公开(公告)号：US20210205472A1

公开(公告)日：2021-07-08

申请号：US15998948

申请日：2017-02-17

Applicant: VIRGINIA COMMONWEALTH UNIVERSITY

Inventor： Yan ZHANG ,  Hu YANG ,  Dana SELLEY ,  William DEWEY ,  Hamid AKBARALI

IPC: A61K47/69 ,  A61K31/485

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).

公开(公告)号：US20190308987A1

公开(公告)日：2019-10-10

申请号：US16306232

申请日：2017-05-26

Applicant: VIRGINIA COMMONWEALTH UNIVERSITY

Inventor： Yan ZHANG ,  Dana SELLEY ,  William DEWEY ,  Hamid AKBARALI

IPC: C07D489/08 ,  A61P1/00

Abstract: Peripherally selective compounds that modulate both the mu opioid receptor (MOR) and the kappa opioid receptor (KOR) are provided. The compounds are substituted derivatives of 6p-N-heterocyclic naltrexamine (NAP) and are used in the treatment of diseases involving visceral pain such as irritable bowel syndrome (IBS), opioid induced constipation (OIC), and others.