1,3-Oxygenated-8-alpha-oestratrienes for post-menopausal disorders - with vaginotropic, but low uterotrophic activity

摘要

8alpha-Oestratrienes of formula (I) are new, (where X is O or R1 and R3 are H, acyl, (cyclo)-alkyl or a satd. O-contg. heterocyclic gp; R2 is lower alkyl; and R4 is H or opt. unsatd., (substd.) hydrocarbyl). (I) have potent vaginotropic but weak uterotropic properties, and are thus useful in the treatment of post-menopausal disorders caused by oestrogen insufficient. (I) may be administered orally or parentally in doses of 0.1-20 mg (pref. 0.05-5 mg). (I) are along intermediates for other pharmaceutically active steroids.