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):	George Joseph Cullinan, Alan David Palkowitz
Assignee:	Eli Lilly and Co
Application Number:	US08/787,041
Patent Claims:	1. A compound of formula I ##STR7## wherein R1 is hydrogen, hydroxy, C1 -C4 alkoxy, ##STR8## wherein Ar is optionally substituted phenyl, or --SO2 (C4 -C6 straight chain alkyl);R2 is R1, Cl or F; and R3 and R4 are, independently, C1 -C4 alkyl or combine to form a C4 -C6 polymethylene or, together with the nitrogen to which they are attached form morpholine, X is --CH2, --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)ethoxy!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)!benzo 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)!benzo 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)ethoxy!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)ethoxy!phenyl!methanone-N-oxide.