US 2019/0160021 A1 · Substituted Stilbenes as Inhibitors of NF-kappaB and Activators of Nrf2

Abstract

The present invention relates to substituted stilbenes and dienones which exhibit unexpected dual activity, as inhibitors of NFκB and as agonists (activators) of Nrf2. In particular, these compounds show dual activity and makes them particularly useful in the treatment of inflammation, including chronic inflammation and a number of related chronic disease states and conditions, including neurological diseases, including Alzheimer's, Alzheimer's prodrome and mild cognitive impairment, and other diseases and conditions, such as Parkinson's disease, depression, bipolar disorders and autism spectrum disorders. Compounds, pharmaceutical compositions and methods of treatment are described.

Claims21

Dependent claims

A method of a treating a subject afflicted with a disease or condition which is modulated through upregulation of NF-κB signaling and inhibition of Nrf2 signalling, the method comprising administering to the subject a composition comprising a therapeutically effective amount of at least one compound which exhibits dual activity as a NF-κB signaling inhibitor and a Nrf2 signaling agonist, optionally in combination with at least one additional bioactive agent.

A pharmaceutical composition comprising an effective amount of a compound according to the chemical structure:

or
a pharmaceutically acceptable salt thereof, or a mixture thereof in combination with a pharmaceutically acceptable carrier, additive and/or excipient.

Dependencies are inferred from the claim text.

Substituted Stilbenes as Inhibitors of NF-kappaB and Activators of Nrf2

Life of this patent

Substituted Stilbenes as Inhibitors of NF-kappaB and Activators of Nrf2

Life of this patent

Abstract

Claims21