公开(公告)号：US11458144B1

公开(公告)日：2022-10-04

申请号：US17560795

申请日：2021-12-23

Applicant: King Abdulaziz University ,  The Children's Hospital of Philadelphia ,  Virginia Commonwealth University

Inventor： Moustafa E. El-Araby ,  Abdelsatter M. Omar ,  Osheiza Abdulmalik ,  Martin K. Safo

IPC: A61K31/5377 ,  A61K31/341 ,  A61K31/4155 ,  A61P7/06 ,  A61K31/496 ,  A61K31/351 ,  A61K31/4525

Abstract: Methods for administering compounds provide a rapid treatment for sickle cell disease (SCD) to inhibit or reverse red blood cell sickling. The compounds are a group of 5-hydroxymethylfurfural (5-HMF) analogs modified to increase water-solubility. The compounds can be formulated in an aqueous carrier and administered intravenously for immediate uptake into red blood cells (RBCs) within hours, rather than days or weeks. In vitro experiments demonstrated rapid uptake into RBCs and increased O2 affinity of HbS to an equilibrium point within 30 to 90 minutes. The compounds have a desired level of safety as well as a short half-life, both of which are compatible with acute usage. Thus, the methods of treatment rapidly achieve therapeutic steady-state drug levels, making it possible to deliver a treatment in critical emergency care situations to prevent, reverse and otherwise treat acute sickling or anemia.

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：US12065408B2

公开(公告)日：2024-08-20

申请号：US18386724

申请日：2023-11-03

Applicant: VIRGINIA COMMONWEALTH UNIVERSITY ,  IIIExcor Holdings, LLC ,  KING ABDULAZIZ UNIVERSITY ,  CHILDREN'S HOSPITAL OF PHILADELPHIA (CHOP)

Inventor： Martin Safo ,  Yan Zhang ,  Andrew Fleischman ,  David Light ,  Moustafa El-Araby ,  Abdelsattar Omar ,  Osheiza Abdulmalik

IPC: C07D213/30 ,  A61P7/06 ,  C07D239/26

CPC classification number: C07D213/30 ,  A61P7/06 ,  C07D239/26

Abstract: Compounds and methods for preventing and/or treating one or more symptoms of sickle cell diseases (SCD) by administering at least one of the compounds are provided. The compounds are chemically modified to increase bioavailability and activity, e.g., so that the compounds prevent adhesion and sickling of red blood cells (RBCs).

公开(公告)号：US20180282287A1

公开(公告)日：2018-10-04

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: C07D233/58 ,  C07D405/12 ,  A61P7/00

CPC classification number: C07D233/58 ,  A61K31/4174 ,  A61K31/4178 ,  A61P7/00 ,  C07D233/64 ,  C07D405/12

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.