Indene compounds having activity as SERMS

Details Indene compounds having activity as SERMS Indene compounds having activity as SERMS

1998-04-22

1999-11-30

Chang, Ceila

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514212, 514428, 514651, 540609, 546205, 548566, 564347, A61K 31445, A61K 3155, C07D21106, C07D20708

Patent

active

059943700

ABSTRACT:
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 ##STR1## in which R.sup.1 is hydrogen, hydroxy, alkoxy, phenylcarbonyloxy, alkylcarbonyloxy, or alkylsulfonyloxy. R.sup.2 is hydrogen, hydroxy, halo, alkoxy, phenylcarbonyloxy, alkylcarbonyloxy, or alkylsulfonyloxy. R.sup.3 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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