Batrachotoxin analogues, compositions, uses, and preparation thereof

US9090627B2 · kind B2 · utility

Assignee

• The Board of Trustees of the Leland Stanford Junior University · US

Inventors

• Justin Du Bois · Stanford, US
• Abigail Sloan Devlin · Cambridge, US
• Matthew M. Logan · San Mateo, US
• Frederic Menard · Menlo Park, US
• Tatsuya Toma · Palo Alto, US

Key dates

• Filing date: Dec 13, 2013
• Grant date: Jul 28, 2015
• Expiry date: Dec 13, 2033

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D498/08
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Compounds relating to batrachotoxin are provided, in particular analogs that modulate the activity of sodium channels. Also provided are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier, including vehicles that modulate transdermal permeation of the compound. The subject compounds are useful in treatments, including treatments to reduce neuronal activity or to bring about muscular relaxation. The compounds also find use in the treatment of subjects suffering from a voltage-gated sodium channel-enhanced ailment or from pain. Further methods are provided for the preparation of the batrachotoxin-related compounds.