N-SUBSTITUTED BENzOYL INDOLES AS ESTROGENIC AGENTS

摘要

The present invention provides compounds of formula (A) wherein R1, R2 and R3 are independently selected from hydrogen, halogen, C1-C6 alkoxy, -CF3, -NO2, cyano, C1-C6 alkyl, trifluoromethyl, -OH or the C1-C12 esters (straight chain or branched) or C1-C12 alkyl ethers thereof, or C1-C6 halogenated ethers, preferably C1-C3 halogenated ethers, including trifluoromthyl ether and trichloromethyl ether; R4 and R5 are independently selected from H or benzyl, the benzyl group being optionally substituted by C1-C6 alkyl, C1-C6 alkoxy, -CF3, or halogen; X is H, C1-C6 alkyl, or CF3; Z is O or S; n is 2 or 3; Y is selected from: a) a moiety of the formula -NR'R' wherein R' is C1-C6 lower alkyl; or b) a moiety selected from the group of (B), (C), (D) or (E); or a pharmaceutically acceptable salt thereof, as well as pharmaceutical formulations and methods of treating or preventing disease states or syndromes which are caused or associated with an estrogen deficiency or an excess of estrogen utilizing these compounds.