[Federal Register Volume 89, Number 67 (Friday, April 5, 2024)]
[Notices]
[Page 24023]
From the Federal Register Online via the Government Publishing Office [www.gpo.gov]
[FR Doc No: 2024-07278]


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

DEPARTMENT OF HEALTH AND HUMAN SERVICES

National Institutes of Health


Government-Owned Inventions; Availability for Licensing

AGENCY: National Institutes of Health, 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. to achieve 
expeditious commercialization of results of federally-funded research 
and development.

FOR FURTHER INFORMATION CONTACT: Licensing information may be obtained 
by contacting Michael Shmilovich, Esq, MS, CLP; 301-435-5019; 
[email protected], at the National Heart, Lung, and Blood, 
Office of Technology Transfer and Development Office of Technology 
Transfer, 31 Center Drive Room 4A29, MSC2479, Bethesda, MD 20892-2479. 
A signed Confidential Disclosure Agreement may be required to receive 
any unpublished information.

SUPPLEMENTARY INFORMATION: This notice is in accordance with 35 U.S.C. 
209 and 37 CFR part 404. Technology description follows. Prazole-Based 
Antiviral Therapeutics:
    Available for licensing and commercial development is a patent 
estate that covers prazole based compounds and their methods of use as 
antiviral therapeutics. Prazoles are benzimidazole derivatives 
generally marketed as stomach-acid reducers, owing to their ability to 
inhibit the H+/K+ ATPases (proton pumps) of the parietal cells in the 
stomach epithelium. Prazoles can inhibit the egress of several viral 
targets: HIV-1, HSV-1 and -2, MAYV, and EBV by interfering with the 
ESCRT complex in the formation of exosomes. In that respect, the target 
for inhibition of these viruses is Tumor susceptibility gene 101 
(Tsg101), a member of the ESCRT-I complex. The N-terminal ubiquitin E2 
variant (UEV) domain of Tsg101 has both ubiquitin and P[T/S]AP motif 
binding sites, where the prazole binds to C73 in the middle of the 
ubiquitin-binding site, sterically inhibiting the Ub-Tsg101 
interaction. By way of example, and not limitation, a prazole compound 
according to this invention can take on the follow core structure:
[GRAPHIC] [TIFF OMITTED] TN05AP24.048

    Where L is optionally present and is a C1-C6 
alkyl group, a C1-C6 alkoxy group, a -
(CH2CH2O)n- group where n is an 
integer from 1 to 6, a phenyl group, or a benzyl group, each of which 
is optionally substituted. B is a substituted or unsubstituted aromatic 
or heteroaromatic substituent, and where

X1 is S(=O) or S;
Y1 is N or CR4; and
each of R1-R7 is independently selected from 
hydrogen, C1-C6 alkyl, C1-
C6 alkoxy, perfluoro C1-C6 alkyl, 
perfluoro C1-C6 alkoxy, halo, -CN, -OH, -
COOR8, substituted or unsubstituted aromatic, or 
substituted or unsubstituted heteroaromatic, and
each R8 independently is hydrogen, C1-
C6 alkyl, phenyl, or benzyl.

    Potential Commercial Applications:

 antivirals
 therapeutics
 ESCRT complex formation
 prazole
 antifungal

    Development Stage:

 Early stage

    Inventors: Nico Tjandra (NHLBI), Carol Carter (Stonybrook), Rolf E. 
Swenson (NHLBI), David Nyenhuis (NHLBI), Natarajan Raju (NHLBI), 
Chandra Mushti, (NHLBI), and Venkata Sabbasani (NHLBI).
    Intellectual Property: HHS Reference No. E-239-2023-0; U.S. 
Provisional Patent Application No. 63/545,080 filed October 20, 2023.
    Publication: D. A. Nyenhuis, S. Watanabe, R. Bernstein, R. E. 
Swenson, N. Raju, V. R. Sabbasani, C. Mushti, D.-Y. Lee, C. Carter, N. 
Tjandra, ``Structural Relationships to Efficacy for Prazole-Derived 
Antivirals.'' Adv. Sci. 2024, 2308312. https://doi.org/10.1002/advs.202308312.
    Licensing Contact: Michael Shmilovich, Esq, MS, CLP; 301-435-5019; 
[email protected].

    Dated: April 2, 2024.
Michael A. Shmilovich,
Senior Licensing and Patenting Manager, National Heart, Lung, and Blood 
Institute, Office of Technology Transfer and Development.
[FR Doc. 2024-07278 Filed 4-4-24; 8:45 am]
BILLING CODE 4140-01-P