IP Library Granted Patent US 8,569,245
Granted Patent B2
US 8,569,245 · App. 13/380,775 · Granted Oct 29, 2013

Protease inhibitors, compositions and methods of use

Inventors: Hendrik Luesch (Gainesville, FL); Valerie J. Paul (Fort Pierce, FL); Jason C. Kwan (Salt Lake City, UT)
Assignees: University of Florida Research Foundation, Inc.; Smithsonian Institution
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Quick Facts
Patent No.
US 8,569,245
App. No.
13/380,775
Granted
Oct 29, 2013
Kind
B2
Abstract

This invention relates to grassystatins A, B and C, and their isolated or purified forms. The compounds of the invention are useful as aspartic protease, gamma secretase, or metalloprotease inhibitors. Methods of using the compounds and compositions thereof are also disclosed.

Claims (8)

1. An isolated compound selected from the group of grassystatins A, B and C as follows:

or a pharmaceutically acceptable salt, ester, amide, hydrate, stereoisomer, or solvate thereof.

2. A pharmaceutical composition comprising a compound selected from the group of grassystatins A, B and C, or a pharmaceutically acceptable salt, ester, amide, hydrate, stereoisomer, or solvate thereof, together with a pharmaceutically acceptable carrier or diluent.

3. A method of treating a disease or disorder in a subject, the method comprising administering to the subject an effective amount of a compound selected from the group of grassystatins A, B and C, or a pharmaceutically acceptable salt, ester, hydrate, or solvate thereof, wherein the disease or disorder is selected from the group consisting of disorders of the cell cycle, neurodegenerative disorders, cancer, and Alzheimer's disease.

4. A method of inhibiting T-cell proliferation in a subject, the method comprising administering to the subject an effective amount of a compound selected from the group of grassystatins A and B, or a pharmaceutically acceptable salt, ester, hydrate, or solvate thereof.

5. The method of claim 4 , comprising reducing IL-17 production in a subject or in a cell, the method comprising administering to the subject or the cell an effective amount of a compound selected from the group of grassystatins A and B, or a pharmaceutically acceptable salt, ester, hydrate, or solvate thereof.

6. The method of claim 4 , comprising reducing IFN-γ production in a subject or in a cell, the method comprising administering to the subject or the cell an effective amount of a compound selected from the group of grassystatins A and B, or a pharmaceutically acceptable salt, ester, hydrate, or solvate thereof.

7. A method of treating a disease or disorder in a subject, the method comprising administering to the subject an effective amount of a compound selected from the group of grassystatins A and B, or a pharmaceutically acceptable salt, ester, hydrate, or solvate thereof, wherein the disease or disorder is selected from the group consisting of infection, autoimmune disorders, allergic diseases, and transplant rejection.

Assignments (3)
CONFIRMATORY LICENSE Recorded Nov 18, 2016
From: UNIVERSITY OF FLORIDA
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 040647/0797 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 5, 2012
From: LUESCH, HENDRIK; KWAN, JASON C.
To: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.
Reel/Frame 027994/0737 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 30, 2012
From: PAUL, VALERIE
To: SMITHSONIAN INSTITUTION
Reel/Frame 027614/0443 →
Continuity (2)
Provisional Application 61221027 · Jun 26, 2009
Related Publication 20120178669A1 · Jul 12, 2012