4-Androsten-3-ones and process for the preparation thereof
AssigneeSchering Corporation
InventorsRainer Philippson, Bernhard Krieger, Jorge Casals-Stenzel, Ulrich Kerb, Wolfgang Losert, Klaus Prezewowsky, Rudolf Wiechert, Dieter Bittler
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Abstract
4-Androsten-3-ones of the formula ##STR1## wherein R.sub.1 is hydrogen or the acyl radical of an organic or inorganic acid, R.sub.2 is hydrogen, alkyl, or the acyl radical of an organic or inorganic acid, R.sub.3 is methyl or ethyl, R.sub.4 is hydrogen or methyl, ##STR2## and R.sub.5 is lower alkyl, have diuretic activity.
Claims74
A 4-androsten-3-one of the formula ##STR20## wherein R.sub.3 is methyl or ethyl,
- R.sub.4 is hydrogen or methyl, ##STR21## R.sub.5 is alkyl or up to 5 carbon atoms, or a physiologically acceptable (a) 17.beta.-hydroxy mono ester thereof, or (b) 17.alpha.-(3-hydroxypropyl) mono ester thereof or mono ether thereof, (c) 17.beta.-hydroxy mono ester, 17.alpha.-(3-hydroxypropyl) mono ether thereof, or (d) 17.beta.-hydroxy-17.alpha.-(3-hydroxypropyl) diester thereof.
17.beta.-Hydroxy-17.alpha.-( 3-hydroxysuccinyloxypropyl)-7.alpha.-acetylthio-4-androsten-3-one.
17.beta.-Hydroxy-17.alpha.-(3-hydroxysuccinyloxypropyl)-7.alph a.-acetylthio-4-androsten-3-one potassium salt.
A pharmaceutical composition comprising, in unit dosage form, and in admixture with a pharmaceutically acceptable carrier, a diuretically effective amount per unit dosage of a 4,6-androstadiene-3-one of the formula ##STR22## wherein R.sub.3 is methyl or ethyl, R.sub.4 is hydrogen or methyl, ##STR23## or a physiologically acceptable (a) 17.beta.-hydroxy mono ester thereof, or (b) 17.alpha.-(3-hydroxypropyl) mono ester thereof or mono ether thereof, (c) 17.beta.-hydroxy mono ester, 17.alpha.-(3-hydroxypropyl) mono ether thereof, or (d) 17.beta.-hydroxy-17.alpha.-(3-hydroxypropyl) diester thereof.
Dependencies are inferred from the claim text.