04-20293. Government-Owned Inventions; Availability for Licensing

AGENCY:

National Institutes of Health, Public Health Service, DHHS.

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.

Integrin Alpha-V Beta-3 Antagonists for Use in Imaging and Therapy

S. Narasimhan Danthi et al. (CC), U.S. Patent Application filed 04 Aug 2004 (DHHS Reference No. E-170-2004/0-US-01).

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

Available for licensing are compounds as shown below for imaging and therapy. These compounds are integrin αvβ3 receptor antagonists and are described and claimed in a patent application available for review. The patent application also includes claim coverage for the administration of these compounds containing a detectable moiety or pharmaceutical compositions of such imaging agents as part of the imaging of cells that express integrin αvβ3.

In which: X is either NH, O, or S; n is zero or a positive integer; R₁ is either CH₂, NH, O, or S; R₂ is either CHR₇, NR₇, O, or S, in which R₇ is H or alkyl; R₃ and R₄, which are either the same or different from each other, are either H, alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, alkyl-substituted aryl, (alkylsubstitutedaryl)alkyl, hydroxy-substituted alkyl, hydroxy-substituted aryl, or (hydroxy-substituted aryl)alkyl; R₅ is either CH₂, NH, O, or S; and R₆ is either H or C(=Y)-R₈-R₉, in which: Y is either NH, O, or S; R₈ is either CHR₁₀, NR₁₀, O, or S, in which R₁₀ is H or alkyl; and R₉ is either H, alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, alkylsubstituted aryl, (alkyl-substituted aryl)alkyl, hydroxy-substituted alkyl, hydroxy-substituted aryl, or (hydroxy-substituted aryl)alkyl.

Use of Protein Kinase C Delta Inhibitor, Specifically Rottlerin, Alone or in Further Combination With Staurosporine, in the Treatment of Metastatic Epithelioid Melanoma

Denise Simmons (NCI), U.S. Provisional Application No. 60/531,876 filed 22 Dec 2003 (DHHS Reference No. E-311-2003/0-US-01).

Licensing Contact: Mojdeh Bahar; 301/435-2950; [e-mail].

This invention is directed to the use of a protein kinase C delta inhibitor, specifically rottlerin, alone or in further combination with staurosporine, in the treatment of metastatic epithelioid melanoma. Preliminary studies show that treatment of cells from a metastasized human epithelioid melanoma with rottlerin reduced cellular proliferation by 90%, without affecting proliferation or morphology of normal melanocytes. Cells from the matched primary site tumor of the same patient were not affected by this inhibitor, nor were cells from a matched tumor pair of fibroblastoid morphology obtained from a second patient. Treatment of cells from a metastasized human epithelioid melanoma with staurosporine caused an increase in branching and in the number of processes in the melanoma cells, without affecting cell number. These staurosporine-induced changes may be indicative of differentiation.

Dated: August 27, 2004.

Steven M. Ferguson,

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