06-5579. 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: [phone]; fax: [phone]. A signed Confidential Disclosure Agreement will be required to receive copies of the patent applications.

Beta-Amyloid PET Imaging Agents

Description of Technology: Available for licensing and commercial development are two novel classes of compounds useful as radioligands for in vivo imaging of beta-amyloid (Aβ) 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.

In addition to the novel compounds, the invention also includes: (1) A new method of synthesizing the IMPY derivatives, using palladium as a catalyst, (2) methods of imaging beta-amyloid deposits in the brain by in vivo PET, magnetic reasonance imaging (MRI) and other imaging methods involving the use of these compounds, and (3) and methods of labeling these compounds with radiotracers ([11-C] and [18-F]).

Inventors: Lisheng Cai (NIMH), Victor Pike (NIMH), and Robert Innis (NIMH).

Publications:

1. Nichols L, Pike VW, Cai L, Innis RB. (2006) “Imaging and In Vivo Quantitation of beta-Amyloid: An Exemplary Biomarker for Alzheimer's Disease?,” Biol Psychiatry. [E-pub ahead of print].

2. Toyoma H, et al. (2006) “PET imaging of brain with the beta-amyloid probe, [11C]6-OH-BTA-1, in a transgenic mouse model of Alzheimer's disease,” Eur J Nucl Med Mol Imaging. 32(5), 593-600.

3. Cai L, et al. (2004) “Synthesis and Evaluation of Two¹⁸ F-Labeled 6-Iodo-2-(4′-N,N-dimethylamino)phenylimidazo[1,2-a]pyidine Derivatives as Prospective Radioligands for -Amyloid in Alzheimer's Disease,” J Med Chem, 47 (9), 2208-2218.

Patent Status: U.S. Provisional Application filed 21 Apr 2006 (HHS Reference No. E-156-2006/0-US-01).

Licensing Status: Available for non-exclusive or exclusive licensing.

Licensing Contact: Michael Shmilovich; 301/435-5019; [e-mail].

Collaborative Research Opportunity: The NIMH Molecular Imaging Branch is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize Beta-Amyloid PET Imaging Agents. Please contact Suzanne Winfield at [e-mail] for more information.

Carbohydrate-Encapsulated Quantum Dots for Cell-Specific Biological Imaging

Description of Technology: Available for licensing is intellectual property covering carbohydrate-encapsulated quantum dots (QD) for use in medical imaging and methods of making the same. Certain carbohydrates, especially those included on tumor glycoproteins are known to have affinity for certain cell types. One notable glycan used in the present invention is the Thomsen-Freidenreich disaccharide (Galb1-3GalNAc) that is readily detectable in 90% of all primary human carcinomas and their metastases. These glycans can be exploited for medical imaging. Quantum Dots (QDs) are semiconductor nanocrystals (CdSe or CdTe) with detectable luminescent properties. Encapsulating luminescent QDs with target-specific glycans permits efficient imaging of the tissue to which the glycans bind with high affinity. Accurate imaging of diseased cells (e.g., primary and metastatic tumors) is of primary importance in disease management. The inventors describe a method for enhancing the luminescence of carbohydrate-encapsulated QDs by addition of specific functional units in a novel synthesis of hybrid CdTe-based core-shell semiconductor nanocrystals.

Inventors: Joseph Barchi and Sergey Svarovsky (NCI).

Patent Status: PCT Application No. PCT/US03/34897 filed 05 Nov 2003 (HHS Reference No. E-325-2003/0-PCT-01).

Licensing Status: Available for non-exclusive or exclusive licensing.

Licensing Contact: Michael Shmilovich; 301/435-5019; [e-mail].

Collaborative Research Opportunity: The National Cancer Institute, Center for Cancer Research, Laboratory of Medicinal Chemistry is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize carbohydrate-encapsulated quantum dots. Please contact Dr. Melissa Maderia by phone: [phone] or fax: [phone] or e-mail: [e-mail] for more information.

Dated: June 14, 2006.

David R. Sadowski,

Acting Director, Division of Technology Development and Transfer, Office of Technology Transfer, National Institutes of Health.