Novel steroid compounds having an oxygen function in the 19-position
AssigneeCiba-Geigy Corporation
InventorsGeorg Anner, Hellmut Ueberwasser, Michel Biollaz, Peter Wieland
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AssigneeCiba-Geigy Corporation
InventorsGeorg Anner, Hellmut Ueberwasser, Michel Biollaz, Peter Wieland
Estimating the term…
Novel 19-oxygenated steroids of the 20-spiroxane series of the formula ##STR1## in which R.sup.3 is a lower alkyl radical carrying an oxygen-containing functional group and R.sup.4 is two hydrogen atoms or an oxo group, and which carry a double bond or a methylene group in the 6,7-position or carry a lower alkanoylthio group in the 7.alpha.-position, and the corresponding 17.beta.-hydroxy-21-carboxylic acids of the formula ##STR2## in which R.sup.3 is as defined above, and which carry a double bond or a methylene group in the 6,7-position, as well as salts thereof and 1,2-dehydro derivatives of all of these compounds are advantageous as potassium-saving diuretics in therapy since they antagonize the physiological effects of aldosterone but have only slight side effects on sexual functions of the body. The compounds are obtainable by conventional general preparation processes of steroid chemistry.
A 19-oxygenated steroid compound selected from the group consisting of a compound of the spiroxane series of the formula ##STR11## in which R.sup.1 is hydrogen and R.sup.2 is hydrogen or an .alpha.-oriented lower alkanoylthio, or R.sup.1 and R.sup.2 conjointly are a carbon-carbon bond, .alpha.-oriented methylene or .beta.-oriented methylene, R.sup.3 is a radical of the partial formula ##STR12## in which R.sub.a.sup.3 and R.sub.b.sup.3 each individually is hydrogen or lower alkyl, and R.sub.c.sup.3 is hydroxyl, esterified hydroxyl or lower alkoxy, or R.sub.a.sup.3 and R.sub.b.sup.3 conjointly are oxo and R.sub.c.sup.3 is hydrogen, lower alkyl, hydroxyl or lower alkoxy, and R.sup.4 is two hydrogens or oxo, and of a corresponding 17.beta.-hydroxy-21-carboxylic acid of the formula ##STR13## in which R.sup.1 and R.sup.2 each are hydrogen or conjointly are a C-C bond, an .alpha.-oriented methylen or a .beta.-oriented methylene and R.sup.3 is as defined above, and a salt thereof, and of a 1,2-dehydro derivative of any of the compounds of the formulae I and IA.
Dependencies are inferred from the claim text.