1-Aryloxy-2-arylnaphthyl compounds, intermediates, compositions, and methods

摘要

The present invention provides a class of compounds having the structure <CHEM> or a pharmaceutically acceptable salt where R<1> is hydrogen, hydroxy, alkoxy, alkoxycarbonyl, alkoxycarbonyloxy, aryloxycarbonyl, phenoxycarbonyloxy, or alkylsulfonyloxy; R<2> and R<3> are independently selected from hydrogen, halo, hydroxy, alkoxy, alkoxycarbonyl, alkoxycarbonyloxy, aryloxycarbonyl, phenoxycarbonyloxy, or alkylsulfonyloxy; R<4> is selected from hydroxy, alkoxy, cycloalklxy, 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, 1-hexamethyleneimino, and-OAr where where Ar is unsubstituted or substituted phenyl; X is selected from the group consisting of alkylene of two to four carbon atoms, -CH=CH-, -CH2CH=CH-, and -CH2CH2CH=CH-; and Y is absent or is carbonyl, with the proviso that when Y is absent, R<4> may not be hydroxy, alkoxy, cycloalkoxy or aryloxy. The compounds are selective estrogen receptor modulators (SERMÕs) and are useful in the treatment of pathological conditions associated with estrogen deprivation or the abnormal response to endogenous estrogen.