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Claims for Patent: 5,731,342

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Claims 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.
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