Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1987-02-24
1991-01-22
Berch, Mark L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
514173, 514176, 514178, 540 15, 540 28, 540 29, 540 30, 540 41, 540 44, 552508, 552523, 552553, 552597, 552598, A61K 3158, A61K 31585, C07J 4300, C07J 3300
Patent
active
049871285
ABSTRACT:
Novel 10.beta.-alkynyl-steroids of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, optionally substituted alkyl and alkoxy of 1 to 8 carbon atoms, optionally substituted alkenyl and alkynyl of 2 to 8 carbon atoms, optionally substituted aryl and aralkyl, optionally esterified carboxy, dialkylamino with alkyl of 1 to 6 carbon atoms, halogen and trialkylsilyl of 1 to 7 alkyl carbon atoms, R.sub.6 and R.sub.7 taken together with the carbon atoms to which they are attached form cyclopropyl or R.sub.6 is hydrogen and R.sub.7 is R.sub.1, R.sub.1 is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms, optionally substituted alkenyl and alkynyl of 2 to 6 carbon atoms and acetylthio, R.sub.2 is methyl or ethyl, X and Y taken together form a member selected from the group consisting of ##STR2## Alk is alkyl of 1 to 8 carbon atoms or X is hydroxy and Y is ##STR3## or X is optionally acylated or etherified hydroxy and Y is selected from the group consisting of --CH.sub.2 --CH.sub.2 --CH.sub.2 --OH, hydrogen, R.sub.4, and --CH.sub.2 --CH.sub.2 --COOM, M is selected from the group consisting of hydrogen, --NH.sub.4 and alkali metal and R.sub.4 is selected from the group consisting of alkyl of 1 to 6 carbon atoms and alkenyl and alkynyl of 2 to 6 carbon atoms, the dotted lines indicate the optional presence of a second carbon-carbon bond when R.sub.6 and R.sub.7 and the carbon to which they are attached do not form cyclopropyl and the wavy lines indicate that R.sub.6 and R.sub.7 may be in the .alpha. or .beta. position with the proviso that R is not hydrogen when R.sub.6 and R.sub.7 are hydrogen, R.sub.2 is methyl, X is optionally acylated or etherified hydroxy, Y is hydrogen or R.sub.4 and the dotted lines are not a second carbon-carbon bond having aldosterone antagonistic activity and increased hydrosodic diuresis with organic potassium conservation with little secondary hormone effects.
REFERENCES:
patent: 3218316 (1916-11-01), Edwards
patent: 4464302 (1984-08-01), Nedelec
patent: 4701449 (1987-10-01), Torelli et al.
Aries, Chem. Abs., 84, 79726g.
Marcolte, Steroids, 39, 2924, (1982).
Moura Anne-Marie
Nedelec Lucien
Nique Francois
Berch Mark L.
Roussel Uclaf
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