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Details for Patent: 4,978,657

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Details for Patent: 4,978,657

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 leat 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, 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## wherein R' and R" are both hydrogen, R.sub.1 contain 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 antiglucocorticoid activity, their preparation and novel intermediates.
Inventor(s): Teutsch; Jean-Georges (Pantin, FR), Torelli; Vesperto (Maison-Alfort, FR), Deraedt; Roger (Pavilons-sous-Bois, FR), Philibert; Daniel (La Varenne-Saint-Hilaire, FR), Costerousse; Germain (Saint-Maurice, FR)
Assignee: Roussel Uclaf (Paris, FR)
Filing Date:Dec 17, 1985
Application Number:06/810,316
Claims:1. A compound selected from the group consisting of 19-nor-steroids of the formula ##STR537## wherein R.sub.1 is an organic group of 1 to 18 carbon atoms containing at least one atom selected from the group consisting of oxygen, sulfur and nitrogen with the atom immediately adjacent the 11-carbon atom being carbon, R.sub.2 is a hydro-carbon 1 to 8 carbon atoms, the A and B rings are selected from the group consisting of ##STR538## R' and R" are individually selected from the group consisting of hydrogen, --CN and alkyl of 1 to 4 carbon atoms, R.sub.a may be in th E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR539## and acyloxy, R'.sub.a and R".sub.a are alkyl of 1 to 4 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts.

2. A compound of claim 1 wherein R.sub.1 is aryl or aralkyl carrying an amino of the formula ##STR540## wherein R.sub.7 and R.sub.8 are alkyl of 1 to 8 carbon atoms or primary, secondary or tertiary alkyl of 1 to 8 carbon atoms containing at least one heteroatom of the group consisting of --O--, --S-- or --N-- with at least one being nitrogen.

3. A compound of claim 1 wherein R.sub.1 is selected from the group consisting of ##STR541##

4. A compound of claim 1 wherein R.sub.1 is ##STR542##

5. A compound of claim 1 wherein R.sub.2 is methyl.

6. A compound of claim 1 wherein the A and B rings are selected from the group consisting of ##STR543##

7. A compound of claim 1 wherein the A and B rings are ##STR544##

8. A compound of claim 1 wherein R.sub.1 is ##STR545## R.sub.2 is methyl and the A and B rings are: ##STR546##

9. An antiprogestomimetic composition comprising an antiprogestomimetically effective amount of at least one compound of claim 1 and an inert carrier.

10. A composition of claim 9 wherein R.sub.1 is ##STR547## R.sub.2 is methyl and the A and B rings are ##STR548##

11. A method of interrupting pregnancy comprising administering to warm-blooded animals an antiprogestomimetically effective amount of the compound of claim 10.

12. A method of inducing menses in warm-blooded animals comprising administering to warm-blooded animals when progesterone plays a physiologically essential role, an antiprogestomimetically effective amount of at least one compound of claim 1.

13. A method of claim 12 comprising administering to women an antiprogestomimetically effective amount of at least one compound of claim 1 during the luteral phase.

14. A method of claim 13 wherein the compound is administered at the end of luteral phase.

15. A method of claim 13 wherein the compound is administered orally or locally.

16. A method of claim 12 wherein the compound is administered orally or locally.

17. A method of claim 12 wherein the compound is administered during 1 to 5 days.

18. A method of interrupting pregnancy comprising administering to warm-blooded animals an antiprogestomimetically effective amount of at least one compound of claim 1.
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