17.alpha.-Pregn-4-ene-3-oxo-21-carboxylic acid esters, process for the preparation thereof, and use thereof as medicinal agents
AssigneeSchering Corporation
InventorsDieter Bittler, Henry Laurent, Klaus Nickisch, Rudolf Weichert, Jorge Casals-Stenzel
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Abstract
17.alpha.-Pregn-4-ene-3-oxo-21-carboxylic acid esters of Formula I ##STR1## wherein C.sub.1 C.sub.2 is a CC single or C.dbd.C double bond, --A--B--is ##STR2## --C--D--is ##STR3## and R is an alkyl or alkenyl residue of up to 6 carbon atoms, in addition to antialdosterone activity, exhibit greatly reduced antiandrogenic and progestational side effects.
Claims21
A 17.alpha.-pregn-4-ene-3-oxo-21-carboxylic acid ester of the formula ##STR8## wherein C.sub.1 C.sub.2 is a CC single or C.dbd.C double bond;
- --A--B-- is ##STR9## --C--D-- is ##STR10## and R is C.sub.1-6 -alkyl or C.sub.2-6 -alkenyl.
A method of achieving an antialdosterone effective in a patient in need of such treatment comprising administering an amount of a compound of the following formula effective as an antialdesterone agent ##STR11## wherein C.sub.1 C.sub.2 is a CC single or C.dbd.C double bond;
- --A'B-- is ##STR12## --C--D-- is ##STR13## and R is C.sub.1-6 -alkyl or C.sub.2-6 -alkenyl.
A method of achieving a diuretic effect in a patient in need of such treatment comprising administering to the patient a diuretically effective amount of a compound of the formula ##STR14## wherein C.sub.1 C.sub.2 is a CC single or C.dbd.C double bond;
- --A--B-- is ##STR15## --C--D-- is ##STR16## and R is C.sub.1-6 -alkyl or C.sub.2-6 -alkenyl.
A 17.alpha.-pregn-4-ene-3-oxo-21-carboxylic acid ester of the formula ##STR17## wherein C.sub.1 C.sub.2 is a CC single or C.dbd.C double bond;
- --A--B-- is ##STR18## --C--D-- is ##STR19## and R is C.sub.1-6 -alkyl or C.sub.2-6 -alkenyl.
A 17.alpha.-pregn-4-ene-3-oxo-21-carboxylic acid ester of the formula ##STR20## wherein C.sub.1 C.sub.2 is a CC single or C.dbd.C double bond;
- --A--B-- is ##STR21## --C--D-- is ##STR22## and R is C.sub.2-6 -alkenyl.
A 17.alpha.-pregn-4-ene-3-oxo-21-carboxylic acid ester of the formula ##STR23## wherein C.sub.1 C.sub.2 is a CC single bond;
- --A--B-- is ##STR24## --C--D-- is ##STR25## and R is C.sub.1-6 -alkyl or C.sub.2-6 -alkenyl.
A 17.alpha.-pregn-4-ene-3-oxo-21-carboxylic acid ester of the formula ##STR26## wherein C.sub.1 C.sub.2 is a CC single bond or a C.dbd.C double bond;
- --A--B-- is ##STR27## --C--D-- is ##STR28## and R is C.sub.1-6 -alkyl or C.sub.2-6 -alkenyl.
A 17.alpha.-pregn-4-ene-3-oxo-21-carboxylic acid ester of the formula ##STR29## wherein C.sub.1 C.sub.2 is a CC single or C.dbd.C double bond;
- --A--B-- is ##STR30## --C--D-- is ##STR31## and R is C.sub.1-6 -alkyl or C.sub.2-6 -alkenyl.
Dependencies are inferred from the claim text.