Compositions and methods for combination antiviral therapy

A technology of composition and use, applied in the field of chemically stable combinations, capable of solving problems such as enhanced toxicity

Inactive Publication Date: 2012-06-06
GILEAD SCI INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it should be noted that combinations of compounds may lead to enhanced toxicity

Method used

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  • Compositions and methods for combination antiviral therapy
  • Compositions and methods for combination antiviral therapy
  • Compositions and methods for combination antiviral therapy

Examples

Experimental program
Comparison scheme
Effect test

preparation example

[0209] The following examples further describe and demonstrate specific embodiments falling within the scope of the present invention. Related methods and formulations can generally be found in Remington's Pharmaceutical Sciences (Mack Publishing Co., Easton, PA). The illustrated embodiments are for the purpose of illustration only and therefore should not be construed as limiting since various modifications are possible without departing from the spirit and scope of the invention. The following examples are for illustration only and are not meant to limit the scope of the invention in any way. "Active ingredient" means tenofovir disoproxil fumarate, emtricitabine, or any one of their physiological function derivatives.

[0210] tablet

[0211] Exemplary formulations A, B, C, D, E, and F below were prepared by wet granulating the ingredients with an aqueous solution followed by the addition of the extragranlar component followed by magnesium stearate and compression ....

Embodiment approach

[0358] A1. A pharmaceutical composition, which jointly contains an effective amount of the compound of the following formula or its physiological function derivatives:

[0359]

[0360] where R 1 and R 2 independently selected from H, C 1 -C 6 Alkyl, substituted C 1 -C 6 Alkyl, C 6 -C 20 Aryl, substituted C 6 -C 20 Aryl, C 6 -C 20 Aralkyl, substituted C 6 -C 20 Aralkyl, acyloxymethyl ester -CH 2 OC(=O)R 9 and acyloxymethyl carbonate-CH 2 OC(=O)OR 9 , where R 9 is C 1 -C 6 Alkyl, substituted C 1 -C 6 Alkyl, C 6 -C 20 Aryl and substituted C 6 -C 20 Aryl;

[0361] R 3 Choose from H, C 1 -C 6 Alkyl, substituted C 1 -C 6 Alkyl, or CH 2 OR 8 , where R 8 is C 1 -C 6 Alkyl, C 1 -C 6 Hydroxyalkyl or C 1 -C 6 Haloalkyl;

[0362] R 4 and R 5 independently selected from H, NH 2 , NHR or NR 2 , where R is C 1 -C 6 alkyl; and

[0363] R 6 and R 7 independently selected from H and C 1 -C 6 alkyl;

[0364] and an effective amount of the c...

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Abstract

The present invention relates to therapeutic combinations of [2-(6-amino-purin-9-yl)-1-methyl-ethoxymethyl]-phosphonic acid diisopropoxycarbonyloxymethyl ester (tenofovir disoproxil fumarate, Viread <*>) and (2R, 5S, cis)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (emtricitabine, Emtriva <TM>, (-)-cis FTC) and their physiologically functional derivatives. The combinations may be useful in the treatment of HIV infections, including infections with HIV mutants bearing resistance to nucleoside and / or non-nucleoside inhibitors. The present invention is also concerned with pharmaceutical compositions and formulations of said combinations of tenofovir disoproxil fumarate and emtricitabine, and their physiologically functional derivatives, as well as therapeutic methods of use of those compositions and formulations.

Description

[0001] This non-provisional application claims the benefit of provisional applications 60 / 440,246 and 60 / 440,308, filed January 14, 2003, which are hereby incorporated by reference. field of invention [0002] The present invention relates generally to combinations comprising compounds having antiviral activity, more particularly anti-HIV properties. In particular, the invention relates to chemically stable combinations containing antiviral agents with different structures. Background of the invention [0003] Human immunodeficiency virus (HIV) infection and related diseases are major public health problems worldwide. Human immunodeficiency virus type 1 (HIV-1) encodes at least three enzymes necessary for viral replication: reverse transcriptase (RT), protease (Prt) and integrase (Int). Although drugs targeting reverse transcriptases and proteases have been widely used and have also been shown to be effective, especially when ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/675A61K31/513
Inventor T·C·达尔M·M·曼宁R·奥里亚
Owner GILEAD SCI INC
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