IP Library Granted Patent US 8,183,274
Granted Patent B2
US 8,183,274 · App. 12/708,523 · Granted May 22, 2012

Treatment of hyperproliferative disorders with diarylhydantoin compounds

Assignee: The Regents of the University of California
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Quick Facts
Patent No.
US 8,183,274
App. No.
12/708,523
Granted
May 22, 2012
Kind
B2
Abstract

The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.

Claims (44)

1. A method for treating prostate cancer comprising administering a therapeutically effective amount of a compound selected from the group consisting of

or a pharmaceutically acceptable salt thereof to a subject in need of such treatment, thereby treating the prostate cancer.

2. The method of claim 1 , wherein the compound is administered at a dosage in the range of from about 0.001 mg per kg body weight per day to about 100 mg per kg body weight per day.

3. The method of claim 1 , wherein the compound is administered at a dosage in the range of from about 1 mg per kg body weight per day to about 10 mg per kg body weight per day.

4. The method of claim 1 , wherein the compound is administered at a dosage in the range of from about 0.1 mg per kg body weight per day to about 10 mg per kg body weight per day.

5. The method of claim 1 , wherein the compound is administered at a dosage of about 1 mg per kg body weight per day.

6. The method of claim 1 , wherein the prostate cancer is hormone refractory prostate cancer.

7. The method of claim 1 , wherein the compound is administered by intravenous injection, by injection into tissue, intraperitoneally, orally, topically, or nasally.

8. The method of claim 1 , wherein the compound is administered orally.

9. The method of claim 1 , wherein the compound is administered in a form selected from the group consisting of a solution, dispersion, suspension, powder, capsule, tablet, pill, time release capsule, time release tablet, and time release pill.

10. The method of claim 1 , wherein the compound is administered in a form selected from the group consisting of a capsule, tablet, and pill.

11. The method of claim 1 , wherein the prostate cancer is hormone sensitive prostate cancer.

12. The method of claim 1 , wherein the compound is

13. The method of claim 1 , wherein the compound is administered with a pharmaceutically acceptable carrier or diluent.

14. The method of claim 13 , wherein the pharmaceutically acceptable carrier or diluent comprises one or more of dimethylsulfoxide (DMSO), polyethylene glycol (PEG), and water.

15. The method of claim 1 , wherein the compound is administered at a dosage of about 2 mg per kg body weight per day.

16. The method of claim 1 , wherein the compound is administered to achieve a peak plasma concentration in the range of from about 0.5 μM to about 75 μM.

17. The method of claim 1 , wherein the compound is administered to achieve a peak plasma concentration of about 10 μM.

18. The method of claim 1 , wherein the compound is administered to achieve a steady state plasma concentration of from about 5 μM to about 100 μM.

19. The method of claim 1 , wherein the compound is administered to achieve a steady state plasma concentration of from about 10 μM to about 50 μM.

20. The method of claim 1 , wherein the compound is administered to achieve a steady state plasma concentration of about 25 μM.

21. The method of claim 1 , wherein the compound is administered daily.

22. The method of claim 1 , wherein the compound is administered three times per day.

23. The method of claim 1 , wherein the compound is administered in a unit dosage form comprising from about 5 mg to about 1000 mg of active ingredient per unit dosage form.

24. The method of claim 1 , wherein the compound is administered in a unit dosage form comprising about 100 mg of active ingredient per unit dosage form.

25. A method for treating benign prostate hyperplasia comprising administering a therapeutically effective amount of a compound selected from the group consisting of

or a pharmaceutically acceptable salt thereof to a subject in need of such treatment, thereby treating the benign prostate hyperplasia.

26. The method of claim 1 , wherein the compound is

27. The method of claim 1 , wherein the compound is

28. The method of claim 25 , wherein the compound is

29. The method of claim 25 , wherein the compound is

30. The method of claim 25 , wherein the compound is

31. The method of claim 12 , wherein the prostate cancer is hormone refractory prostate cancer.

32. The method of claim 12 , wherein the prostate cancer is hormone sensitive prostate cancer.

33. A method for treating breast cancer comprising administering a therapeutically effective amount of a compound selected from the group consisting of

or a pharmaceutically acceptable salt thereof to a subject in need of such treatment, thereby treating the breast cancer.

34. The method of claim 33 , wherein the compound is

35. The method of claim 33 , wherein the compound is

36. The method of claim 33 , wherein the compound is

37. A method for treating ovarian cancer comprising administering a therapeutically effective amount of a compound selected from the group consisting of

or a pharmaceutically acceptable salt thereof to a subject in need of such treatment, thereby treating the ovarian cancer.

38. The method of claim 37 , wherein the compound is

39. The method of claim 37 , wherein the compound is

40. The method of claim 37 , wherein the compound is

Assignments (5)
CONFIRMATORY LICENSE Recorded Feb 20, 2013
From: UNIVERSITY OF CALIFORNIA LOS ANGELES
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 029839/0078 →
CONFIRMATORY LICENSE Recorded Oct 24, 2012
From: REGENTS OF THE UNIVERSITY OF CALIFORNIA
To: US ARMY, SECRETARY OF THE ARMY
Reel/Frame 029187/0722 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 1, 2012
From: HOWARD HUGHES MEDICAL INSTITUTE
To: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Reel/Frame 027787/0457 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 1, 2012
From: SAWYERS, CHARLES L.; TRAN, CHRISTOPHER T.; WONGVIPAT, JOHN
To: HOWARD HUGHES MEDICAL INSTITUTE
Reel/Frame 027787/0474 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 1, 2012
From: JUNG, MICHAEL E.; CHEN, CHARLIE D.; OUK, SAMEDY
To: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Reel/Frame 027787/0481 →
Continuity (6)
Division 11433829 · May 15, 2006
Provisional Application 60680835 · May 13, 2005
Provisional Application 60750351 · Dec 15, 2005
Provisional Application 60756552 · Jan 6, 2006
Provisional Application 60786837 · Mar 29, 2006
Related Publication 20100172975A1 · Jul 8, 2010