Benzothiophene compounds, compositions, and method
AssigneeEli Lilly and Company
InventorsGeorge Joseph Cullinan, Brian Stephen Muehl
Life of this patent
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Abstract
The invention provides benzothiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia, and estrogen-dependent cancer.
Claims6
A method of inhibiting bone loss or bone resorption which comprises administering to a patient in need thereof an effective amount of a compound of formula I:
- ##STR15## wherein:
- R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.6 alkyl), --O(CO)O(C.sub.1 -C.sub.6 alkyl), --OCOAr, --O(CO)OAr, where Ar is phenyl or optionally substituted phenyl, or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl);
- R.sup.2 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.6 alkyl), --O(CO)O(C.sub.1 -C.sub.6 alkyl), --OCOAr, --O(CO)OAr, where Ar is phenyl or optionally substituted phenyl, --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl), --Cl, or --F;
- R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;
- and
- n is 2, 3, or 4;
- or a pharmaceutically acceptable salt or solvate thereof.
A method of lowering serum cholesterol levels which comprises administering to a patient in need thereof an effective amount of a compound of formula I:
- ##STR16## wherein:
- R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.6 alkyl), --O(CO)O(C.sub.1 -C.sub.6 alkyl), --OCOAr, --O(CO)OAr, where Ar is phenyl or optionally substituted phenyl, or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl);
- R.sup.2 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.6 alkyl), --O(CO)O(C.sub.1 -C.sub.6 alkyl), --OCOAr, --O(CO)OAr, where Ar is phenyl or optionally substituted phenyl, --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl), --Cl, or --F;
- R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;
- and
- n is 2, 3, or 4;
- or a pharmaceutically acceptable salt or solvate thereof.
A method of inhibiting estrogen-dependent cancer which comprises administering to a patient in need thereof an effective amount of a compound of formula I:
- ##STR17## wherein:
- R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.6 alkyl), --O(CO)O(C.sub.1 -C.sub.6 alkyl), --OCOAr, --O(CO)OAr, where Ar is phenyl or optionally substituted phenyl, or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl);
- R.sup.2 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.6 alkyl), --O(CO)O(C.sub.1 -C.sub.6 alkyl), --OCOAr, --O(CO)OAr, where Ar is phenyl or optionally substituted phenyl, --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl), --Cl, or --F;
- R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;
- and
- n is 2, 3, or 4;
- or a pharmaceutically acceptable salt or solvate thereof.
Dependencies are inferred from the claim text.