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Last Updated: November 30, 2020

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Claims for Patent: 10,052,314

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Summary for Patent: 10,052,314
Title:Anti-androgens for the treatment of non-metastatic castrate-resistant prostate cancer
Abstract: Described herein are methods of treating non-metastatic castrate-resistant prostate cancer with anti-androgens.
Inventor(s): Chen; Isan (San Diego, CA)
Assignee: Aragon Pharmaceuticals, Inc. (San Diego, CA)
Application Number:15/851,444
Patent Claims: 1. A method of treating a male human with non-metastatic castration-resistant prostate cancer, the method comprising administering an anti-androgen at a dose of about 30 mg per day to about 480 mg per day to a male human in need of such treatment, wherein the anti-androgen is: 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspir- o[3.4]oct-5-yl]-2 fluoro-N-methylbenzamide, 4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimida- zolidin-1-yl)-2-fluoro-N-methylbenzamide, or 4-[7-[4-cyano-3-(trifluoromethyl)phenyl]-8-oxo-6-thioxo-5,7-diazaspiro[3.- 4]oct-5-yl]-2-fluoro-N-methylbenzamide; wherein said method further comprises administering a gonadotropin releasing hormone (GnRH) agonist.

2. The method of claim 1, wherein the non-metastatic castration-resistant prostate cancer is a high risk non-metastatic castration-resistant prostate cancer.

3. The method of claim 1, wherein the anti-androgen is 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspir- o[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide.

4. The method of claim 3, wherein 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspir- o[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide is administered daily to the male human.

5. The method of claim 3, wherein 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5, 7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide (ARN-509) is administered orally to the male human at a dose of about 180 mg per day to about 480 mg per day.

6. The method of claim 3, wherein 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspir- o[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide (ARN-509) is administered orally to the male human at a dose of: (a) about 30 mg per day; (b) about 60 mg per day; (c) about 90 mg per day; (d) about 120 mg per day; or (e) about 240 mg per day.

7. The method of claim 3, wherein 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspir- o[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide is administered orally to the male human on a continuous daily dosage schedule.

8. The method of claim 3, wherein the GnRH agonist is leuprolide, buserelin, naferelin, histrelin, goserelin or deslorelin.

9. The method of claim 1, wherein the anti-androgen is 4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimida- zolidin-1-yl)-2-fluoro-N-methylbenzamide.

10. The method of claim 9, wherein the GnRH agonist is leuprolide, buserelin, naferelin, histrelin, goserelin or deslorelin.

11. The method of claim 1, wherein the anti-androgen is 4-[7-[4-cyano-3-(trifluoromethyl)phenyl]-8-oxo-6-thioxo-5,7-diazaspiro[3.- 4]oct-5-yl]-2-fluoro-N-methylbenzamide.

12. The method of claim 11, wherein the GnRH agonist is leuprolide, buserelin, naferelin, histrelin, goserelin or deslorelin.

13. The method of claim 1, wherein the anti-androgen is administered orally to the male human.

14. A method of treating a male human with non-metastatic castration-resistant prostate cancer, the method consisting essentially of administering an anti-androgen at a dose of about 30 mg per day to about 480 mg per day to a male human in need of such treatment, wherein the anti-androgen is: 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspir- o[3.4]oct-5-yl]-2 fluoro-N-methylbenzamide, 4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimida- zolidin-1-yl)-2-fluoro-N-methylbenzamide, or 4-[7-[4-cyano-3-(trifluoromethyl)phenyl]-8-oxo-6-thioxo-5,7-diazaspiro[3.- 4]oct-5-yl]-2-fluoro-N-methylbenzamide; wherein said method further comprises administering a gonadotropin releasing hormone (GnRH) agonist.

15. The method of claim 14, wherein the anti-androgen is 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspir- o[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide.

16. The method of claim 15, wherein the GnRH agonist is leuprolide, buserelin, naferelin, histrelin, goserelin or deslorelin.

17. The method of claim 15, wherein 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspir- o[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide (ARN-509) is administered orally to the male human at a dose of: (a) about 30 mg per day; (b) about 60 mg per day; (c) about 90 mg per day; (d) about 120 mg per day; or (e) about 240 mg per day.

18. The method of claim 9, wherein the 4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimida- zolidin-1-yl)-2-fluoro-N-methylbenzamide is administered orally to the male human at a dose of about 160 mg per day.

19. The method of claim 3, wherein 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspir- o[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide is administered orally to the male human at a dose of about 240 mg per day.

20. The method of claim 3, wherein the GnRH agonist is leuprolide.

21. The method of claim 3, wherein the GnRH agonist is buserelin.

22. The method of claim 3, wherein the GnRH agonist is naferelin.

23. The method of claim 3, wherein the GnRH agonist is histrelin.

24. The method of claim 3, wherein the GnRH agonist is goserelin.

25. The method of claim 3, wherein the GnRH agonist is deslorelin.

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