Novel 11.beta.-substituted -19-nor-steriods

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai

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514178, 514179, 552505, 552508, 552515, A61K 3156, A61K 3158, C07S 5300

Patent

active

050433326

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, 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 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 antiglucocorticoid activity, their preparation and novel intermediates.

REFERENCES:
patent: 4701499 (1987-10-01), Torelli et al.
patent: 4891365 (1990-01-01), Wiechert et al.
patent: 4891368 (1990-01-01), Chwalisz et al.

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