BENZOTHIOPHENES, FORMULATIONS CONTAINING SAME, AND METHODS

摘要

This invention provides compounds of formula (I) wherein R<1> is hydrogen, hydroxy, C1-C4 alkoxy, -OCOO(C1-C6 alkyl), -OCO(C1-C6 alkyl), -OCOAr wherein Ar is phenyl or optionally substituted phenyl, -OSO2 (C4-C6 straight chain alkyl), or -OSO3H; R<2> is R<1>, C1 or F; with the proviso that at least one of R<1> or R<2> is -OSO3H; R<3> is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; and n is 2 or 3; or a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to 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.