| abstract |
Cpds. of formula (I) are new: alkylenedioxy 16alpha, 17alpha or 16Beta, 17Beta; R1 and R3 = H3, acyl, alkyl, cycloalkyl, or satd. O-contg. heterocyclyl; R2 = lower alkyl; R4 = H or opt. unsatd. or substd. hydrocarbyl; R5 and R6 = H, lower alkyl, aralkyl or opt. substd. phenyl). Prepn. is basically by oxidising corresp. (17-acyloxy)-DELTA16- cpds. opt. followed by convention acylations etc. (I) have strong vaginotropic but weak uterotropic activity useful for treating oestrogen insufficiency e.g. menopausal disorders. Pref. dose is 0.03-5 mg/day. |