| abstract |
The present invention provides a compound of the formula (I) wherein R<SUP>1 </SUP>is -H, -OH, -O(C<SUB>1</SUB>-C<SUB>4 </SUB>alkyl), -OCOC<SUB>6</SUB>H<SUB>5</SUB>, -OCO(C<SUB>1</SUB>-C<SUB>6 </SUB>alkyl), or -OSO<SUB>2</SUB>(C<SUB>2</SUB>-C<SUB>6 </SUB>alkyl); R<SUP>0</SUP>, R<SUP>2 </SUP>and R<SUP>3 </SUP>are each independently -H, -OH, -O(C<SUB>1</SUB>-C<SUB>4 </SUB>alkyl), -OCOC<SUB>6</SUB>H<SUB>5</SUB>, -OCO(C<SUB>1</SUB>-C<SUB>6 </SUB>alkyl), -OSO<SUB>2</SUB>(C<SUB>2</SUB>-C<SUB>6 </SUB>alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; X is -S- or -HC-CH-; G is -O-, -S-, -SO-, SO<SUB>2</SUB>, or -N(R<SUP>5</SUP>)-, wherein R<SUP>5 </SUP>is -H or C<SUB>1</SUB>-C<SUB>4 </SUB>alkyl; and Y is -O-, -S-, -NH-, -NMe-, or -CH<SUB>2</SUB>-, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation, and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen. |