IP Library Granted Patent US 11,851,439
Granted Patent B2
US 11,851,439 · App. 17/305,215 · Granted Dec 26, 2023

Compositions and methods of use for opioid hexadienoates and optionally substituted hexadienoates

Inventors: Georgiy Nikonov (Gainesville, FL); Levon Isakulyan (New York, NY); Michael Voronkov (Chelsea, MA)
Assignee: Kappa-Pharma LLC
C07D489/02A61P25/36C07C229/38C07D221/28A61K9/0053
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Quick Facts
Patent No.
US 11,851,439
App. No.
17/305,215
Granted
Dec 26, 2023
Kind
B2
Abstract

The present invention relates to opiate derived compositions and their antagonists useful in therapeutic areas associated with opioid receptor modulation. A 3-hexadienoate modification of the opioids is formulated to improve opiates' engagement of the opioid receptors when given orally. A 3-hexadienoate modification of nalbuphine or a pharmaceutically acceptable salt of thereof to improve quality of pain management when given intravenously, intranasally, transdermally, sublingually, rectally, topically, intramuscularly, subcutaneously or via inhalation. A 3-hexadienoate modification of the opioids antagonists is formulated to improve inhibition of the opioid receptors when given orally. A 3-hexadienoate modification of naloxone or a pharmaceutically acceptable salt of thereof to improve quality of Sobering when given intravenously, intranasally, transdermally, sublingually, rectally, topically, intramuscularly, subcutaneously or via inhalation.

Claims (8)

1. A method for treating a disease or condition, comprising administering an effective amount of a composition to a patient in need of such treatment, wherein said composition comprises a modified opioid, wherein said modified opioid is 3-allyl-4a-hydroxy-7-oxo-2,3,4,4a,5,6,7,7a-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-9-yl-(2E,4E)-hexa-2,4-dienoate, and wherein said disease or condition is an opioid addiction, pruritis or a dyskinesia associated with Tourette's syndrome.

2. A method for treating a disease or condition, comprising administering an effective amount of a composition to a patient in need of such treatment, wherein said composition comprises a modified opioid, wherein said modified opioid is 3-(cyclobutylmethyl)-4a, 7-dihydroxy-2,3,4,4a,5,6,7,7a-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-9-yl (2E,4E)-hexa-2,4-dienoate, and wherein said disease or condition is pruritis or pain.

3. The method of claim 1 , wherein said disease or condition is an opioid addiction.

4. The method of claim 1 , wherein said disease or condition is pruritis.

5. The method of claim 1 , wherein said disease or condition is a dyskinesia associated with Tourette's syndrome.

6. The method of claim 2 , wherein said disease or condition is pruritis.

7. The method of claim 2 , wherein said disease or condition is pain.

8. A method for treating or preventing opioid overdose, comprising administering an effective amount of a composition to a patient who has taken an opioid, wherein said composition comprises a modified opioid, wherein said modified opioid is 3-allyl-4a-hydroxy-7-oxo-2,3,4,4a,5,6,7,7a-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-9-yl -(2E,4E)-hexa-2,4-dienoate.

Continuity (4)
Continuation 16540058 · Aug 14, 2019
Provisional Application 62885311 · Aug 11, 2019
Provisional Application 62719417 · Aug 17, 2018
Related Publication 20210395260A1 · Dec 23, 2021