University of California

Kansas State University Research Foundation

Afasci, Inc.

Lee-way Jin

Izumi Maezawa

Kit S Lam

Duy H Hua

Ruiwu Liu

Xinmin Xie

Hyun-Seok Hong

Tricyclic pyrone compounds having high oral bioavailability, excellent blood-brain barrier permeability, and low toxicity are presented. Administration of the compounds to Alzheimer's Disease transgenic models resulted in substantially reduced soluble and insoluble A&#x3b2; species in the brain without affecting general behavior and motor coordination. Furthermore, in addition to blocking the toxicity and formation of both intraneuronal and extracellular A&#x3b2; aggregates, the compounds also increase cellular cholesterol efflux, restore axonal trafficking, and enhance hippocampal synaptic plasticity.

Tricyclic pyrone compounds reduce amyloid beta aggregates

In one aspect, the present invention provides for compounds and labeled compounds of Formula I, and pharmaceutical compositions thereof. In another aspect, the present invention provides for methods of using compounds or labeled compounds of Formula I for various therapeutic and imaging purposes, including, but not limited to, treating Alzheimer's disease in patient and imaging A&#x3b2; peptide aggregates in a patient.

A&#x3b2;-binding small molecules

Growing community of inventors

Davis, CA, United States of America

Lee-way Jin