This technology is a series of selective phosphodiesterase 4 (PDE4) inhibitors for treating memory impairment in Alzheimer’s Disease (AD).
There are currently only a limited number of drugs available to attenuate memory deficits in AD. These drugs offer limited efficacy and have severe side effects. Recent research suggests that phosphodiesterase (PDE) inhibitors, notably PDE4, may be a promising target for the treatment of a variety of cognitive deficits and, in particular, memory impairment. Rolipram (a well-known unselective PDE4 inhibitor) is able to reverse the beta-amyloid induced dysfunction to ameliorate cognitive deficits in mouse models. However, despite the potential clinical relevance, the therapeutic use of Rolipram is limited because of its major side effect of emesis. Currently, there are no selective PDE4 inhibitors available on the market.
This technology identifies several compounds that are capable of selectively inhibiting PDE4 activity. These compounds are selective for the type D isoform of PDE4, which is expressed in the hippocampus and cortex and has been implicated in AD-related memory deficits. As a result, these compounds are able to improve cyclic adenosine monophosphate (cAMP) release in hippocampi without the side effects associated with unselective inhibition of PDE4. These compounds, therefore, offer a potent therapeutic strategy for preventing memory loss in AD.
This technology has been validated in vivo in rodent models of AD.
IR CU13335
Licensing Contact: Ron Katz
