[Federal Register Volume 75, Number 158 (Tuesday, August 17, 2010)]
[Notices]
[Pages 50768-50769]
From the Federal Register Online via the Government Publishing Office [www.gpo.gov]
[FR Doc No: 2010-20274]


-----------------------------------------------------------------------

DEPARTMENT OF HEALTH AND HUMAN SERVICES

National Institutes of Health


Government-Owned Inventions; Availability for Licensing

AGENCY: National Institutes of Health, Public Health Service, HHS.

ACTION: Notice.

-----------------------------------------------------------------------

SUMMARY: The inventions listed below are owned by an agency of the U.S. 
Government and are available for licensing in the U.S. in accordance 
with 35 U.S.C. 207 to achieve expeditious commercialization of results 
of federally-funded research and development. Foreign patent 
applications are filed on selected inventions to extend market coverage 
for companies and may also be available for licensing.

ADDRESSES: Licensing information and copies of the U.S. patent 
applications listed below may be obtained by writing to the indicated 
licensing contact at the Office of Technology Transfer, National 
Institutes of Health, 6011 Executive Boulevard, Suite 325, Rockville, 
Maryland 20852-3804; telephone: 301/496-7057; fax: 301/402-0220. A 
signed Confidential Disclosure Agreement will be required to receive 
copies of the patent applications.

A Novel Scaffold for Multivalent Display of Ligands

    Description of Invention: Multivalent interactions are important in 
cell attachment, wound healing and immune responses. Such interactions 
are associated with cancer metastasis, blood clotting and the 
generation of antibodies from a vaccination. Mimicking multivalent 
interactions on a synthetic scaffold is challenging especially when 
large numbers of ligands (such as 5 or more) need to be displayed. 
There are numerous synthetic scaffolds that have been developed, but 
there are significant limitations that remain.
    Scientists at the NIH have designed a novel multivalent scaffold 
that can display anywhere from 1 to 200 ligands. This system allows 
different types of ligands to be displayed in a controlled, spatially-
addressable manner. This system uses peptide nucleic acids (PNAs) 
containing [gamma]-substituted side

[[Page 50769]]

chains. PNAs are synthetic molecules that possess the bases derived 
from DNA. This invention could revolutionize the way in which 
multivalent display is used in research as well as help make 
vaccinations or prevent disease.
    Applications:
     Controlled interactions ensure only a single stoichiometry 
is attained.
     Simple access to a wide range of multivalent platforms.
    Development Status: Early stage.
    Inventors: Daniel Appella et al. (NIDDK).
    Patent Status: U.S. Provisional Application No. 61/333,442 filed 11 
May 2010 (HHS Reference No. E-129-2010/0-US-01).
    Licensing Status: Available for licensing.
    Licensing Contact: Charlene Sydnor, PhD; 301-435-4689; 
[email protected].
    Collaborative Research Opportunity: The NIDDK Laboratory of 
Bioorganic Chemistry is seeking statements of capability or interest 
from parties interested in collaborative research to further develop, 
evaluate, or commercialize this novel scaffold or to collaborate on 
related laboratory interests. Please contact Marguerite J. Miller at 
301-496-9003 and/or [email protected] for more information.

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

    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.
    Applications:
     Cardiac arrhythmias or ischemia
     Inflammation
     Stroke
     Diabetes
     Asthma
     Cancer
     Imaging
    Development Status: Research quantities of compounds have been 
synthesized and tested for receptor selectivity.
    Inventors: Kenneth A Jacobson and Dilip K. Tosh (NIDDK).
    Patent Status:
    U.S. Provisional Application No. 61/266,084 filed 02 Dec 2009 (HHS 
Reference No. E-049-2010/0-US-01).
    U.S. Provisional Application No. 61/313,961 filed 15 Mar 2010 (HHS 
Reference No. E-049-2010/1-US-01).
    Licensing Status: Available for licensing.
    Licensing Contact: Steven Standley, PhD; 301-435-4074; 
[email protected].
    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 
[email protected] for more information.

Species-Independent A3 Adenosine Receptor Agonists Which May 
Be Useful for Treating Ischemia, Controlling Inflammation, and 
Regulating Cell Proliferation

    Description of Invention: This invention claims species-independent 
agonists of A3AR, specifically (N)-methanocarba adenine 
nucleosides and pharmaceutical compositions comprising such 
nucleosides. 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 developed that are also 
selective for the mouse A3AR while retaining selectivity for 
the human receptor. This solves a problem for clinical development 
because animal model testing is important for pre-clinical validation 
of drug function. Novel agonists have been made that exhibit as much as 
6000x selectivity for A3 versus A1 in humans 
while retaining at least 400x selectivity for A3 versus 
A1 in mice. In addition, the molecules of the invention 
exhibit very low nanomolar affinity. This innovation will not only 
facilitate moving A3 agonists into the clinical phase of 
drug development by being more amenable to animal studies, but also 
provide much greater selectivity in humans, and thereby potentially 
fewer side effects than drugs currently undergoing clinical trials.
    Applications:
     Cardiac arrhythmias or ischemia
     Inflammation
     Stroke
     Diabetes
     Asthma
     Cancer
    Development Status: Research quantities of compounds have been 
synthesized and tested for receptor selectivity.
    Inventors: Kenneth A. Jacobson and Artem Melman (NIDDK).
    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: 
18424135].
    Patent Status: PCT Application No. PCT/US09/38026 filed 24 Mar 
2009, which published as WO 2009/123881 on 08 Oct 2009 (HHS Reference 
No. E-140-2008/0-PCT-02).
    Licensing Status: Available for licensing.
    Licensing Contact: Steven Standley, Ph.D.; 301-435-4074; 
[email protected].
    Collaborative Research Opportunity: The NIDDK Laboratory of 
Bioorganic Chemistry is seeking statements of capability or interest 
from parties interested in collaborative research to further develop, 
evaluate, or commercialize A3 Adenosine Receptor Agonists. 
Please contact Marguerite J. Miller at 301-496-9003 or 
[email protected] for more information.

    Dated: August 11, 2010.
Richard U. Rodriguez,
Director, Division of Technology Development and Transfer, Office of 
Technology Transfer, National Institutes of Health.
[FR Doc. 2010-20274 Filed 8-16-10; 8:45 am]
BILLING CODE 4140-01-P