The technology is a series of modafinil analogues that bind with moderate to high affinity to the dopamine (DA) transporter (DAT). Some compounds also have affinity for the serotonin (5-HT) transporter (SERT) and/or sigma-1 receptor. The compounds retain the desired dopamine transporter affinity with greater metabolic stability over previously described unsubstituted piperazine ring analogues. Importantly, these compounds have no predicted addictive liability. Also disclosed are methods for treating substance use disorders as well as other neuropsychiatric disorders such as ADHD, depression, narcolepsy, and cognitive impairment. Researchers at the National Institute on Drug Abuse (NIDA) seek licensing and/or co-development research collaborations for further development and commercialization of the compounds.
Scientists at the National Institute on Drug Abuse (NIDA) have developed novel dopamine D3 receptor (D3R) agonists with high affinity and selectivity. Two lead compounds, 53 and eutomer 53a, have demonstrated significantly higher D3R binding selectivity than reference compounds. Moreover, 53 and 53a showed metabolic stability in liver microsomes, which is favorable for the future use of these compounds as therapeutic agents for diseases related to dopamine system dysregulation such as Parkinson’s Disease and Restless Legs Syndrome. Researchers at NIDA seek licensing and/or co-development research collaborations for the use of these D3R agonists as molecular tools for the study of D3R physiology and as potential therapeutics to treat neurological and neuropsychiatric disorders.
The National Cancer Institute (NCI) seeks research co-development partners and/or licensees for Leucine Zipper-bearing Kinase (LZK) -targeting proteolysis-targeting chimeras (PROTACs) as a therapeutic for treating head and neck, lung and ovarian squamous cell carcinoma, as well as small cell lung cancers which over-express LZK.
Investigators at the National Center for Complimentary and Integrative Health (NCCIH) and the University of Tennessee Health and Science Center have shown that administration of margaric acid can ameliorate pain induced by a variety of noxious stimuli in mice. In vitro and ex vivo studies in human and murine neural cells indicate that the mechanism of action of margaric acid is mediated by PIEZO2 (Piezo-type mechanosensitive ion channel component 2) function. NCCIH seeks research co-development partners and/or licensees for methods of using the fatty acid, margaric acid to treat pain.
A library of novel compounds that selectively bind the dopamine D3 receptor have been designed and characterized extensively. In vivo rodent studies indicate selected lead molecules may be useful to treat drug addiction/dependence.
The National Cancer Institute (NCI) seeks licensing and/or co-development research collaborations for a polymeric drug delivery platform that targets scavenger receptor A1 (SR-A1), a receptor highly expressed in macrophages, monocytes, mast cells, dendritic cells (myeloid lineages), and endothelial cells. The platform delivers various immunomodulatory therapeutic cargo including small molecule drugs, therapeutic peptides, and vaccines, to the lymphatic system and myeloid/antigen presenting cell (APC) sub-populations.
The National Cancer Institute (NCI) seeks research co-development partners and/or licensees for small molecules that inhibit histone lysine demethylases (KDMs). These compounds may be effective therapeutics for Rhabdomyosarcoma (RMS) and other cancers.
The Section on Translational Neuroscience of NICHD seeks parties interested in licensing and/or collaborative research to co-develop this therapeutic management of Menkes Disease and related copper transport disorders.