# US 7,612,093 B2 · Compositions of treating hepatitis virus infections with N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds in combination therapy

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- Number: US 7,612,093 B2
- Document ID: US7612093B2
- Status: Granted
- Kind: B2
- Application number: 11/300,464
- Filed: 2005-12-15
- Published: 2006-05-04
- Granted: 2009-11-03
- Earliest claimed: 1997-02-14
- Assignees: United Therapeutics Corporation
- Inventors: Gary S. Jacob; Timothy M. Block; Raymond A. Dwek
- Web page: https://patentgrep.com/patent/US7612093B2

## CPC

- C07D 211/46: having a hydrogen atom as the second substituent in position 4
- A61K 31/445: Non condensed piperidines, e.g. piperocaine
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- 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

Provided are methods and compositions for treating hepatitis virus infections in mammals, especially humans. The methods comprise (1) administering N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds in combination with nucleoside antiviral agents, nucleotide antiviral agents, mixtures thereof, or immunomodulating/immunostimulating agents, or (2) administering N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds in combination with nucleoside antiviral agents, nucleotide antiviral agents, or mixtures thereof, and immunomodulating/immunostimulating agents.

## Claims

### Claim 1

A pharmaceutical composition for treating a hepatitis B virus infection in a human patient, comprising from about 0.1 mg to about 100 mg of N-(n-nonyl-)-1,5-dideoxy-1,5-imino-D-glucitol and from about 0.1 mg to about 500 mg of (−)-2′-deoxy-3′-thiocytidine-5′-triphosphate.

### Claim 2

A pharmaceutical composition for treating hepatitis virus infection, comprising a first amount of an N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compound of Formula I:
wherein R is selected from the group consisting of straight chain alkyl having a chain length of C7 to C12 and
W, X, Y, and Z are each independently selected from the group consisting of hydrogen, and butanoyl; and
a second amount of an antiviral compound selected from the group consisting of 2′,3′-dideoxycytidine, 2′,3′-dideoxycytidine-5′-triphosphate, (−)-2′,3′-dideoxy-3′-thiacytidine, (−)-2′-deoxy-3′-thiocytidine-5′-triphosphate, and mixtures thereof and a pharmaceutical acceptable carrier, diluent, or excipient
wherein said first and second amounts of said compounds together comprise an anti-hepatitis virus effective amount of said compounds.

### Claim 3 (depends on 2)

The pharmaceutical composition of claim 2, wherein R is a straight chain alkyl having a chain length of C7 to C12 and W, X, Y, and Z are each hydrogen.

### Claim 4 (depends on 3)

The pharmaceutical composition of claim 3, wherein R is nonyl.

### Claim 5 (depends on 2)

The pharmaceutical composition of claim 2, wherein R is nonyl and W, X, Y, and Z are each butanoyl.

### Claim 6 (depends on 2)

The pharmaceutical composition of claim 2, wherein said N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compound is selected from the group consisting of N-(n-nonyl)-1,5-dideoxy-1,5-imino-D-glucitol and N-(n-nonyl)-1,5-dideoxy-1,5-imino-D-glucitol, tetrabutyrate, and said antiviral compound is (−)-2′-deoxy-3′-thiocytidine-5′-triphosphate.

### Claim 7 (depends on 6)

The pharmaceutical composition of claim 6, wherein said N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compound is N-(n-nonyl)-1,5-dideoxy-1,5-imino-D-glucitol.

### Claim 8 (depends on 2)

The pharmaceutical composition of claim 2, wherein said first amount of said N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compound is in the range of from about 0.1 mg to about 100 mg.

### Claim 9 (depends on 2)

The pharmaceutical composition of claim 2, wherein said second amount of said nucleoside or nucleotide antiviral compound, or mixture thereof, is in the range of from about 0.1 mg to about 500 mg.