2-Benzyl-3-Arylbenzothiophenes useful for the treatment of post-menopausal syndrome

The present invention provides a compound of formula I wherein- R1 is hydrogen, a hydroxy protecting group, or methyl; R2 and R3 are independently C1-C6 alkyl, or R2 and R3, together with the nitrogen to which they are attached, form a heterocycle selected from the group consisting of pyrrolidino, hexamethyleneimino, morpholino, and piperidino; Z is bromo, chloro, fluoro, hydroxy, a protected hydroxy, or hydrogen; and pharmaceutically acceptable salts and solvates thereof. The present invention further provides pharmaceutical compositions containing compounds of formula I, optionally containing estrogen or progestin, and the use of such compounds alone, or in combination with estrogen or progestin, for alleviating the symptoms of post-menopausal syndrome, particularly osteoporosis, cardiovascular related pathological conditions, and estrogen-dependent cancer. The compounds of the present invention also are useful for inhibiting uterine fibroid disease and endometriosis in women and aortal smooth muscle cell proliferation, particularly restenosis, in humans. Also encompassed are novel intermediates.