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US 5,843,963 AGranted
Benzothiophene compounds, intermediates, processes, compositions, and methods
AssigneeEli Lilly and Company
InventorsKenneth Lee Hauser, Alan David Palkowitz, Kenneth Jeff Thrasher
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Abstract
The invention provides benzothiophene compounds, of formula I, ##STR1## wherein R1, R2, R3, R4 and n are as defined in the specification, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions, including hyperlipidemia, and other cardiovascular pathologies.
Claims13
A compound of formula I formula I ##STR10## wherein:
- R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOAr, --(CO)OAr, where Ar is phenyl or substituted phenyl, --OCO(C.sub.1 -C.sub.6 alkyl), --O(CO)O(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl);
- R.sup.2 is --H, --Cl, --F, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOAr, --O(CO)OAr, where Ar is phenyl or substituted phenyl, --OCO(C.sub.1 -C.sub.6 alkyl), --O(CO)O(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl);
- R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino;
- R.sup.4 is --H, C.sub.1 -C.sub.5 alkyl, --COAr, --(CO)H, --CO(C.sub.1 -C.sub.6 alkyl), --SO.sub.2 (C.sub.2 -C.sub.6 alkyl), or --SO.sub.2 Ar, where Ar is phenyl or substituted phenyl;
- and
- n is 2 or 3;
- or a pharmaceutically acceptable salt or solvate thereof.
4 more elements
Dependencies are inferred from the claim text.