[Federal Register Volume 72, Number 133 (Thursday, July 12, 2007)]
[Notices]
[Pages 38087-38088]
From the Federal Register Online via the Government Publishing Office [www.gpo.gov]
[FR Doc No: E7-13541]
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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.
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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.
Compounds Binding to the N-Terminal Domains of STAT Proteins as
Therapeutic Agents
Description of Technology: Signal transducer and activator
transcription (STAT) proteins, specifically STAT1, 2, 3, 4, 5a, 5b, and
6, are involved in the cellular and biological processes of cell
proliferation, differentiation, apoptosis, host defense, and
transformation. Constitutively active STAT proteins occur in many human
tumor cells and cells transformed by oncoproteins. Inhibiting these
STAT proteins has great therapeutic potential in the treatment of
certain cancers.
The current invention describes a family of short peptides that
bind to the N-terminus domains of STAT proteins and their use as
therapeutic agents. These compounds are the first inhibitors that can
directly bind to N-domains of STATs and exhibit a direct inhibitory
effect. STAT1, 3, and 5 inhibitors can serve as potent therapeutic
agents for the treatment of a variety of tumors and STAT 4 inhibitors
can be used to control autoimmune disorders.
Applications and Modality: Other applications for this technology
include using STAT1, STAT3 and STAT5 inhibitors for the treatment of
various tumors; using STAT4 inhibitors to control autoimmune disorders;
and using STAT inhibitors as research tools to study the function of
STAT proteins.
Market: There were approximately 600,000 deaths from cancer related
diseases estimated in 2006. In 2006, the cancer drug market was
estimated to be $25 billion.
Development Status: The technology is currently in the pre-clinical
stage of development.
Inventors: Nadya I. Tarasova et al. (NCI).
Relevant Publications: A manuscript directly related to the above
technology will be available as soon as it is accepted for publication.
Patent Status: U.S. Provisional Application No. 60/940,916 filed 30
May 2007 (HHS Reference No. E-164-2007/0-US-01).
Licensing Status: Available for exclusive and non-exclusive
license.
Licensing Contact: Adaku Nwachukwu, J.D.; 301/435-5560;
[email protected].
Benztropinamine Analogs as Dopamine Transport Inhibitors
Description of Technology: Dopamine is a neurotransmitter that is
directly involved in motor activity, motivation and reward, and
cognition. The dopamine transporter is expressed on the plasma membrane
of dopamine neurons and is responsible for clearing dopamine released
into the extracellular space, thereby regulating neurotransmission. The
dopamine transporter plays a significant role in neuropsychiatric
diseases, such as Parkinson's disease, drug abuse (especially cocaine
addiction), Attention Deficit Disorder/Attention Deficit Hyperactivity
Disorder (ADD/ADHD), narcolepsy and a number of other CNS disorders.
Therefore, the dopamine transporter is a target for research and
potential therapeutics for the treatment of these indications.
Benztropine and its analogs are an important class of dopamine
transport
[[Page 38088]]
inhibitors that are indicated for the treatment of cocaine abuse and
ADHD. They bind with high affinity to the dopamine transporter and
block dopamine uptake, but generally do not produce behavioral effects
comparable to those produced by cocaine. In animal models of drug
abuse, many benztropine analogs have been shown to (1) Reduce cocaine-
induced locomotor stimulation, (2) have long-lasting effects, and (3)
lack a significant abuse liability. This suggests they may be useful
medications for the treatment of human diseases where dopamine-related
behavior is compromised, especially in situations in which an (partial)
agonist treatment is indicated.
However, some of the reported analogs have limited or poor
solubility in aqueous systems or poor stability characteristics. To
remedy this, the 3-position benzhydrylether moiety of the benztropine
analogs was replaced with the isosteric benzhydrylamine system in order
to reduce hydrolysis of the less stable ether function, observed in the
benztropine series, and further reduce lipophilicity to ultimately
increase water solubility and bioavailability for improved therapeutic
formulation and utility.
Inventors: Amy H. Newman et al. (NIDA).
Publication: P Grundt; TA Kopajtic, JL Katz, AH Newman. N-8-
substituted-benztropinamine analogs as selective dopamine transporter
ligands. Bioorg Med Chem Lett. 2005 Dec 15;15(24):5419-5423.
Patent Status: U.S. Provisional Application No. 60/689,746 filed 10
Jun 2005 (HHS Reference No. E-089-2005/0-US-01); International
Application No. PCT/US2006/22401 filed 07 Jun 2006, which published as
WO 2006/135715 on 21 Dec 2006 (HHS Reference No. E-089-2005/0-PCT-02).
Licensing Status: Available for exclusive or non-exclusive
licensing.
Licensing Contact: Tara L. Kirby, Ph.D.; 301/435-4426;
[email protected]
Dated: July 5, 2007.
Steven M. Ferguson,
Director, Division of Technology Development and Transfer, Office of
Technology Transfer, National Institutes of Health.
[FR Doc. E7-13541 Filed 7-11-07; 8:45 am]
BILLING CODE 4140-01-P