IP Library Granted Patent US 8,658,681
Granted Patent B2
US 8,658,681 · App. 13/448,964 · Granted Feb 25, 2014

Treatment of hyperproliferative disorders with diarylhydantoin compounds

Inventors: Charles L. Sawyers (New York, NY); Michael E. Jung (Los Angeles, CA); Charlie D. Chen (Los Angeles, CA); Samedy Ouk (Los Angeles, CA); Chris Tran (New York, NY); John Wongvipat (Nanuet, NY)
Assignee: The Regents of the University of California
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Quick Facts
Patent No.
US 8,658,681
App. No.
13/448,964
Granted
Feb 25, 2014
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 (49)

1. A method for treating a 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 cancer.

2. The method of claim 1 , further comprising administering an antiandrogen to the subject.

3. The method of claim 2 , wherein the composition is administered at a dosage of the compound in a range selected from the group consisting of from about 0.001 mg per kg body weight per day to about 100 mg per kg body weight per day, from about 0.01 mg per kg body weight per day to about 100 mg per kg body weight per day, and from about 0.1 mg per kg body weight per day to about 10 mg per kg body weight per day.

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

5. The method of claim 2 , wherein the compound is administered by intravenous injection, by injection into tissue, intraperitoneally, orally, or nasally.

6. The method of claim 2 , wherein the compound is 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.

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

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

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

10. The method of claim 2 , wherein the compound is

11. The method of claim 2 , wherein the antiandrogen is selected from the group consisting of a non-steroidal antiandrogen and bicalutamide.

12. The method of claim 2 , wherein the cancer is selected from the group consisting of prostate cancer, hormone sensitive prostate cancer, and hormone refractory prostate cancer.

13. The method of claim 2 ,

wherein the cancer is prostate cancer and

wherein administering the compound prevents the prostate cancer from progressing to hormone refractory prostate cancer.

14. The method of claim 2 ,

wherein the cancer is hormone sensitive prostate cancer and

wherein administering the compound prevents the hormone sensitive prostate cancer from progressing to hormone refractory prostate cancer.

15. The method of claim 2 , wherein the cancer is selected from the group consisting of breast cancer, hormone sensitive breast cancer, and hormone refractory breast cancer.

16. The method of claim 2 ,

wherein the cancer is breast cancer and

wherein administering the compound prevents the breast cancer from progressing to hormone refractory breast cancer.

17. The method of claim 2 ,

wherein the cancer is hormone sensitive breast cancer and

wherein administering the compound prevents the hormone sensitive breast cancer from progressing to hormone refractory breast cancer.

18. The method of claim 2 , wherein the cancer is selected from the group consisting of ovarian cancer, hormone sensitive ovarian cancer, and hormone refractory ovarian cancer.

19. The method of claim 1 ,

further comprising administering an antiandrogen to the subject,

wherein the compound is administered after administering the antiandrogen.

20. The method of claim 19 , wherein the compound is

21. The method of claim 19 , wherein the antiandrogen is bicalutamide.

22. The method of claim 19 , wherein the cancer is selected from the group consisting of prostate cancer, hormone sensitive prostate cancer, hormone refractory prostate cancer, breast cancer, and ovarian cancer.

23. The method of claim 1 , further comprising administering an antiestrogen to the subject.

24. The method of claim 23 , wherein the compound is

25. The method of claim 23 , wherein the cancer is selected from the group consisting of breast cancer, hormone sensitive breast cancer, and hormone refractory breast cancer.

26. The method of claim 23 ,

wherein the cancer is breast cancer and

wherein administering the compound prevents the breast cancer from progressing to hormone refractory breast cancer.

27. The method of claim 23 ,

wherein the cancer is hormone sensitive breast cancer and

wherein administering the compound prevents the hormone sensitive breast cancer from progressing to hormone refractory breast cancer.

28. The method of claim 23 , wherein the cancer is selected from the group consisting of ovarian cancer, hormone sensitive ovarian cancer, and hormone refractory ovarian cancer.

29. The method of claim 1 ,

further comprising administering an antiestrogen to the subject,

wherein the compound is administered after administering the antiestrogen.

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

31. The method of claim 29 , wherein the cancer is selected from the group consisting of breast cancer and ovarian cancer.

32. The method of claim 1 , further comprising administering a receptor modulator selected from the group consisting of an estrogen receptor modulator and a nuclear receptor modulator to the subject.

Assignments (4)
CONFIRMATORY LICENSE Recorded Feb 12, 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 029794/0379 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 12, 2012
From: JUNG, MICHAEL E.; CHEN, CHARLIE D.; OUK, SAMEDY
To: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Reel/Frame 029451/0209 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 12, 2012
From: SAWYERS, CHARLES L.; TRAN, CHRISTOPHER T.; WONGVIPAT, JOHN
To: HOWARD HUGHES MEDICAL INSTITUTE
Reel/Frame 029451/0213 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 12, 2012
From: HOWARD HUGHES MEDICAL INSTITUTE
To: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Reel/Frame 029451/0233 →
Continuity (7)
Continuation 12708523 · Feb 18, 2010
Division 11433829 · May 15, 2006
Provisional Application 60786837 · Mar 29, 2006
Provisional Application 60756552 · Jan 6, 2006
Provisional Application 60750351 · Dec 15, 2005
Provisional Application 60680835 · May 13, 2005
Related Publication 20120295944A1 · Nov 22, 2012