abstract |
The present invention provides compounds with nitrogen-containing non-basic side chains of formula II <IMAGE> II wherein R1 and R2, independently, are H, OH, O(C1-C6 alkyl), O-C(O)-(C1-C6 alkyl), O-C(O)-O(C1-C6 alkyl), O-C(O)-Ar, O-C(O)-O-Ar, O-SO2-(C4-C6 alkyl), chloro, fluoro, or bromo; W is CHOH, C(O), or CH2; Y is (CH2)n, or CH(C1-C4 alkyl); V is S, 0, or CH2CH2; n is 1, 2, or 3; and Ar is optionally substituted phenyl. The present invention also provides pharmaceutical compositions containing compounds of formula II, 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 symptoms, particularly osteoporosis, cardiovascular related pathological conditions, and estrogen-dependent cancer. The present invention further provides the use of the compounds of the present invention for inhibiting uterine fibroid disease and endometriosis in women and aortal smooth muscle cell proliferation, particularly restenosis, in humans. |