Beta-Amyloid and Tau Fibril Positron Emissions Tomography (PET) Imaging Agents


The invention relates to two novel classes of compounds useful as radioligands for in vivo imaging of beta-amyloid fibrils, peptides and plaques in humans. Beta-amyloid peptide deposition in the brain is a pathological feature of Alzheimer's disease (AD). Early detection of beta-amyloid load in patients with suspected AD is vital to initiating early treatment, which can improve cognitive function and quality of life for many patients. The invention describes novel derivatives of imidazopyridinylbenzeneamine (IMPY) and benzothizolylbenzeneamine (BTA), which demonstrate high in vitro binding affinity to human beta-amyloid. The difference between existing IMPY compounds and the novel derivatives is the substitution of an aryl halide with an aryl thioether group and replacement of a sulfur group of the pyridine ring with a nitrogen group. The new classes of compounds have the potential of providing improved amyloid imaging agents for Positron Emission Tomography (PET) with higher specificity for amyloid, low background noise, better entry into the brain and improved labeling efficiency.

diagram of radioligand structure



Potential Commercial Applications: Competitive Advantages:
  • Alzheimer's disease
  • Alzheimer's disease diagnostics
  • Alzheimer's disease early detection
 
  • Specificity


Related Inventoion(s):
E-136-2008/0
E-225-2011/0
E-225-2011/1


Inventors:
Lisheng Cai (NIMH)
Victor Pike (NIMH)
Robert Innis (NIMH)


Intellectual Property:
US Application No. 14/223,782
US Application No. 12/293,340
PCT Application No. PCT/US2007/066939
US Application No. 60/793,807

Publications:
Nichols L, et al. PMID 16487944
Toyama H, et al. PMID 15791432
Cai L, et al. PMID 15084119

Collaboration Opportunity:

The National Institute of Mental Health is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate or commercialize Alzheimer's disease diagnostics. For collaboration opportunities, please contact Suzanne Winfield, Ph.D. at 301-402-4324.


Licensing Contact:
Michael Shmilovich , J.D.
NIH Office of Technology Transfer
Email: shmilovm@mail.nih.gov
Phone: 301-435-5019

OTT Reference No: E-156-2006/0

Updated: Feb-28-2014