This technology includes two chemical compounds that are phosphodiesterase type 5 (PDE5) inhibitors with a benzonaphthyridine derivative chemical scaffold that has not previously been used to treat Alzheimer’s disease or other conditions involving phosphodiesterase PDE5 function.
There is currently no cure for Alzheimer’s disease (AD) and current therapeutic options are limited, mainly targeting related symptoms rather than mediating disease progression. Phosphodiesterase (PDE) is an enzyme that breaks phosphodiester bonds and PDE type 5 (PDE5) is found in various tissue types, including the brain. Prior studies have shown that PDE5 inhibition in the brain can improve memory and synaptic plasticity in different AD mouse models. Most importantly, large population studies on people who have been administered PDE5 inhibitors, have shown lowered risk to start Alzheimer’s Disease. Although various PDE5 inhibitors are marketed to treat erectile dysfunction (ED), they are not useful for AD as they have low selectivity or are unable to penetrate the blood brain barrier. There are currently no available compounds or approaches to selectively target PDE5 as a treatment for AD or related conditions.
This technology describes two phosphodiesterase type 5 (PDE5) inhibitors based on a benzonaphthyridine derivative chemical scaffold that has previously not been used for PDE5 inhibition. Compared to current PDE5 inhibitors, these compounds have improved selectivity and efficacy for PDE5 inhibition with an increase in penetrance across the blood brain barrier. Furthermore, these compounds can inhibit other PDE isozymes to further evaluate and assess the impact of PDE inhibition in the brain and the overall effect on memory, plasticity, and in treating conditions such as Alzheimer’s disease.
Patent Issued (US 11,851,427)
IR CU12089
Licensing Contact: Jerry Kokoshka
