Therapeutic regimens

• US 9,555,014 B2
• Filed: 05/19/2014
• Issued: 01/31/2017
• Est. Priority Date: 05/12/2010
• Status: Active Grant

• Current Assignee: Radius Health, Inc.
• Original Assignee: Radius Health, Inc.
• Inventors: O'Dea, Louis, Lyttle, C. Richard, Guerriero, Jonathan
• Primary Examiner(s): TRAN, MY CHAU T
• Application Number:
  US14/281,475
• Publication Number:
  US 20160022608A1
• Time in Patent Office: 988 Days
• Field of Search: 514/546, 514/647, 514/648, 514/649, 514/650
• US Class Current: 1/1
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 9/485 Inorganic compounds
• CPC Class Codes: A61K 9/4866 Organic macromolecular compounds
• CPC Class Codes: A61P 15/12 for climacteric disorders
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 5/00 Drugs for disorders of the endocrine system
• CPC Class Codes: A61P 5/24 of the sex hormones

Abstract

This invention relates to clinically useful therapeutic regimens comprising the administration of (R)-6-(2-(ethyl(4-(2-(ethylamino)ethyl)benzyl)amino)-4-methoxyphenyl)-5,6,7,8-tetrahydronaphthalen-2-ol.

Claims

1. A unit dosage form suitable for once daily administration to a human subject in need thereof comprising 0.9 mg to 1.1 mg, 2.2 mg to 2.8 mg, 4.4 mg to 5.6 mg, or 9 mg to 11 mg of the compound of formula I as its dihydrochloride salt

2. The unit dosage form according to claim 1, further comprising one or more pharmaceutically acceptable excipients.

3. The unit dosage form according to claim 2, wherein the unit dosage form is a tablet or capsule suitable for oral administration.

28. The unit dosage form according to claim 1, wherein the unit dosage form comprises 1 mg, 2.5 mg, 5 mg, or 10 mg of the compound of Formula I or a salt thereof.

4. A unit dosage form comprising 0.9 mg to 1.1 mg, 2.2 mg to 2.8 mg, 4.4 mg to 5.6 mg, or 9 mg to 11 mg of the compound of formula I or a salt thereof

5. The unit dosage form according to claim 4, wherein the unit dosage form is not coated with an acid resistant coating.

29. The unit dosage form according to claim 4, further comprising one or more pharmaceutically acceptable excipients.

30. The unit dosage form according to claim 29, wherein the unit dosage form is a tablet or capsule suitable for oral administration.

31. The unit dosage form according to claim 4, wherein the unit dosage form comprises 1 mg, 2.5 mg, 5 mg, or 10 mg of the compound of Formula I or a salt thereof.

32. The unit dosage form according to claim 4, wherein the unit dosage form comprises an acid addition salt of the compound of Formula I.

33. The unit dosage form according to claim 32, wherein the unit dosage form comprises a dihydrochloride salt of the compound of Formula I.

6. A method of treating vasomotor disturbances in a peri-menopausal or postmenopausal woman in need thereof comprising administering to the woman a composition comprising a compound of formula I or a salt thereof

7. The method according to claim 6, wherein the composition is administered orally, once-daily.

8. The method according to claim 7, wherein the composition is a tablet or capsule suitable for oral administration.

9. The method according to claim 8, wherein the composition is more than 50% dissolved in the stomach prior to being released into the small intestines.

10. The method according to claim 9, wherein the composition is not coated with an acid resistant coating.

34. The method according to claim 6, wherein the daily total dosage of the compound of Formula I or a salt thereof is 1 mg, 2.5 mg, 5 mg, or 10 mg.

35. The method according to claim 6, wherein the composition comprises an acid addition salt of the compound of Formula I.

36. The method according to claim 35, wherein the composition comprises a dihydrochloride salt of the compound of Formula I.

11. A method of treating vasomotor disturbances in a peri-menopausal or postmenopausal woman in need thereof comprising administering to the woman a compound of formula I or a salt thereof

12. The method of claim 11, wherein a steady state trough level of the compound of formula I ranging from 0.11 ng/mL to 0.79 ng/mL or ranging from 0.12 ng/mL to 0.86 ng/mL is achieved.

13. The method of claim 11, wherein the compound of formula I is in the form of a dihydrochloride salt.

14. The method of claim 13, wherein the compound of formula I or a salt thereof is orally administered once-daily.

15. The method of claim 14, wherein the compound is in a unit dosage form.

16. The method of claim 15, wherein the compound is administered as a capsule or tablet.

17. The method of claim 16, wherein the capsule or tablet is more than 50% dissolved in the stomach prior to being released into the small intestines.

18. The method according to claim 17, wherein the unit dosage form is not coated with an acid resistant coating.

19. A method of treating vasomotor disturbances in a peri-menopausal or postmenopausal woman in need thereof comprising administering to the woman a compound of formula I or a salt thereof

20. The method of claim 19, wherein the compound of formula 1 is in its dihydrochloride salt form.

21. The method of claim 19, wherein a steady state trough level of the compound of formula I ranging from 0.11 ng/mL to 0.79 ng/mL or ranging from 0.12 ng/mL to 0.86 ng/mL is achieved.

22. The method of claim 19, wherein the compound of formula I is in the form of a dihydrochloride salt.

23. The method of claim 22, wherein the compound of formula I or a salt thereof is orally administered once-daily.

24. The method of claim 23, wherein the compound is in a unit dosage form.

25. The method of claim 24, wherein the unit dosage formulation is a capsule or tablet.

26. The method of claim 25, wherein the capsule or tablet is more than 50% dissolved in the stomach prior to being released into the small intestines.

27. The method according to claim 26, wherein the unit dosage form is not coated with an acid resistant coating.