-4 carbon atoms, or alkanoyl of 1-8 carbon atoms, or R.sup.I and R.sup.II together with the connecting N-atom form a 5- or 6-membered saturated ring, the remaining atoms all being C-atoms or one being another N-atom or an O or S atom, a pyrrole ring being optionally substituted by 1-4 methyl groups;
- a corresponding N-oxide ##STR27## --OR.sup.III, wherein R.sup.III is hydrogen, methyl, ethyl, propyl, methoxyphenyl, allyl, or dimethylaminoethyl,
- --SR.sup.IV, wherein R.sup.IV is hydrogen, methyl, ethyl, propyl, or dimethylaminoethyl, or
- --SiR.sub.3.sup.V, wherein R.sup.V is methyl, ethyl, propyl, butyl, or benzyl,
- R.sup.2 is a hydrogen atom, a methyl group, or an ethyl group,
- R.sup.3 is a hydrogen atom or an alkanoyl group of 1-8 carbon atoms, and ##STR28## wherein R.sup.4 and R.sup.6 each mean alkyl of 1-4 carbon atoms in the .alpha.- or .beta.-position, and R.sup.5 and R.sup.7 each mean C.sub.1-4 -alkylidene in the E- or Z-configuration, and
- the C.sub.20 /C.sub.21 -double bond has a Z- or E-configuration, or a pharmacologically acceptable acid addition salt thereof when the compound is basic.
An intermediate compound of the Formula III ##STR40## wherein R.sup.1 is a hydrogen atom, ##STR41## with R.sup.I and R.sup.II meaning hydrogen, alkyl of 1-4 carbon atoms, or acyl of 1-8 carbon atoms, or R.sup.I and R.sup.II with inclusion of N meaning a 5- or 6-membered ring wherein, besides N, still another hetero atom, such as O, N, S can be contained in the ring, as well as the corresponding N-oxides and acid addition salts, or R.sup.I and R.sup.II with inclusion of N meaning a pyrrole ring optionally substituted by methyl,
- --OR.sup.III with R.sup.III meaning hydrogen, methyl, ethyl, propyl, methoxyphenyl, allyl, or dimethylaminoethyl,
- --SR.sup.IV with R.sup.IV meaning hydrogen, methyl, ethyl, propyl, or dimethylaminoethyl, and
- --SiR.sub.3.sup.V with R.sup.V meaning methyl, ethyl, propyl, butyl, or benzyl,
- R.sup.2 is hydrogen atom, a methyl group, or an ethyl group, and ##STR42## wherein R.sup.4 and R.sup.6 each mean alkyl of 1-4 carbon atoms ln the .alpha.- or .beta.-position, and R.sup.5 and R.sup.7 each mean an alkylidene group in the E- or Z-configuration, and the C.sub.20 /C.sub.21 -double bond has a Z- or E-configuration.
Dependencies are inferred from the claim text.