Virginia Commonwealth University

The Children's Hospital of Philadelphia

King Abdulaziz University

Illexcor Holdings, LLC

Yan Zhang

Martin K Safo

Dana E Selley

Osheiza Abdulmalik

William Dewey

Jurgen Venitz

Mohini Ghatge

Tanvi Deshpande

Guoyan Xu

Kurt F Hauser

Abdelsattar Mansour Omar

Moustafa Elsayed El-Araby

Richmond E Danso-Danquah

Moustafa El-Sayed El-Araby

Hu Yang

Hamid Akbarali

Hamid Abkarali

Dwight A Williams

Piyusha Pradeep Pagare

Richmond Danso-Danqua

Andrew Fleischman

David Light

Abdelsattar Mansour Ebid Omar

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).

Benzaldehyde compounds with direct polymer destabilizing effects to treat sickle cell disease

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).

Nanoparticle conjugated synthetic opioid prodrugs and methods of their uses

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 based on vanillin which is chemically modified to increase bioavailability and activity, e.g. so that the compounds bind to the F helix of hemoglobin (Hb) and prevent adhesion of red blood cells (RBCs).

Aromatic aldehydes with sustained and enhanced in vitro and in vivo pharmacologic activity to treat sickle cell disease

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.

Non-peptide opioid receptor modulators

Analogues of 6 &#x3b1;/&#x3b2;-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.

Potent and selective mu opioid receptor modulators

Prodrugs and derivatives of 5-hydoxymethyl-2-furfural (5-HMF) with protected or modified aldehyde and/or alcohol moieties are provided. The prodrugs or derivatives exhibit increased bioavailability, e.g. due to having extended half-lives in circulation. The drugs are therefore administered i) at lower doses and/or ii) less frequently than 5-HMF, while still maintaining the beneficial therapeutic effects of 5-HMF.

Prodrug and protected forms of 5-hydroxymethylfurfuranal (5-HMF) and its derivatives

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.

Ester nitrates derivatives of aromatic aldehydes with multiple pharmalogic properties to treat sickle cell disease

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. 

Azolylacryloyl derivatives as therapeutic agents for sickle cell disease

A family of compounds which function as selective ligands for the serotonin receptor 2B (5-HT) 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-HT). Because the compounds, both naturally occurring and synthetically produced, function as ligands for 5-HTthey will have application in, for example, the treatment and/or prevention of nervous system disorders such as Alzheimer's disease.

2-substituted-5-hydroxy-4H-chromen-4-ones as novel ligands for the serotonin receptor 2B (5-HT2B)

Bivalent ligands that contain two pharmacophores linked through a spacer, one of which interacts with the &#x3bc;-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.

Bivalent ligands for the treatment of neurological disorders

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).

Non-peptidyl, potent, and selective mu opioid receptor antagonists and their use in treating opioid addiction and opioid induced constipation

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.

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Glen Allen, VA, United States of America

Yan Zhang