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公开(公告)号：US11590241B2
公开(公告)日：2023-02-28
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
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).
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2.发明授权Non-peptidyl, potent, and selective mu opioid receptor antagonists and their use in treating opioid addiction and opioid induced constipation 有权非肽，有效和选择性的阿片样物质受体拮抗剂及其在治疗阿片样物质成瘾和阿片样物质诱发便秘中的应用公开(公告)号：US08980908B2
公开(公告)日：2015-03-17
申请号：US14287254
申请日：2014-05-27
Applicant: Virginia Commonwealth University
Inventor： Yan Zhang , Dana E. Selley , William Dewey
IPC: A61K31/485 , C07D489/08 , G01N33/53
CPC classification number: C07D489/08 , G01N33/53 , G01N33/9486 , G01N2500/04
Abstract: Selective, non-peptide antagonists of the mu opioid receptor (MOR) and methods of their use are provided. The antagonists may be used, for example, to identify MOR agonists in competitive binding assays, and to treat conditions related to addiction in which MOR is involved, e.g. heroin, prescription drug and alcohol addiction, as well as in the treatment of opioid induced constipation (OIC).
Abstract translation: 提供了μ阿片受体（MOR）的选择性非肽拮抗剂及其使用方法。 拮抗剂可以用于例如在竞争性结合测定中鉴定MOR激动剂，并且用于治疗与其中涉及MOR的成瘾有关的病症，例如， 海洛因，处方药和酒精成瘾，以及治疗阿片样物质诱发便秘（OIC）。
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公开(公告)号：US10988481B2
公开(公告)日：2021-04-27
申请号：US16301765
申请日：2017-05-16
Applicant: VIRGINIA COMMONWEALTH UNIVERSITY
Inventor： Yan Zhang , Dana E. Selley , William Dewey , Hamid Abkarali
IPC: A61P25/30 , C07D489/08 , A61P25/04
Abstract: Analogues of 6 α/β-naltrexamine (NAQ) are provided. The analogues are selective, reversible antagonists of the mu opioid receptor (MOR) that exhibit good blood brain barrier penetration. The compounds are used in the treatment of opioid addiction and other diseases and conditions, including for the treatment of pain.
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4.发明申请NON-PEPTIDYL, POTENT, AND SELECTIVE MU OPIOID RECEPTOR ANTAGONISTS AND THEIR USE IN TREATING OPIOID ADDICTION AND OPIOID INDUCED CONSTIPATION 有权非肽，脂肪酸和选择性胡萝卜素受体拮抗剂及其在治疗阿片类药物和阿片样物质诱导剂中的应用公开(公告)号：US20140371255A1
公开(公告)日：2014-12-18
申请号：US14287254
申请日：2014-05-27
Applicant: Virginia Commonwealth University
Inventor： Yan Zhang , Dana E. Selley , William Dewey
IPC: C07D489/08 , G01N33/53
CPC classification number: C07D489/08 , G01N33/53 , G01N33/9486 , G01N2500/04
Abstract: Selective, non-peptide antagonists of the mu opioid receptor (MOR) and methods of their use are provided. The antagonists may be used, for example, to identify MOR agonists in competitive binding assays, and to treat conditions related to addiction in which MOR is involved, e.g. heroin, prescription drug and alcohol addiction, as well as in the treatment of opioid induced constipation (OIC).
Abstract translation: 提供了μ阿片受体（MOR）的选择性非肽拮抗剂及其使用方法。 拮抗剂可以用于例如在竞争性结合测定中鉴定MOR激动剂，并且用于治疗与其中涉及MOR的成瘾有关的病症，例如， 海洛因，处方药和酒精成瘾，以及治疗阿片样物质诱发便秘（OIC）。
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