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Claims for Patent: RE39049

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Claims 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): Black; Larry J. (Franklin, IN), Cullinan; George J. (Trafalgar, IN)
Assignee: Eli Lilly and Company (Indianapolis, IN)
Application Number:10/375,341
Patent Claims: 1. A method of inhibiting .Iadd.post-menopausal .Iaddend.bone loss .Iadd.in a postmenopausal woman in need of treatment to prevent or to treat post-menopausal osteoporosis .Iaddend.comprising administering to .[.a human.]. .Iadd.said woman .Iaddend.in need of .Iadd.said .Iaddend.treatment an amount of a compound of Formula I ##STR00011## wherein X is a bond, CH.sub.2, or CH.sub.2CH.sub.2; R and R.sup.1, independently, are hydrogen, hydroxyl, C.sub.1-C.sub.6-alkoxy, C.sub.1-C.sub.6-acyloxy, C.sub.1-C.sub.6-akoxy-C.sub.2-C.sub.6-acyloxy, R.sup.3-substituted aryloxy, R.sup.3-substituted aroyloxy, R.sup.4-substituted carbonyloxy, chloro, or bromo; R.sup.2 is a heterocyclic ring selected from the group consisting of pyrrolidino, piperidino, and hexamethyleneimino; R.sup.3 is C.sub.1-C.sub.3-alkyl, C.sub.1-C.sub.3-alkoxy, hydrogen, or halo; and R.sup.4 is C.sub.1-C.sub.6-alkoxy or aryloxy; or a pharmaceutically acceptable salt thereof, that is effective to inhibit .Iadd.post-menopausal .Iaddend.bone loss in .[.a human.]. .Iadd.said woman.Iaddend..

2. A method of claim 1 wherein the .[.human.]. .Iadd.woman .Iaddend.has been diagnosed as suffering from .Iadd.post-menopausal .Iaddend.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 R.sup.2 is piperidino or pyrrolidino.

8. A method of claim 6 wherein R.sup.2 is piperidino or pyrrolidino.

9. A method of claim 6 wherein R.sup.2 is piperidino.

10. A method of claim 6 wherein R.sup.2 is pyrrolidino.

11. A method of claim 1 wherein R and R.sup.1 are both hydroxyl, C.sub.1-C.sub.6-acyloxy, C.sub.1-C.sub.6-alkoxy-C.sub.2-C.sub.6-acyloxy, R.sup.3-substituted aroyloxy, or R.sup.4-substituted carbonyloxy.

12. A method of claim 11 wherein R and R.sup.1 are both hydroxyl.

13. A method of claim 11 wherein R and R.sup.1 are both C.sub.1-C.sub.6-acyloxy.

14. A method of claim 13 wherein R and R.sup.1 are both n-butanoyloxy, 2,2-dimethylpropanoyloxy, or 3,3-dimethylbutanoyloxy.

15. A method of claim 11 wherein R and R.sup.1 are both R.sup.4-substituted carbonyloxy.

16. A method of claim 15 wherein R and R.sup.1 are both methoxycarbonyloxy or phenyloxycarbonyloxy.

17. A method of claim 11 wherein R and R.sup.1 are both R.sup.3-substituted aroyloxy.

18. A method of claim 17 wherein R and R.sup.1 are both benzoyloxy, methylbenzoyloxy, or naphthoyloxy.

19. A method of claim 8 wherein R and R.sup.1 are both hydroxyl, C.sub.1-C.sub.6-acyloxy, C.sub.1-C.sub.6-alkoxy-C.sub.2-C.sub.6-acyloxy, R.sup.3-substituted aroyloxy, or R.sup.4-substituted carbonyloxy.

20. A method of claim 9 wherein R and R.sup.1 are both hydroxyl.

21. A method of claim 10 wherein R and R.sup.1 are both hyroxyl.

22. A method of claim 8 wherein R and R.sup.1 are both C.sub.1-C.sub.6-acyloxy.

23. A method of claim 22 wherein R and R.sup.1 are both n-butanoyloxy, 2,2-dimethylpropanoyloxy, or 3,3-dimethylbutanoyloxy.

24. A method of claim 8 wherein R and R.sup.1 are both R.sup.4-substituted carbonyloxy.

25. A method of claim 24 wherein R and R.sup.1 are both methoxycarbonyloxy or phenyloxycarbonyloxy.

26. A method of claim 8 wherein R and R.sup.1 are both R.sup.3-substituted aroyloxy.

27. A method of claim 26 wherein R and R.sup.1 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.]. .Iadd.woman .Iaddend.has been diagnosed as suffering from .Iadd.post-menopausal .Iaddend.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.
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