3-SUBSTITUTED-D-HOMO-1,3,5,(10)-ESTRATRIENE DERIVATIVES

摘要

PURPOSE: Estratriene derivatives of the following formula have a powerful inhibitory effect on estrone sulfatase and are hence useful for the prophylaxis or treatment of diseases caused by estrogens, such as breast cancer, uterine cancer, ovarian cancer, endometriosis, adenomyosis uteri and mayoralty. CONSTITUTION: In the formula, one of A and B represents C=O or CH2 and the other represents O or NH; and R represents -SO2NR(1)R(2) or -PO(OM)2 in which R(1) and R(2) each independently represent a hydrogen atom or a lower alkyl group and M represents a hydrogen atom or an alkali metal; provided that, when one of A and B represents NH, the other represents C=O.