摘要 |
<p>The present invention provides pharmaceutically active compounds formula I <CHEM> wherein R<1> is -H, -OH, -O(C1-C4 alkyl), -OCOC6H5, -OCO(C1-C6 alkyl), or -OSO2(C2-C6 alkyl); R<2> is -H, -OH, -O(C1-C4 alkyl), -OCOC6H5, -OCO(C1-C6 alkyl), -OSO2(C2-C6 alkyl), or halo; 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; and or a pharmaceutically acceptable salt thereof. Also provided are compounds of formula II <CHEM> wherein R<1a> is -H or -OR<5> in which R<5> is a hydroxy protecting group. R<2a> is -H, halo, or -OR<6> in which R<6> is a hydroxy protecting group; and R<4> is -OH or -CHO; or a pharmaceutically acceptable salt thereof. Further provided are pharmaceutical compositions of compounds of formula I, and methods of using formula I compounds for, inter alia, alleviating the symptoms of post menopausal syndrome and hormonally-dependent cancer, particularly, breast cancer.</p> |
申请人 |
ELI LILLY AND CO., INDIANAPOLIS, IND., US |
发明人 |
PALKOWITZ, ALAN DAVID, CARMEL, INDIANA 46032, US |