NAPHTHYL COMPOUNDS, INTERMEDIATES, COMPOSITIONS, AND METHODS

摘要

The present invention provides pharmaceutically active compounds formula I I wherein R1 is -H, -OH, -O(C1-C4 alkyl), -ococ6H5, -OCO(C1-C6 alkyl), or -OSO2(C2-C6 alkyl); R2 is -H, -OH, -O(C1-C4 alkyl), -OCOC6H5, -OCO(C1-C6 alkyl), -OSO2(C2-C6 alkyl), or halo; R3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1hexamethyleneimino; and n is 2 or 3; and or a pharmaceutically acceptable salt thereof. Also provided are compounds of formula wherein R1a is -H or -OR5 in which R5 is a hydroxy protecting group. R2a is -H, halo, or -OR6 in which R6 is a hydroxy protecting group; and R4 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.