Benzo[B]thiophene compounds, intermediates, processes, compositions, and methods

摘要

The invention provides benzoÄbÜthiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia and related cardiovascular pathologies. The benzoÄbÜthiophenes have the following formula: wherein: X is -CH2-, -CH(OH)-, or -CO-; R<1> is -H, -OH, -O(C1-C4 alkyl), -OCOAr where Ar is phenyl or substituted phenyl, -OCO(C1-C6 alkyl), or -OSO2(C4-C6 alkyl); R<2>, R<3>, and R<4> are, independently, -R<1>, -F, -Cl, C1-C4 alkyl, or -CF3, with the proviso that R<3> and R<4> are not both hydrogen unless R<2> is CF3, and with the further proviso that when X is -CH2-, then R<3> is -H, -Cl, -F, C1-C4 alkyl, or CF3; n is 2 or 3; and R<5> is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; or a pharmaceutically acceptable salt or solvate thereof.