IP Library Granted Patent US 9,072,743
Granted Patent B2
US 9,072,743 · App. 14/037,481 · Granted Jul 7, 2015

Modulators of androgen synthesis

Inventors: Suzanne Dilly (Oxfordshire, UA); Gregory Stoloff (London, GB); Paul Taylor (London, GB)
Assignee: Tangent Reprofilling Limited
A61K31/519A61K31/201A61K45/06
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Quick Facts
Patent No.
US 9,072,743
App. No.
14/037,481
Granted
Jul 7, 2015
Kind
B2
Abstract

The present specification discloses compositions comprising at least one therapeutic compound capable of modulating androgen production and methods and uses for treating a disorder associated with androgen production using such compositions and/or compounds.

Claims (30)

1. A pharmaceutical composition comprising a therapeutically effective amount of a benzo(iso)oxazolepiperidine, a therapeutically effective amount of a 9Z,11E conjugated Linoleic Acid,

wherein there is a synergistic effect between the therapeutically effective amount of the benzo(iso)oxazolepiperidine and the therapeutically effective amount of a 9Z,11E conjugated Linoleic Acid; and

wherein the modulating activity of the composition reduces a symptom of a disorder associated with androgen production.

2. The composition according to claim 1 , wherein the composition reduces a level of a dihydrotestosterone, reduces a level of a testosterone, a level of an androstenedione, a level of an androstenediol, a level of a dehydroepiandrosterone, a level of an estrogen, or any combination thereof.

3. The composition according to claim 1 , wherein the benzo(iso)oxazolepiperidine is an optionally substituted lloperidone, an optionally substituted ocaperidone, an optionally substituted paliperidone, an optionally substituted risperidone, or any combination thereof.

4. A pharmaceutical composition consisting essentially of a therapeutically effective amount of a benzo(iso)oxazolepiperidine, a therapeutically effective amount of a 9Z,11 E conjugated Linoleic Acid, pharmaceutically-acceptable carriers and/or pharmaceutically-acceptable components,

wherein there is a synergistic effect between the therapeutically effective amount of the benzo(iso)oxazolepiperidine and the therapeutically effective amount of a 9Z,11 E conjugated Linoleic Acid.

5. The composition according to claim 4 , wherein the benzo(iso)oxazolepiperidine is an optionally substituted lloperidone, an optionally substituted ocaperidone, an optionally substituted paliperidone, an optionally substituted risperidone, or any combination thereof.

6. The composition according to claim 4 , wherein the benzo(iso)oxazolepiperidine is optionally substituted risperidone.

7. The composition according to claim 4 , wherein the pharmaceutically-acceptable carriers include vehicles, stabilizers, diluents, additives, auxiliarys or excipients.

8. The composition according to claim 4 , wherein the pharmaceutically-acceptable components include buffers, preservatives, tonicity adjusters, salts, antioxidants, osmolality adjusting agents, physiological substances, pharmacological substances, bulking agents, emulsifying agents, wetting agents, flavoring agents, or coloring agents.

9. The composition according to claim 1 , wherein the benzo(iso)oxazolepiperidine is optionally substituted risperidone.

10. The composition according to claim 1 , wherein the benzo(iso)oxazolepiperidine is risperidone.

11. The composition according to claim 3 , wherein the benzo(iso)oxazolepiperidine is risperidone.

12. The composition according to claim 9 , wherein the benzo(iso)oxazolepiperidine is risperidone.

13. The composition according to claim 1 , further comprising a pharmaceutically-acceptable carrier.

14. The composition according to claim 13 , wherein the pharmaceutically-acceptable carrier includes vehicles, stabilizers, diluents, additives, auxiliarys or excipients.

15. The composition according to claim 1 , further comprising a pharmaceutically-acceptable component.

16. The composition according to claim 15 , wherein the pharmaceutically-acceptable component includes buffers, preservatives, tonicity adjusters, salts, antioxidants, osmolality adjusting agents, physiological substances, pharmacological substances, bulking agents, emulsifying agents, wetting agents, flavoring agents, or coloring agents.

17. The composition according to claim 4 , wherein the benzo(iso)oxazolepiperidine is risperidone.

18. The composition according to claim 6 , wherein the benzo(iso)oxazolepiperidine is risperidone.

19. The composition according to claim 1 , further comprising a therapeutically effective amount of a chemotherapeutic or anti-proliferative agent, wherein the chemotherapeutic or anti-proliferative agent is selected from the group consisting of an alkylating agent, a platinum agent, an antimetabolite, a topoisomerase inhibitor,-an antitumor antibiotic, an aromatase inhibitor, a thymidylate synthase inhibitor, a DNA antagonist, farnesyltransferase inhibitor, a pump inhibitor, a metalloproteinase inhibitor, a ribonucleoside reductase inhibitor, a TNFα agonist, an endothelin A receptor antagonist, a retinoic acid receptor agonist, an immuno-modulator, a hormonal and antihormonal agent, a photodynamic agent, a tyrosine kinase inhibitor, and any combination thereof.

20. The composition according to claim 1 , wherein the therapeutically effective amount of the benzo(iso)oxazolepiperidine about 0.1 mg/day to about 20 mg/day.

21. The composition according to claim 1 , wherein the therapeutically effective amount of the benzo(iso)oxazolepiperidine is from about 0.01 mg/kg/day to about 0.5 mg/kg/day.

22. The composition according to claim 1 , wherein the therapeutically effective amount of the 9Z,11 E conjugated Linoleic Acid when formulated with the benzo(iso)oxazolepiperidine is from about 1 mg/day to about 20 mg/day.

23. The composition according to claim 1 , wherein the therapeutically effective amount of the 9Z,11 E conjugated Linoleic Acid when formulated with the benzo(iso)oxazolepiperidine is from about 0.01 mg/kg/day to about 0.5 mg/kg/day.

24. The composition according to claim 4 , wherein the therapeutically effective amount of the benzo(iso)oxazolepiperidine about 0.1 mg/day to about 20 mg/day.

25. The composition according to claim 4 , wherein the therapeutically effective amount of the benzo(iso)oxazolepiperidine is from about 0.01 mg/kg/day to about 0.5 mg/kg/day.

26. The composition according to claim 4 , wherein the therapeutically effective amount of the 9Z,11 E conjugated Linoleic Acid when formulated with the benzo(iso)oxazolepiperidine is from about 1 mg/day to about 20 mg/day.

27. The composition according to claim 4 , wherein the therapeutically effective amount of the 9Z,11 E conjugated Linoleic Acid when formulated with the benzo(iso)oxazolepiperidine is from about 0.01 mg/kg/day to about 0.5 mg/kg/day.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 10, 2015
From: DILLY, SUZANNE; STOLOFF, GREGORY; TAYLOR, PAUL
To: TANGENT REPROFILING LIMITED
Reel/Frame 035602/0447 →
Continuity (3)
Provisional Application 61871662 · Aug 29, 2013
Provisional Application 61705790 · Sep 26, 2012
Related Publication 20140088120A1 · Mar 27, 2014