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Novel Small Molecules to Treat Alzheimer's Disease: Amyloid Beta Channel Blockers with Anti-inflammatory Properties

Posted Jan 05 2012 7:00pm

Description of Invention:
Alzheimer's Disease (AD) is a common, chronic neurodegenerative disease which is thought to be due to the neurotoxic effect of the Amyloid beta (Abeta) peptide. The inventors discovered that Abeta has intrinsic calcium channel activity, and that entry of calcium into neurons through this channel leads to neuronal cell death, playing a role in Alzheimer's Disease pathology. Consistently, Abeta channel blocking drugs act as a “cork” to save neurons from Abeta-dependent cell death. Two potent and efficacious candidate drugs, MRS2481 and its enantiomeric species MRS2485, have been discovered. Both block the Abeta channel with similar potency (ca. 500 nM) and efficacy (100%). However, inhibition by MRS2481 is easily reversible, while inhibition by MRS2485 is virtually irreversible.

Candidate compounds for Alzheimer's disease drug discovery.

Although no cause or cure is currently known, targeting Ca2+ dyshomeostasis as an underlying and integral component of AD pathology may result in novel and effective treatments for AD.

Development Status:

Kenneth A Jacobson (NIDDK)

Patent Status:
HHS, Reference No. E-264-2003/0
US, , Patent No. 7,893,094, Issued 22 Feb 2011

National Phase filings are pending in Europe, Australia, and Canada

Relevant Publication:
  1. Diaz JC, et al. [ PMID 19204293 ]

Collaborative Research Opportunity:
The National Institute of Diabetes and Digestive and Kidney Diseases is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate or commercialize a small molecule drug to treat Alzheimer's Disease. For collaboration opportunities, please contact Marguerite J. Miller, M.B.A. at 301-496-9003 or .

For Licensing Information Please Contact:
Betty Tong Ph.D.
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Phone: 301-594-6565
Fax: 301-402-0220

Ref No: 2347

Updated: 01/2012

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