10-(1,2-Propadienyl) steroids as irreversible aromatase inhibitors

摘要

Irreversible aromatase inhibitors are provided having the formulae <IMAGE> I <IMAGE> II wherein represents a single or a double bond; R1 is CH3 or C2H5; R2 is (H) (OR8) or O; R3 is H or C1-3 alkyl; R4 is H or OR8; R5 is H2, O or (H) (C1-3 alkyl); R6 and R7 are each independently H or C1-3 alkyl; and R8 is H or C1-4 alkanoyl. Intermediates useful in preparing the foregoing aromatase inhibitors, methods of using them and a pharmaceutical composition containing them are also provided.