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N-Methanocarba Adenosine Derivatives and Their Dendrimer Conjugates as A3 Receptor Agonists

Posted Aug 10 2010 5:00pm

Description of Invention:
This technology relates to specific (N)-methanocarba adenine nucleosides that have been developed and dendrimers that connect these compounds to create molecules with multiple targets. Dendrimers are essentially repeated molecular branches presenting the core receptor-binding molecules. The compounds synthesized function as agonists and antagonists of a receptor of the G-protein coupled receptor (GPCR) superfamily. In particular, the receptors of interest for this invention include A3 adenosine receptors and agonists and antagonists of P2Y receptors, such as P2Y1 and P2Y14.

Dendrimer conjugates may have one or more advantages, such as increased solubility, reduced toxicity, and improved pharmacokinetic properties. They can also be used to connect other types of molecules without affecting the agonist or antagonists properties. For instance, molecules such as those used for imaging or tracing can be added. Dendrimers can also be used to link more than one type of agonist or antagonist to confer multiple functionalities. This technology provides a novel mechanism to treat a number of disorders related to dysregulation of A3 adenosine receptors.

  • cardiac arrhythmias or ischemia
  • inflammation
  • stroke
  • diabetes
  • asthma
  • cancer
  • imaging

Development Status:
Research quantities of compounds have been synthesized and tested for receptor selectivity.

Kenneth A Jacobson (NIDDK)
Dilip K Tosh (NIDDK)

Patent Status:
HHS, Reference No. E-049-2010/0
US, Application No. 61/266,084 filed 02 Dec 2009
US, Application No. 61/313,961 filed 15 Mar 2010

Licensing Status:
Available for licensing.

Collaborative Research Opportunity:
The National Institute of Diabetes and Digestive and Kidney Diseases, Laboratory of Bioorganic Chemistry, Molecular Recognition Section, is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize this technology. Please contact Dr. Kenneth Jacobson at for more information.

Internal Medicine
Internal Medicine - Diagnostics
Internal Medicine - Therapeutics
Ophthalmology - Therapeutics

For Licensing Information Please Contact:
Steven Standley Ph.D.
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Phone: 301-435-4074
Fax: 301-402-0220

Ref No: 2143

Updated: 08/2010

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