IP Library Granted Patent US 10,195,191
Granted Patent B2
US 10,195,191 · App. 14/941,867 · Granted Feb 5, 2019

Opioid agonist antagonist combinations

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Quick Facts
Patent No.
US 10,195,191
App. No.
14/941,867
Granted
Feb 5, 2019
Kind
B2
Abstract

The invention relates a composition comprising an opioid agonist and Compound-1:

Claims (27)

1. A composition comprising a pharmaceutically effective amount of buprenorphine and Compound-1:

wherein Compound-1:buprenorphine has a molar ratio of about 0.5-5.0:1.0.

2. The composition according to claim 1 , wherein the molar ratio of Compound-1:agonist is about 0.5-4.0:1.0.

3. A controlled release formulation comprising a composition according to claim 1 .

4. The composition according to claim 1 , further comprising an additional agent for the treatment of depression selected from the group consisting of a selective serotonin re-uptake inhibitor, serotonin reuptake inhibitor (S SRI), serotonin-norepinephrine reuptake inhibitor (SNRI), monoamine oxidase inhibitor (MAOIs) and tricyclic antidepressants, or an antidepressant compound belonging to the heterocyclic class.

5. The composition of claim 4 , wherein said additional anti-depressant is selected from the group consisting of fluoxetine, norfluoxetine, paroxetine, sertraline, fluvoxamine, citalopram, escitalopram, bupropion, nefazodone, mirtazapine, venlafaxine, duloxetine, milnacipran, reboxetine, zimelidine, indalpine, gepirone, femoxetine and alaproclate.

6. A unit dosage form comprising a composition according to claim 1 .

7. The composition according to claim 1 , wherein the molar ratio of Compound-1:agonist is about 0.9-1.3:1.0.

8. A method of treating a depressive disorder comprising the step of administering Compound-1 in combination with buprenorphine to a patient in need thereof:

wherein Compound-1:buprenorphine has a molar ratio of about 0.5-5.0:1.0.

9. The method according to claim 8 , wherein said depressive disorder is selected from the group consisting of major depressive disorder, chronic depression, severe unipolar recurrent major depressive episodes, dysthymic disorder, depressive neurosis and neurotic depression, melancholic depression, atypical depression, reactive depression, treatment resistant depression, seasonal affective disorder and pediatric depression; premenstrual syndrome, premenstrual dysphoric disorder, hot flashes, bipolar disorders or manic depression, bipolar I disorder, bipolar II disorder and cyclothymic disorder.

10. The method according to claim 9 , wherein said depressive disorder is major depressive disorder.

11. The method according to claim 10 , wherein said major depressive disorder is resistant to two or more antidepressants.

12. The method according to claim 11 , wherein the antidepressants are selected from the group consisting of the group comprising selective serotonin reuptake inhibitors (SSRIs), Serotonin-norepinephrine reuptake inhibitors (SNRIs), Monoamine oxidase inhibitors (MAOIs) and Tricyclic antidepressants.

13. The method according to claim 8 , wherein said depressive disorder is treatment resistant depression.

14. The method according to claim 8 , wherein said subject exhibits one or more depressive symptoms selected from the group consisting of irritability, feelings of hopelessness and helplessness, inability to concentrate, sadness, insomnia, appetite loss, lack of interest in life's activities, thoughts of suicide, dizziness, nausea, vomiting, hyperhidrosis, menorrhagia, pain in extremity, constipation, sedation, fatigue, feeling abnormal, flushing and somnolence.

15. The method according to claim 8 , wherein the molar ratio of Compound-1:agonist is about 0.5-4.0:1.0.

16. The composition according to claim 1 , wherein the molar ratio of Compound-1:agonist is about 0.5-3.0:1.0.

17. The composition according to claim 1 , wherein the molar ratio of Compound-1:agonist is about 0.5-2.5:1.0.

18. The composition according to claim 1 , wherein the molar ratio of Compound-1:agonist is about 0.5-1.75:1.0.

19. The composition according to claim 1 , wherein the molar ratio of Compound-1:agonist is about 0.75-1.5:1.0.

20. The method according to claim 8 , wherein the molar ratio of Compound-1:agonist is about 0.5-3.0:1.0.

21. The method according to claim 8 , wherein the molar ratio of Compound-1:agonist is about 0.5-2.5:1.0.

22. The method according to claim 8 , wherein the molar ratio of Compound-1:agonist is about 0.5-1.75:1.0.

23. The method according to claim 8 , wherein the molar ratio of Compound-1:agonist is about 0.75-1.5:1.0.

24. The method according to claim 8 , wherein the molar ratio of Compound-1:agonist is about 0.9-1.3:1.0.

25. The composition according to claim 1 , wherein the molar ratio of Compound-1:agonist is about 0.9-1.3:1.0.

Assignments (3)
SECURITY INTEREST Recorded Feb 13, 2026
From: ALKERMES PHARMA IRELAND LIMITED
To: JPMORGAN CHASE BANK, N.A. AS ADMINISTRATIVE AGENT
Reel/Frame 074858/0405 →
RELEASE OF SECURITY INTEREST IN PATENTS PREVIOUSLY RECORDED AT REEL/FRAME (073213/0302) Recorded Feb 13, 2026
From: JPMORGAN CHASE BANK, N.A., AS ADMINISTRATIVE AGENT
To: ALKERMES PHARMA IRELAND LIMITED
Reel/Frame 074858/0429 →
SECURITY INTEREST Recorded Oct 23, 2025
From: ALKERMES PHARMA IRELAND LIMITED
To: JPMORGAN CHASE BANK, N.A. AS ADMINISTRATIVE AGENT
Reel/Frame 073213/0302 →