IP Library Granted Patent US 11,590,241
Granted Patent B2
US 11,590,241 · App. 15/998,948 · Granted Feb 28, 2023

Nanoparticle conjugated synthetic opioid prodrugs and methods of their uses

Inventors: Yan Zhang (Glen Allen, VA); Hu Yang (Richmond, VA); Dana Selley (Richmond, VA); William Dewey (Richmond, VA); Hamid Akbarali (Richmond, VA)
Assignee: Virginia Commonwealth University
A61K47/6935A61K31/485A61K47/6907B82Y5/00B82Y30/00B82Y40/00
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Quick Facts
Patent No.
US 11,590,241
App. No.
15/998,948
Granted
Feb 28, 2023
Kind
B2
Abstract

Provided herein are nanoparticle conjugated synthetic opioid prodrugs that target the peripheral mu opioid receptor (MOR). The prodrugs exhibit long-lived bioavailability, do not compromise the analgesic effects of opioids administered for pain relief (and in some cases can be used for pain relief), and do not induce opioid withdrawal symptoms, when their use is discontinued. Certain of the prodrugs are especially useful for the prevention and/or treatment of unwanted opioid-induced side effects such as opioid-induced constipation (OIC).

Claims (15)

1. A compound having the general formula:

where

m=0-16;

y=5-20;

z=10-30; and

R′ and R″ are independently hydrogen or a substituted or unsubstituted aromatic or aliphatic moiety.

2. The compound of claim 1 , wherein the compound is

3. A method of preventing or treating opioid induced constipation (OIC) in a subject in need thereof, comprising

administering to the subject a therapeutically effective amount of a compound having the general formula

where

m=0-16;

y=5-20;

z=10-30; and

R′ and R″ are independently hydrogen or a substituted or unsubstituted aromatic or aliphatic moiety.

4. The method of claim 2 , wherein the compound is

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 23, 2023
From: ZHANG, YAN; YANG, HU; SELLEY, DANA; DEWEY, WILLIAM; AKBARALI, HAMID
To: VIRGINIA COMMONWEALTH UNIVERSITY
Reel/Frame 062451/0467 →
CONFIRMATORY LICENSE Recorded Nov 4, 2022
From: VIRGINIA COMMENWEALTH UNIVERSITY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 061883/0356 →
Continuity (2)
Provisional Application 62296671 · Feb 18, 2016
Related Publication 20210205472A1 · Jul 8, 2021