Compositions and methods for combination antiviral therapy

Details Compositions and methods for combination antiviral therapy Compositions and methods for combination antiviral therapy

A - Human Necessities

61

K

A61K 31/675 (2006.01) A61K 31/513 (2006.01) A61P 31/18 (2006.01) A61K 9/20 (2006.01) A61K 9/48 (2006.01)

Patent

CA 2512475

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-l-(2~ hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (emtricitabine, EmtrivaTM, (-)-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.

L'invention concerne des combinaisons thérapeutiques de diisopropoxycarbonyloxyméthyl ester d'acide [2-(6-amino-purin-9-yl)-1-méthyl-éthoxyméthyl]-phosphonique (tenofovir disoproxil fumarate, Viread®) et de (2R, 5S, cis)-4-amino-5-fluoro-l-(2- hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (emtricitabine, Emtriva<SP>TM</SP>, (-)-cis FTC) et leurs dérivés physiologiquement fonctionnels. Ces combinaisons peuvent être utilisées pour traiter des infections par le VIH, comprenant les infections à mutants du VIH résistant à des inhibiteurs nucléosidiques et/ou non nucléosidiques. L'invention concerne également des compositions pharmaceutiques et des formulations de combinaisons de tenofovir disoproxil fumarate et d'emtricitabine et leurs dérivés physiologiquement fonctionnels ainsi que des méthodes thérapeutiques utilisant ces compositions et ces formulations.

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