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US 4,447,424 AGranted
Steroid derivatives
AssigneeRoussel Uclaf
InventorsJean G. Teutsch, Germain Costerousse, Daniel Philibert, Roger Deraedt
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AssigneeRoussel Uclaf
InventorsJean G. Teutsch, Germain Costerousse, Daniel Philibert, Roger Deraedt
Estimating the term…
Novel 19-nor steroids and 19-nor-D-homo-steroids of the formula ##STR1## wherein R.sub.1 is an organic radical of 1 to 18 carbon atoms containing at least one atom selected from the group consisting of nitrogen, phosphorous and silicon with the atom immediately adjacent to the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is selected from the group consisting of a pentagonal ring and a hexagonal ring optionally substituted and optionally containing a double bond, B and C together form a double bond or an epoxy group, the C.dbd.A group at position 3 is selected from the group consisting of C--O, ketal, which may be open or closed ##STR2## --C.dbd.NOH, --C--NOAlK.sub.3 and C--CH.sub.2, AlK.sub.1, AlK.sub.2 and AlK.sub.3 are selected from the group consisting of alkyl of 1 to 8 carbon atoms and aralkyl of 7 to 15 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having anti-glucocorticoid activity and a process for their preparation.
An antiprogestomimetic composition comprising an anti-progestomimetically effective amount of at least one compound selected from the group consisting of 19-nor steroids and 19-nor-D-homo-steroids of the formula ##STR100## wherein R.sub.1 is an organic radical of 1 to 18 carbon atoms containing at least one atom selected from the group consisting of nitrogen, phosphorous and silicon with the atom immediately adjacent to the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is selected from the group consisting of a pentagonal ring and a hexagonal ring optionally substituted and optionally containing a double bond, B and C together form a double bond or an epoxy group, the ring C.dbd.A group at position 3 is selected from the group consisting of C.dbd.O, ketal, ##STR101## >C.dbd.NOH, >C.dbd.NOAlK.sub.3 and CH.sub.2, AlK.sub.1, ALK.sub.2 and AlK.sub.3 are selected from the group consisting of alkyl of 1 to 8 carbon atoms and aralkyl of 7 to 15 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts and an inert carrier.
A method of inducing menses in warm-blooded animals comprising administering to warm-blooded animals, when progesterone plays a physiologically essential role, an anti-progestomimetically effective amount of at least one compound selected from the group consisting of 19-nor steroids and 19-nor-D-homo-steroids of the formula ##STR108## wherein R.sub.1 is an organic radical of 1 to 18 carbon atoms containing at least one atom selected from the group consisting of nitrogen, phosphorous and silicon with the atom immediately adjacent to the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is selected from the group consisting of a pentagonal ring and a hexagonal ring optionally substituted and optionally containing a double bond, B and C together form a double bond or an epoxy group, the ring C.dbd.A group at position 3 is selected from the group consisting of C.dbd.O, ketal, ##STR109## >C.dbd.NOH, >C.dbd.NOAlK.sub.3 and CH.sub.2, AlK.sub.1, AlK.sub.2 and AlK.sub.3 are selected from the group consisting of alkyl of 1 to 8 carbon atoms and aralkyl of 7 to 15 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts.
Dependencies are inferred from the claim text.