3-a-norandrostene-1 2-c pyrazoles anti-androgenic

摘要

(A) Cpds. (I) and (II) and (III) where R=H, acyl (claims acyl from following acids (12C); lower alkanoic (opt. substd. by Ph, cycloalkyl and cycloalkenyl (both 3-6C) and alkenoic, PhCO2H, toluic, and cycloalkyl and cycloalkenyl (both 3-6C) acids) R'=H, lower alkyl X=H, or pref. lower alkyl, cycloalkyl, or Ph (opt. substd. by halogen, 1-2 lower alkyl or 1-3 NO2) (B) Salts of (I) and (II) with non-toxic acids. (I) and (II) have anti-androgenic activity, and are useful for the treatment of hyper androgenic acne, for admin. to male swine (to make meat palatable), and for the caponization of male chickens (i.e. without castration). In addn. (I)-(III) are surface active agents, U.V absorbers (may be used as sun screening agents), antioxidants, and corrosion inhibitors.