abstract |
The present invention provides compounds with nitrogen,nsulfur or carbon linked basic side chains of formulan nwhere R 1 and R 2 are independently hydrogen, halo, hydroxy,nalkoxy, alkylcarbonyloxy, alkoxycarbonyl, alkoxycarbonyloxy,narylcarbonyloxy, aryloxycarbonyloxy, or alkylsulfonyloxy; O-SO 2 -(C 4 -C 6 nalkyl), chloro, fluoro, or bromo; W is CHOH,nC(O), or CH 2 ; Y is -CH 2 -, -NH-, -NMe-, -S-, -SO 2 -; and R 3 nand R 4 are independently hydrogen, alkyl, alkylcarbonyl,nalkylamino-carbonyl, or arylcarbonyl, or together with thennitrogen to which they are attached form 1-pyrrolidinyl, 1-piperidinyl,nor a 5- or 6-membered imide or cyclic amidenring. n The present invention also provides pharmaceuticalncompositions containing the compounds optionally containingnestrogen or progestin, and the use of such compounds, alone,nor in combination with estrogen or progestin, for treatingnosteoporosis, aortal smooth muscle cell proliferation,n(particularly restenosis), and estrogen-dependent cancern(particularly breast cancer). |