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Details for Patent: 4,634,696

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Details for Patent: 4,634,696

Title: Novel 11 beta-substituted-19-nor-steroids
Abstract:Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 is an organic group of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom immediately adjacent the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is the remainder of a pentagonal or hexagonal ring optionally substituted and optionally containing one unsaturated--bond, the A and B rings are selected from the group consisting of ##STR2## R' and R" are individually selected from the group consisting of hydrogen, --CN and alkyl of 1 to 4 carbon atoms with at least one being other than hydrogen, R.sub.x is selected from the group consisting of hydrogen and OR.sub.e, R.sub.e is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl, R.sub.a may be in the E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR3## and acyloxy, R.sub.a ' and R.sub.a " are alkyl of 1 to 4 carbon atoms or taken together with the nitrogen atom form a heterocycle of 5 to 6 chain members optionally containing another heteroatom with the proviso that when A and B are ##STR4## R.sub.1 contains at least one nitrogen, phosphorus or silicium atom and when A and B are ##STR5## R.sub.1 is not a linear alkyl and their non-toxic, pharmaceutically acceptable acid addition salts having a remarkable antigluococorticoid activity, their preparation and novel intermediates.
Inventor(s): Teutsch; Jean-Georges (Pantin, FR), Torelli; Vesperto (Maisons-Alfort, FR), Deraedt; Roger (Pavillons-sous-Bois, FR), Philibert; Daniel (La Varenne-Saint-Hilaire, FR)
Assignee: Roussel Uclaf (Paris, FR)
Filing Date:Jul 30, 1985
Application Number:06/760,703
Claims:1. A method of treating hormonal irregularities and hormonodependent cancers in warm-blooded animals comprising administering to warm-blooded animals an amount of at least one compound selected from the group consisting of 19-norsteroids of the formula ##STR182## wherein R.sub.1 is an organic group of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom immediately adjacent the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is the remainder of a pentagonal or hexagonal ring optionally substituted and optionally containing one unsaturated bond, the A and B rings are selected from the group consisting of ##STR183## R' and R" are individually selected from the group consisting of hydrogen, --CN and alkyl of 1 to 4 carbon atoms with at least one being other than hydrogen, R.sub.x is selected from the group consisting of hydrogen and OR.sub.e, R.sub.e is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl, R.sub.a may be in the E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR184## and acyloxy, R.sub.a ' and R.sub.a " are alkyl of 1 to 4 carbon atoms or taken together with the nitrogen atom form a heterocycle of 5 to 6 chain members optionally containing another heteroatom with the provisio that when A and B are ##STR185## R.sub.1 contains at least one nitrogen, phosphorus or silicium atom and when A and B are ##STR186## R.sub.1 is not a linear alkyl and their non-toxic, pharmaceutically acceptable acid addition salts sufficient to treat hormonal irregularity and hormonodependent cancers.
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