IP Library Granted Patent US 11,186,585
Granted Patent B2
US 11,186,585 · App. 16/540,058 · Granted Nov 30, 2021

Compositions and methods of enhancing opioid receptor engagement by opioid hexadienoates and optionally substituted hexadienoates

Inventors: Georgiy Nikonov (Gainsville, FL); Levon Isakulyan (New York, NY); Michael Voronkov (Pennington, NJ)
Assignee: Kappa-Pharma LLC
C07D489/02A61P25/36C07C229/38C07D221/28A61K9/0053
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Quick Facts
Patent No.
US 11,186,585
App. No.
16/540,058
Granted
Nov 30, 2021
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 (4)

1. The compound having the chemical formula 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 or any pharmaceutically acceptable salts thereof.

2. A composition comprising a pharmaceutically effective amount of the compound of claim 1 and a pharmaceutically acceptable carrier.

3. The compound having the chemical formula 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 or any pharmaceutically acceptable salts thereof.

4. A composition comprising a pharmaceutically effective amount of the compound of claim 3 and a pharmaceutically acceptable carrier.

Assignments (3)
NUNC PRO TUNC ASSIGNMENT Recorded Nov 18, 2019
From: NIKONOV, GEORGIY
To: KAPPA-PHARMA LLC
Reel/Frame 051035/0027 →
NUNC PRO TUNC ASSIGNMENT Recorded Nov 18, 2019
From: ISAKULYAN, LEVON
To: KAPPA-PHARMA LLC
Reel/Frame 051035/0137 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 18, 2019
From: VORONKOV, MICHAEL
To: KAPPA-PHARMA LLC
Reel/Frame 051851/0123 →
Continuity (3)
Provisional Application 62885311 · Aug 11, 2019
Provisional Application 62719417 · Aug 17, 2018
Related Publication 20200055864A1 · Feb 20, 2020