# US 8,569,245 B2 · Protease inhibitors, compositions and methods of use

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- Number: US 8,569,245 B2
- Document ID: US8569245B2
- Status: Granted
- Kind: B2
- Application number: 13/380,775
- Filed: 2010-06-26
- Published: 2012-07-12
- Granted: 2013-10-29
- Earliest claimed: 2009-06-26
- Assignees: University of Florida Research Foundation, Inc.; Smithsonian Institution
- Applicants: Hendrik Luesch; Valerie J. Paul; Jason C. Kwan
- Inventors: Hendrik Luesch; Valerie J. Paul; Jason C. Kwan
- Web page: https://patentgrep.com/patent/US8569245B2

## CPC

- C07K 11/00: Depsipeptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61P 7/00: Drugs for disorders of the blood or the extracellular fluid
- A61P 11/06: Antiasthmatics
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 31/18: for HIV
- A61P 35/00: Antineoplastic agents
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## 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

### Claim 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.

### Claim 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.

### Claim 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.

### Claim 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.

### Claim 5 (depends on 4)

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.

### Claim 6 (depends on 4)

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.

### Claim 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.