# US 2010/0167996 A1 · 3-Ether and 3-Thioether Substituted Cyclosporin Derivatives For the Treatment and Prevention of Hepatitis C Infection

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- Number: US 2010/0167996 A1
- Document ID: US20100167996A1
- Status: Published application
- Kind: A1
- Application number: 12/643,860
- Filed: 2009-12-21
- Published: 2010-07-01
- Earliest claimed: 2004-10-01
- Inventors: Hans Georg Fliri; David Renwick Houck
- Web page: https://patentgrep.com/patent/US20100167996A1

## CPC

- A61K 38/13: Cyclosporins
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 31/12: Antivirals
- A61P 31/14: for RNA viruses
- A61P 31/16: for influenza or rhinoviruses
- A61P 31/18: for HIV
- C07K 7/645: {Cyclosporins; Related peptides}
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- 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
- 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)
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

This invention relates to cyclosporin derivatives of general formula (I): wherein A, B, R1, R2 and X are as defined in the specification, and pharmaceutical compositions prepared from the same, for use in treatment of hepatitis C virus.

## Claims

### Claim at position 1

-20. (canceled)

### Claim 21

A pharmaceutically acceptable salt of 3-[(R)-2-(N,N-dimethylamino)ethylthio-Sar]-4-(gamma-hydroxymethylleucine)cyclosporin.

### Claim 22 (depends on 21)

The salt as claimed in claim 21, wherein said salt is a phosphate, citrate, acetate, chloride, methanesulfonate or propionate salt.

### Claim 23 (depends on 21)

A hydrate of a salt as claimed in claim 21.

### Claim 24

A composition comprising a pharmaceutically acceptable salt of 3-[(R)-2-(N,N-dimethylamino)ethylthio-Sar]-4-(gamma-hydroxymethylleucine)cyclosporin, in combination with one or more compatible and pharmaceutically acceptable carriers.

### Claim 25 (depends on 24)

The composition as claimed in claim 24 which is in oral form.

### Claim 26 (depends on 25)

The composition as claimed in claim 25 which is a tablet.

### Claim 27 (depends on 24)

The composition as claimed in claim 24, wherein said salt is a phosphate, citrate, acetate, chloride, methanesulfonate or propionate salt.

### Claim 28

A composition comprising a pharmaceutically acceptable salt of 3-[(R)-2-(N,N-dimethylamino)ethylthio-Sar]-4-(gamma-hydroxymethylleucine)cyclosporin, and one or more other anti-HCV agents.