IP Library › Granted Patent US 10,314,838
Granted Patent B2
US 10,314,838 · App. 15/718,139 · Granted Jun 11, 2019

Compositions of buprenorphine and μ antagonists

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Quick Facts
Patent No.
US 10,314,838
App. No.
15/718,139
Granted
Jun 11, 2019
Kind
B2
Abstract

The invention relates to a composition comprising buprenorphine and a μ opioid receptor antagonist, wherein the composition is characterized by an Agonist Antagonist Activity Index (AAnAI) of between about 0.7 and about 2.2; wherein; AAnAI = [ c ma ⁢ ⁢ x ⁡ ( BUP ) / EC 50 ] [ c ma ⁢ ⁢ x ⁡ ( ANTAGONIST ) / IC 50 ] .

Claims (18)

1. A composition comprising about 2 mg to about 25 mg of buprenorphine and a therapeutically effective amount of Compound-1, wherein Compound-1 has the structure:

2. The composition according to claim 1 , comprising about 1.0 to about 20 mg of Compound-1.

3. The composition according to claim 1 , comprising about 1.0 to about 10 mg of Compound-1.

4. The composition according to claim 1 , comprising about 1.0 to about 8 mg of Compound-1.

5. The composition according to claim 1 , comprising about 1.0 to about 4 mg of Compound-1.

6. The composition according to claim 1 , comprising about 2 mg of Compound-1.

7. The composition according to claim 1 , comprising about 2 mg to about 8 mg of buprenorphine.

8. The composition according to claim 1 , comprising about 2 mg to about 4 mg of buprenorphine.

9. The composition according to claim 1 , comprising about 2mg of buprenorphine.

10. A composition comprising about 0.5 mg to about 20 mg of Compound-1 and a therapeutically effective amount of buprenorphine, wherein Compound-1 has the structure:

11. The composition according to claim 10 , comprising about 1.0 to about 10 mg of Compound-1.

12. The composition according to claim 10 , comprising about 1.0 to about 8 mg of Compound-1.

13. The composition according to claim 10 , comprising about 1.0 to about 4 mg of Compound-1.

14. The composition according to claim 10 , comprising about 2mg of Compound-1.

15. The composition according to claim 10 , comprising about 2 mg to about 50 mg of buprenorphine.

16. The composition according to claim 10 , comprising about 2 mg to about 8 mg of buprenorphine.

17. The composition according to claim 10 , comprising about 2 mg to about 4 mg of buprenorphine.

18. The composition according to claim 10 , comprising about 2mg of buprenorphine.

Assignments (6)
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 →
RELEASE OF PATENT SECURITY AGREEMENTS Recorded Dec 24, 2024
From: MORGAN STANLEY SENIOR FUNDING, INC.
To: ALKERMES PHARMA IRELAND LIMITED
Reel/Frame 069771/0701 →
SECURITY INTEREST Recorded Mar 20, 2020
From: ALKERMES PHARMA IRELAND LIMITED
To: MORGAN STANLEY SENIOR FUNDING, INC.
Reel/Frame 052914/0832 →
SECURITY INTEREST Recorded Dec 4, 2018
From: ALKERMES PHARMA IRELAND LIMITED
To: MORGAN STANLEY SENIOR FUNDING, INC.
Reel/Frame 047671/0386 →