IRREVERSIBLE INHIBITORS OF 17β-HSD1

Abstract

Novel compounds of formula (I), as well as pharmaceutical compositions and kits containing them. In said formula, A¹ is C(O) or CHRz¹ and A² is CH2 or O. R¹ is selected from hydrogen, (C1-C5) alkyl, (C1-C5) alkoxy, (C2-C5) alkenyl or (C2-C5) alkynyl —all optionally substituted by one or more Z groups—, (C3-C8) cycloalkyl, aryl or heteroaryl. R² is a 5-, 6- or 7-membered aromatic heterocyclic ring containing at least one heteroatom selected from N, S or O, the remainder being CRz², N, S or O. R³ is (C1-C5) alkyl substituted by one or more atoms of Br (including Br76) or I (including I¹²³, I¹²4 or I¹³¹). The myn indices are integers from 0 to 2, and yp is an integer from 0 to 5. These compounds act as inhibitors with improved inhibitory activity and greater metabolic stability compared to known inhibitors.