Claims for Patent: 5,731,342

Summary for Patent: 5,731,342

Title:	Benzothiophenes, formulations containing same, and methods
Abstract:	This invention provides novel benzothiophene compounds.
Inventor(s):	Cullinan; George Joseph (Trafalgar, IN), Palkowitz; Alan David (Carmel, IN)
Assignee:	Eli Lilly and Company (Indianapolis, IN)
Application Number:	08/787,041
Patent Claims:	1. A compound of formula I ##STR7## wherein R.sup.1 is hydrogen, hydroxy, C.sub.1 -C.sub.4 alkoxy, ##STR8## wherein Ar is optionally substituted phenyl, or --SO.sub.2 (C.sub.4 -C.sub.6 straight chain alkyl); R.sup.2 is R.sup.1, Cl or F; and R.sup.3 and R.sup.4 are, independently, C.sub.1 -C.sub.4 alkyl or combine to form a C.sub.4 -C.sub.6 polymethylene or, together with the nitrogen to which they are attached form morpholine, X is --CH.sub.2, --CHOH--, --O--, or ##STR9## or a pharmaceutically acceptable salt or solvate thereof. 2. A compound according to claim 1 wherein said compound is [2-(4-hydroxyphenyl)-6-hydroxybenzo[b]thien-3-yl][4-[2-(1-piperidinyl)etho xy]phenyl]methanone-N-oxide. 3. A compound according to claim 2 wherein said compound is the hydrochloride salt thereof. 4. A compound according to claim 1 wherein said compound is [6-hydroxy-3-[4-[2-(1-piperidinyl)ethoxy]phenoxy]-2-(4-methoxyphenyl)]benz o[b]thiophene-N-oxide. 5. A compound according to claim 1 wherein said compound is [6-hydroxy-3-[4-[2-(1-piperidinyl)ethoxy]phenoxy]-2-(4-hydroxyphenyl)]benz o[b]thiophene-N-oxide. 6. A compound according to claim 4 wherein said compound is the hydrochloride salt thereof. 7. A method for inhibiting osteoporosis which comprises, administering to patient in need thereof an effective amount of a compound of claim 1. 8. A method for lowering serum cholesterol levels which comprises administering to a patient in need thereof an effective amount of a compound of claim 1. 9. A method for inhibiting estrogen-dependent cancer comprising administering to a patient in need thereof an effective amount of a compound of claim 1. 10. A formulation comprising a compound of formula I of claim 1 and, optionially, pharmaceutically acceptable carriers, diluents, or excipients therefor. 11. A pharmaceutical formulation comprising a compound of formula I of claim 1 and further comprising [2-(4-hydroxyphenyl)-6-hydroxybenzo[b]thien-3-yl][4-[2-(1-piperidinyl)etho xy]phenyl]methanone hydrochloride and, optionally, pharmaceutically acceptable carriers, diluents, or excipients therefor. 12. A formulation according to claim 11 wherein the formula I compound comprises less than 10% by weight of the total active ingredients. 13. A formulation according to claim 12 wherein the formula I compound comprises less than 1% by weight of the total active ingredients. 14. A formulation according to claim 13 wherein the formula I compound comprises less than 0.3% by weight of the total active ingredients. 15. A formulation according to claim 11 wherein said formula I compound is [2-(4-hydroxyphenyl)-6-hydroxybenzo[b]thien-3-yl][4-[2-(1-piperidinyl)etho xy]phenyl]methanone-N-oxide.