Technologies
PDF


WARF: P150023US03

Synthesizing Natural Products to Treat High Blood Cholesterol


INVENTORS -

Weiping Tang, Dongxu Shu, Gabrielle Winston-McPherson, Xiaoxun Li

The Wisconsin Alumni Research Foundation (WARF) is seeking commercial partners interested in developing indole compounds to treat health problems associated with high blood cholesterol.
OVERVIEWIndole is one of the most abundant heterocycles in pharmaceuticals and bioactive natural products, such as indometacin, a non-steroid anti-inflammatory drug, and vincristine, a natural product used to treat a number of types of cancers. Given the importance of indoles, much effort has been devoted to preparing them from a variety of starting materials. However, inefficiency, low selectivity and low yield remain a problem for polysubstituted indoles or when the indole is in a complex polycyclic system.
THE INVENTIONUW–Madison researchers have developed an efficient method to synthesize indole compounds, specifically polysubstituted dimeric indoles. These compounds have potential health benefits because they are able to reduce the amount of PCSK9 in cells. PCSK9 is an enzyme known to play a major role in controlling the concentration of LDL cholesterol in the bloodstream.

Some of the compounds have been tested in vitro for their ability to increase the secretion of a potent blood sugar hormone in the body called glucagon-like peptide 1 (GLP-1). Others have the ability to selectively inhibit the secretion of interleukin-17 (IL-17), which is essential in many autoimmune diseases including arthritis, multiple sclerosis, psoriasis and inflammatory bowel disease.

The synthesis process involves a cascade reaction with transition metal catalysts. The resulting compounds can be further functionalized to yield more substituted indoles.
APPLICATIONS
  • Synthesizing indole compounds to treat ailments in mammals connected to GLP-1, PCSK9 and/or IL-17
KEY BENEFITS
  • More efficient than other methods
  • Potential health implications are significant – from treating hyperglycemia to high cholesterol and autoimmune diseases.
STAGE OF DEVELOPMENTThe development of this technology was supported by WARF Accelerator. WARF Accelerator selects WARF's most commercially promising technologies and provides expert assistance and funding to enable achievement of commercially significant milestones. WARF believes that these technologies are especially attractive opportunities for licensing.
Contact Information
For current licensing status, please contact Rafael Diaz at rdiaz@warf.org or 608-960-9847.
The WARF Advantage

WARF: A Leader in Technology Transfer Since 1925
Since its founding as a private, nonprofit affiliate of the University of Wisconsin–Madison, WARF has provided patent and licensing services to UW–Madison and worked with commercial partners to transform university research into products that benefit society. WARF intellectual property managers and licensing staff members are leaders in the field of university-based technology transfer. They are familiar with the intricacies of patenting, have worked with researchers in relevant disciplines, understand industries and markets, and have negotiated innovative licensing strategies to meet the individual needs of business clients.

The University of Wisconsin and WARF –
A Single Location to Accelerate Translational Development of New Drugs

UW–Madison has the integrative capabilities to complete many key components of the drug development cycle, from discovery through clinical trials. As one of the top research universities in the world, and one of the two best-funded universities for research in the country, UW–Madison offers state-of-the-art facilities unmatched by most public universities.

These include the Small Molecule Screening Facility at the UW Comprehensive Cancer Center; the Zeeh Pharmaceutical Experiment Station, which provides consulting and laboratory services for developing formulations and studying solubility, stability and more; the Waisman Clinical Biomanufacturing Facility; the Wisconsin Institute for Medical Research, which provides UW–Madison with a complete translational research facility; and the innovative, interdisciplinary Wisconsin Institutes for Discovery, home to the private, nonprofit Morgridge Institute for Research and its public twin, WID, part of the university's graduate school. The highly qualified experts at these facilities are ready to work with you to create a library of candidates for drug development.