Texas Tech University System

Research Triangle Institute

Nadezhda German

Yanan Zhang

Thuy Nguyen

Wei Wang

Luca Cucullo

Ruwein Zhang

Mikelis Constantinos

Mohammad Anwar Hossain

Constantinos Mikelis

The present invention provides novel diarylurea derivatives (compounds of formula (I)) and their uses. The compounds of the present invention are demonstrated to be allosteric modulators of the CB1 receptor, and therefore useful for the treatment of diseases and conditions mediated by CB1.

Diarylureas as CB1 allosteric modulators

Disclosed is a composition and method for a therapeutic treatment that is able to combat triple negative breast cancers (TNBCs). The class of urea compounds acts by blocking at inhibiting the mTOR signaling pathway, which, as a central regulator of mammalian metabolism and physiology that when inhibited leads to the induction of autophagocytosis. The disclosed compounds are further capable of reinitiating the p53 cycle as well as inhibition of the BNIP3/BNIP3L pathway. The disclosed compounds also shows the ability to cross the blood-brain-barrier where metastases can form. This new drug has the potential to be a powerful new treatment to combat invasive TNBCs.

Substituted bisphenylalkylurea compounds and methods of treating breast cancer

Disclosed is a composition and method for a therapeutic treatment that is able to combat neuroinflammation caused by diseases and disorders such as Alzheimer's disease, Parkinson's disease, and traumatic brain injury. The class of urea compounds acts by blocking at targeted receptors in the brain that contribute to the increase in inflammation. Combinations of receptors, H1 receptor, H2 receptor, dopamine transporter (DAT), and/or 5HT3C receptor, are individually and/or collectively inhibited by the same compositions of the present disclosure, and this ability leads to a decrease in brain edema. The DAT inhibitory effects additionally maintains dopamine levels in a patient.

Substituted bisphenylalkylurea compounds and methods

Disclosed is a composition and method for a therapeutic treatment that is able to combat certain conditions such as alcohol dependence, opioid abuse treatment, neurological disorders, neuropathic pain, and fibromyalgia. The novel gliotoxin analog compound acts by acting as an antagonist to one or more opioid receptors, which, when present leads to the inhibition of conditions, providing increased performance over known treatments. The disclosed compounds also shows the ability to cross the blood-brain-barrier in a highly efficient manner.

Growing community of inventors

Amarillo, TX, United States of America

Nadezhda German