Technology Overview

The present invention comprises a novel series of potent inhibitors of AMP-activated protein kinase AMPK around the lead compound TUG-1874, the most selective AMPK inhibitor known to date.

Tools to enhance AMPK activity are extensively investigated. However, the development of tools to reduce AMPK activity has previously been neglected. Selective inhibitors of AMPK like TUG-1874 are crucial tools to evaluate AMPK as drug target and will enable the discovery of new therapeutics to treat AMPK-dependent diseases with a high socio-economic impact. These diseases include but are not limited to obesity, type 2 diabetes and other metabolic disorders (). Certain types of cancer, including drug-resistant brain tumors, are potential targets for AMPK inhibitors.

The invention comprises a series of small molecules designed to enable the development of therapeutics for oral administration. As such, the current lead compound TUG-1874 displays drug-like properties.

Stage of Development

Established synthesis routes enable fast exploration of the compound series and established biological assays enable fast characterisation of new compounds. Further optimization of potency is currently a major focus while retaining the excellent target selectivity profile.

Moreover, studies of the lead TUG-1874 in diverse biological systems are currently ongoing to explore its potential as a tool compound. In addition, a procedure for large-scale synthesis of TUG-1874 has been developed.

Opportunity

SDU offer out-licensing of TUG-1874. SDU can provide supporting data on selectivity and potency, SOP’s for chemical synthesis and access to the chemists who invented the compound as well as TUG-1874 in significant amounts for initial assessment and even first sales.

In Control of Metabolism - New Selective Inhibitors Targeting the Master Energy Switch AMPK

Patents

IP Status

Seeking