| 摘要 |
The present invention provides a class of substituted indene compounds and their pharmaceutically acceptable salts which possess selective estrogen receptor modulator (SERM) activity and are thus useful in the treatment of osteoporosis and cardiovascular disease, particularly hyperlipidemia in women. The compounds possess the structure in which R1 is hydrogen, hydroxy, alkoxy, phenylcarbonyloxy, alkylcarbonyloxy, or alkylsulfonyloxy. R2 is hydrogen, hydroxy, halo, alkoxy, phenylcarbonyloxy, alkylcarbonyloxy, or alkylsulfonyloxy. R3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexa-methyleneimino, and n is 2 or 3. The dashed line bond between the carbon atoms at positions 1 and 2 of the indene nucleus represent an optional double bond with the proviso that when the double bond is absent, the parenthetic hydroxy group at position 1 is present and vice versa. Certain 2,3-dihydro-1H-indene precursors to the disclosed indene compounds also possess SERM activity and are useful for the same purposes.
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