公开(公告)号：US10858331B1

公开(公告)日：2020-12-08

申请号：US16987609

申请日：2020-08-07

Applicant: VIRGINIA COMMONWEALTH UNIVERSITY

Inventor： Martin Safo ,  Yan Zhang ,  Jurgen Venitz ,  Richmond Danso-Danqua ,  Tanvi Deshpande

IPC: C07D307/58 ,  C07D213/30

Abstract: The invention provides new aromatic aldehyde compounds that have greater potency in increasing the affinity of Hb for oxygen, greater potency for preventing sickling, and additional pharmacologic properties that ameliorate other symptoms of SCD. The invention further provides methods for treating SCD by providing a subject having SCD with a compound according to the invention.

公开(公告)号：US20200369638A1

公开(公告)日：2020-11-26

申请号：US16987609

申请日：2020-08-07

Applicant: VIRGINIA COMMONWEALTH UNIVERSITY

Inventor： Martin Safo ,  Yan Zhang ,  Jurgen Venitz ,  Richmond Danso-Danqua ,  Tanvi Deshpande

IPC: C07D307/58 ,  C07D213/30

Abstract: The invention provides new aromatic aldehyde compounds that have greater potency in increasing the affinity of Hb for oxygen, greater potency for preventing sickling, and additional pharmacologic properties that ameliorate other symptoms of SCD. The invention further provides methods for treating SCD by providing a subject having SCD with a compound according to the invention.

公开(公告)号：US10344001B2

公开(公告)日：2019-07-09

申请号：US15764052

申请日：2016-09-30

Applicant: VIRGINIA COMMONWEALTH UNIVERSITY

Inventor： Martin K. Safo ,  Yan Zhang ,  Mohini Ghatge ,  Osheiza Abdulmalik ,  Abdelsattar Mansour Ebid Omar ,  Moustafa El-Sayed El-Araby

IPC: A61K31/4174 ,  A61K31/4178 ,  C07D233/58 ,  A61P7/00 ,  C07D405/12 ,  C07D233/64

Abstract: Azolylacryloyl derivatives with hypoxic properties are provided. The compounds have a generic formula: and are suitable for treating sickle cell disease and hypoxia-underlying diseases, e.g. hemorrhagic and traumatic shock, cardiac arrest and cardiogenic shock, traumatic brain injury, cancer, stroke, myocardial infarction, myocardial ischemia, vaso-occlusive crisis, etc.

公开(公告)号：US20140357656A1

公开(公告)日：2014-12-04

申请号：US14371075

申请日：2013-01-10

Applicant: Virginia Commonwealth University

Inventor： Yan Zhang ,  Kurt F. Hauser ,  Dana E. Selley

IPC: C07D489/08 ,  A61K31/485

CPC classification number: A61K47/481 ,  A61K31/485 ,  A61K47/55 ,  C07D489/08 ,  A61K2300/00

Abstract: Bivalent ligands that contain two pharmacophores linked through a spacer, one of which interacts with the μ-opioid receptor (MOR) and the other of which interacts with the co-receptor CC chemokine receptor 5 (CCR5), are used for the treatment of neurological disorders such as those associated with AIDS.

Abstract translation: 含有通过间隔基连接的两个药效团的二价配体，其中一个与μ-阿片受体（MOR）相互作用，另一个与辅助受体CC趋化因子受体5（CCR5）相互作用）用于治疗神经系统 诸如与艾滋病相关的疾病。

公开(公告)号：US11014933B2

公开(公告)日：2021-05-25

申请号：US16726420

申请日：2019-12-24

Applicant: Virginia Commonwealth University

Inventor： Yan Zhang

IPC: C07D489/08

Abstract: Non-peptide MOR opioid receptor modulators are provided. The compounds exhibit predominantly central activity and are used to treat e.g. substance use disorders, and pain.

公开(公告)号：US09884836B2

公开(公告)日：2018-02-06

申请号：US15113449

申请日：2015-01-22

Applicant: VIRGINIA COMMONWEALTH UNIVERSITY

Inventor： Dwight A. Williams ,  Yan Zhang

IPC: C07D311/22 ,  C07D407/06 ,  C07D409/06

CPC classification number: C07D311/22 ,  C07D407/06 ,  C07D409/06

Abstract: A family of compounds which function as selective ligands for the serotonin receptor 2B (5-HT2B) is identified. Some of the compounds are synthetic non-natural ligands which have a relatively strong interaction with 5-HT2B compared to naturally occurring compounds (some of which are identified for the first time herein as ligands for 5-HT2B). Because the compounds, both naturally occurring and synthetically produced, function as ligands for 5-HT2B they will have application in, for example, the treatment and/or prevention of nervous system disorders such as Alzheimer's disease.

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）。

公开(公告)号：US08946254B2

公开(公告)日：2015-02-03

申请号：US14371075

申请日：2013-01-10

Applicant: Virginia Commonwealth University

Inventor： Yan Zhang ,  Kurt F. Hauser ,  Dana E. Selley

IPC: A61K31/485 ,  C07D489/08

CPC classification number: A61K47/481 ,  A61K31/485 ,  A61K47/55 ,  C07D489/08 ,  A61K2300/00

Abstract: Bivalent ligands that contain two pharmacophores linked through a spacer, one of which interacts with the μ-opioid receptor (MOR) and the other of which interacts with the co-receptor CC chemokine receptor 5 (CCR5), are used for the treatment of neurological disorders such as those associated with AIDS.

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

IPC: A61K47/69 ,  A61K31/485 ,  A61P25/04 ,  A61P1/00 ,  B82Y5/00 ,  B82Y30/00 ,  B82Y40/00

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：US10800751B2

公开(公告)日：2020-10-13

申请号：US14913180

申请日：2014-08-21

Applicant: Virginia Commonwealth University

Inventor： Martin Safo ,  Jurgen Venitz ,  Richmond Danso-Danquah ,  Tanvi Deshpande ,  Yan Zhang

IPC: C07D307/58 ,  C07D213/30

Abstract: The invention provides new aromatic aldehyde compounds that have greater potency in increasing the affinity of Hb for oxygen, greater potency for preventing sickling, and additional pharmacologic properties that ameliorate other symptoms of SCD. The invention further provides methods for treating SCD by providing a subject having SCD with a compound according to the invention.