Claims for Patent: RE39049

Summary for Patent: RE39049

Title:	Methods for inhibiting bone loss
Abstract:	The current invention provides methods and pharmaceutical formulations that are useful for inhibiting the loss of bone. These methods and formulations can be used without the associated adverse effects of estrogen therapy, and thus serve as an effective and acceptable treatment for osteoporosis.
Inventor(s):	Larry J. Black, George J. Cullinan
Assignee:	Eli Lilly and Co
Application Number:	US10/375,341
Patent Claims:	1. A method of inhibiting post-menopausal bone loss in a postmenopausal woman in need of treatment to prevent or to treat post-menopausal osteoporosis comprising administering to a human said woman in need of said treatment an amount of a compound of Formula I wherein X is a bond, CH2, or CH2CH2; R and R1, independently, are hydrogen, hydroxyl, C1-C6-alkoxy, C1-C6-acyloxy, C1-C6-akoxy-C2-C6-acyloxy, R3-substituted aryloxy, R3-substituted aroyloxy, R4-substituted carbonyloxy, chloro, or bromo; R2 is a heterocyclic ring selected from the group consisting of pyrrolidino, piperidino, and hexamethyleneimino; R3 is C1-C3-alkyl, C1-C3-alkoxy, hydrogen, or halo; and R4 is C1-C6-alkoxy or aryloxy; or a pharmaceutically acceptable salt thereof, that is effective to inhibit post-menopausal bone loss in a human said woman. 2. A method of claim 1 wherein the human woman has been diagnosed as suffering from post-menopausal osteoporosis. 3. A method of claim 1 wherein the human is a post-menopausal female. 4. A method of claim 1 wherein the human is a male. 5. A method of claim 1 wherein the compound is administered prophylactically. 6. A method of claim 1 wherein X is a bond. 7. A method of claim 1 wherein R2 is piperidino or pyrrolidino. 8. A method of claim 6 wherein R2 is piperidino or pyrrolidino. 9. A method of claim 6 wherein R2 is piperidino. 10. A method of claim 6 wherein R2 is pyrrolidino. 11. A method of claim 1 wherein R and R1 are both hydroxyl, C1-C6-acyloxy, C1-C6-alkoxy-C2-C6-acyloxy, R3-substituted aroyloxy, or R4-substituted carbonyloxy. 12. A method of claim 11 wherein R and R1 are both hydroxyl. 13. A method of claim 11 wherein R and R1 are both C1-C6-acyloxy. 14. A method of claim 13 wherein R and R1 are both n-butanoyloxy, 2,2-dimethylpropanoyloxy, or 3,3-dimethylbutanoyloxy. 15. A method of claim 11 wherein R and R1 are both R4-substituted carbonyloxy. 16. A method of claim 15 wherein R and R1 are both methoxycarbonyloxy or phenyloxycarbonyloxy. 17. A method of claim 11 wherein R and R1 are both R3-substituted aroyloxy. 18. A method of claim 17 wherein R and R1 are both benzoyloxy, methylbenzoyloxy, or naphthoyloxy. 19. A method of claim 8 wherein R and R1 are both hydroxyl, C1-C6-acyloxy, C1-C6-alkoxy-C2-C6-acyloxy, R3-substituted aroyloxy, or R4-substituted carbonyloxy. 20. A method of claim 9 wherein R and R1 are both hydroxyl. 21. A method of claim 10 wherein R and R1 are both hyroxyl. 22. A method of claim 8 wherein R and R1 are both C1-C6-acyloxy. 23. A method of claim 22 wherein R and R1 are both n-butanoyloxy, 2,2-dimethylpropanoyloxy, or 3,3-dimethylbutanoyloxy. 24. A method of claim 8 wherein R and R1 are both R4-substituted carbonyloxy. 25. A method of claim 24 wherein R and R1 are both methoxycarbonyloxy or phenyloxycarbonyloxy. 26. A method of claim 8 wherein R and R1 are both R3-substituted aroyloxy. 27. A method of claim 26 wherein R and R1 are both benzoyloxy, methylbenzoyloxy, or naphthoyloxy. 28. A method of claim 1 wherein the compound of formula I is administered in an amount of 0.1 to 1000 mg. 29. A method of claim 1 wherein the compound of formula I is administered in an amount of 200 to 600 mg. 30. A method of claim 1 wherein the compound of formula I is administered in an amount of 600 to 1000 mg. 31. A method of claim 20 wherein the human woman has been diagnosed as suffering from post-menopausal osteoporosis. 32. A method of claim 20 wherein the human is a post-menopausal woman. 33. A method of claim 20 wherein the compound is administered prophylactically. 34. A method of claim 1 wherein the administration of a compound of formula I does not significantly affect the primary six target tissues. 35. A method of claim 1 wherein a compound of formula I is administered in combination with estrogen.