# US 9,040,479 B2 · HCV NS3 protease inhibitors

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- Number: US 9,040,479 B2
- Document ID: US9040479B2
- Status: Granted
- Kind: B2
- Application number: 14/365,329
- Filed: 2013-01-11
- Published: 2014-11-27
- Granted: 2015-05-26
- Earliest claimed: 2012-01-12
- Assignees: Cocrystal Pharma, Inc.
- Applicants: RFS Pharma, LLC
- Inventors: Steven J. Coats
- Web page: https://patentgrep.com/patent/US9040479B2

## CPC

- C07K 5/101: {the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu}
- A61K 31/4035: Isoindoles, e.g. phthalimide
- A61K 38/07: Tetrapeptides
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 31/14: for RNA viruses
- C07D 403/12: linked by a chain containing hetero atoms as chain links
- 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)
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

The present invention is directed to compounds, compositions and methods for treating or preventing HCV viral infections in human patients or other animal hosts.

## Claims

### Claim 1

A compound of Formula (I):
or a pharmaceutically acceptable salt, or solvate thereof, wherein
J and J1 can be present or absent, and when present are independently selected from the group consisting of lower alkyl (C1-C6), aryl, arylalkyl, alkoxy, aryloxy, heterocyclyl, heterocyclyloxy, keto, hydroxy, amino, arylamino, carboxyalkyl, carboxamidoalkyl, halo, cyano, formyl, sulfonyl, or sulfonamido; and
R is alkyl (C1-C10), alkenyl (C2-C10), alkynyl (C2-C10), cycloalkyl(C3-C8), aryl, heteroaryl, or heterocyclyl each containing 1 to 9 fluorine atoms and/or 1 to 3 silicon atoms.

### Claim 2 (depends on 1)

The compound of claim 1, wherein the compounds, or pharmaceutically acceptable salts, or solvates thereof, can be in the form of individual enantiomers, stereoisomers, rotamers, tautomers, racemates, or mixtures thereof.

### Claim 3 (depends on 1)

A method for treating an HCV infection, or reducing the biological activity of HCV, comprising administering a therapeutically effective amount of a compound of claim 1 to a patient in need of treatment thereof.

### Claim 4 (depends on 3)

The method of claim 3, wherein the compound is administered in combination with another anti-HCV agent.

### Claim 5 (depends on 1)

A method for inhibiting serine protease activity, comprising the step of administering to said patient a compound according to claim 1.

### Claim 6 (depends on 3)

The method according to claim 3, wherein said compound is administered to a patient and is formulated together with a pharmaceutically suitable carrier into a pharmaceutically acceptable composition.

### Claim 7 (depends on 4)

The method according to claim 4, wherein said compound is administered to a patient and is formulated together with a pharmaceutically suitable carrier into a pharmaceutically acceptable composition.

### Claim 8 (depends on 5)

The method according to claim 5, wherein said compound is administered to a patient and is formulated together with a pharmaceutically suitable carrier into a pharmaceutically acceptable composition.