| 摘要 |
The present invention provides compounds with nitrogen, sulfur or carbon linked basic side chains of formula (see fig. I) where R1 and R2 are independently hydrogen, halo, hydroxy, alkoxy, alkylcarbonyloxy, alkoxycarbonyl, alkoxycarbonyloxy, arylcarbonyloxy, aryloxycarbonyloxy, or alkylsulfonyloxy; O-SO2-(C4-C6 alkyl), chloro, fluoro, or bromo; W is CHOH, C(O), or CH2; Y is -CH2-, -NH-, -NMe-, -S-, -SO2-; and R3 and R4 are independently hydrogen, alkyl, alkylcarbonyl, alkylamino-carbonyl, or arylcarbonyl, or together with the nitrogen to which they are attached form 1-pyrrolidinyl, 1-piperidinyl, or a 5- or 6-membered imide or cyclic amide ring. The present invention also provides pharmaceutical compositions containing the compounds optionally containing estrogen or progestin, and the use of such compounds, alone, or in combination with estrogen or progestin, for treating osteoporosis, aortal smooth muscle cell proliferation, (particularly restenosis), and estrogen-dependent cancer (particularly breast cancer).
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