[Federal Register Volume 83, Number 143 (Wednesday, July 25, 2018)]
[Notices]
[Pages 35279-35280]
From the Federal Register Online via the Government Publishing Office [www.gpo.gov]
[FR Doc No: 2018-15907]


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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, HHS.

ACTION: Notice.

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SUMMARY: The invention listed below is jointly owned by an agency of 
the U.S. Government with Vanderbilt University, University of Alabama 
and University of Pennsylvania and is available for licensing 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.

FOR FURTHER INFORMATION CONTACT: Licensing information and copies of 
the U.S. patent application listed below may be obtained by 
communicating with Sury Vepa, Ph.D., J.D., Senior Licensing and 
Patenting Manager,

[[Page 35280]]

National Center for Advancing Translational Sciences, NIH, 9800 Medical 
Center Drive, Rockville, MD 20850, Phone: 301-827-7181, or email 
[email protected]. A signed Confidential Disclosure Agreement will be 
required to receive copies of unpublished patent applications.

SUPPLEMENTARY INFORMATION: Technology description follows.

Thiazole Based Inhibitors of Lactate Dehydrogenase (LDH) for the 
Treatment of Cancer

    Description of Technology: Agents that target enzymes involved in 
cancer cell metabolism offer an attractive therapeutic route in view of 
the potential to preferentially target cancer tissue over normal 
tissue. While normal tissue typically uses glycolysis as a major 
cellular metabolic path only when the oxygen supply is low, cancer 
tissue relies heavily on aerobic glycolysis regardless of the oxygen 
supply level. In addition, metabolic switching to a more glycolytic 
phenotype is a required step with inflammatory cells and other 
pathologies which require activated glycolysis in their metabolism. 
Lactate dehydrogenase (LDH) is involved in the final step of 
glycolysis, in which pyruvate is converted to lactate and the 
conversion of NADH to NAD+. There are two different genes of LDH, LDHA 
and LDHB, but both proteins (subunits) have the same active site and 
catalyze the conversion of pyruvate to lactate or lactate to pyruvate. 
In cancer patients, serum total lactate dehydrogenase (levels are often 
increased, and the gene for LDH, is up-regulated. LDH inhibition is 
expected to reduce the ability of the cell to effectively metabolize 
glucose and reduce tumor cell proliferation and tumor growth and other 
pathologies which involve a glycolytic metabolic switch. Thus, 
compounds that inhibit LDH activity have potential for the development 
of anti-cancer therapeutics. Previously developed LDH inhibitors have 
significant drawbacks, including poor potency and/or poor 
bioavailability, limiting their utility as therapeutics. The present 
technology provides novel 1 H-PYRAZOL-1 -YL-THIAZOLE based LDH 
inhibitors with improved potency, selectivity, and/or bioavailability 
for the treatment of cancer.
    This technology is available for licensing for commercial 
development in accordance with 35 U.S.C. 209 and 37 CFR part 404, as 
well as for further development and evaluation under a research 
collaboration.
    Potential Commercial Applications:
     Novel therapeutics for cancer AND indications which depend 
on a metabolic switch to glycolysis (e.g., inflammation, autoimmune 
disease, etc.)
    Competitive Advantages:
     Novel LDH inhibitors with improved potency, selectivity, 
and/or bioavailability for the treatment of cancer.
    Development Stage:
     Optimized lactate dehydrogenase inhibitors are in pre-
clinical development.
    Inventors:
     David J. Maloney, Alex Gregory Waterson, Ganesha Rai 
Bantukallu, Kyle Ryan Brimacombe, Plamen Christov, Chi V. Dang, Victor 
M. Darley-Usmar, Matthew Hall, Xin Hu, Ajit Jadhav, Somnath Jana, 
Kwangho Kim, William J. Moore, Brian T. Mott, Leonard M. Neckers, Anton 
Simeonov, Gary Allen Sulikowski, Daniel Jason URBAN, and Shyh Ming 
Yang.
    Publications: This manuscript reports early compounds in the 
series: https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b00941.
    Intellectual Property: 1. SMALL MOLECULE INHIBITORS OF LACTATE 
DEHYDROGENASE AND METHODS OF USE THERE OF, PCT/US2015/067895 filed on 
December 29, 2015 and published as WO 2016/109559 on July 7, 2016 (HHS 
Ref. No. E-244-2014), and
    2. 1 H-PYRAZOL-1 -YL-THIAZOLES AS INHIBITORS OF LACTATE 
DEHYDROGENASE AND METHODS OF USE THERE OF, PCP/US2017/040021 filed on 
June 29, 2017 and published as WO 2018/005807 on January 8, 2018 9HHS 
Ref. No. E-190-2016).
    Related Intellectual Property: HHS Reference Number E-293-2011.
    Licensing Contact: Sury Vepa, Ph.D., J.D., 301-827-7181; 
[email protected].

    Dated: July 5, 2018.
Lili Portilla,
Technology Development Coordinator, National Center for Advancing 
Translational Sciences.
[FR Doc. 2018-15907 Filed 7-24-18; 8:45 am]
 BILLING CODE 4140-01-P