Description of Invention:
The A3 adenosine receptor (A3AR) subtype has been linked with helping protect the heart from ischemia, controlling inflammation, and regulating cell proliferation. Agonists of the human A3AR subtype have been described; however, they lack selectivity for the corresponding receptor of the mouse. This poses a problem for clinical development because animal model testing is important for pre-clinical validation of drug function. Consequently, a novel agonist was made that is selective for the mouse A3AR while retaining selectivity for the human receptor. This innovation should facilitate moving A3 agonists into the clinical phase of drug development with confidence.
This invention claims species-independent agonists of A3AR, specifically (N)-methanocarba adenine nucleosides. In addition, it describes pharmaceutical compositions comprising such nucleosides, and methods of use such as administering an effective amount to a mammal.
Applications:
cardiac arrhythmias or ischemia
inflammation
stroke
diabetes
asthma
cancer
Market:
Heart disease and cancer are the leading causes of death for both women and men in the United States despite many advances in drug development. Hence, there is a need for drugs with unique mechanism of action. It is noteworthy that the first synthetic adenosine receptor agonist has recently been approved for use in humans.
Development Status:
Research quantities of compounds have been synthesized and tested for receptor selectivity.
Patent Status:
DHHS Reference No. E-140-2008/0 --
U.S. Provisional Application No. 61/040,985 filed 31 Mar 2008
Relevant Publication: A Melman et al. Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists. Bioorg Med Chem Lett. 2008 May 1;18(9):2813-2819. [PubMed abs]
Licensing Status: Available for exclusive or non-exclusive licensing.
