Gilead Sciences, Inc.

Bristol-myers Squibb & Gilead Sciences, Inc.

K.u. Leuven Research & Development

International Partnership for Microbicides, Inc.

The Conrad Program Of The Eastern Virginia Medical School (“Conrad”)

Other

Gerhard Puerstinger

Puerstinger, Gerhard

Terrence C Dahl

Reza Oliyai

Mark Michael Menning

Taiyin Yang

Robert L Jerzewski

Munir A Hussain

Robert A Lipper

Winston C Tse

David A Oare

Vahid Zia

Steven S Bondy

Lung-Chi J Yuan

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&#xae;) and (2R,5S,cis)-4-amino-5-fluoro-1-(2 hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (emtricitabine, Emtriva&#x2122;, (&#x2212;)-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.

Compositions and methods for combination antiviral therapy

In accordance with this invention a novel pharmaceutical product containing efavirenz, emtricitabine and tenofovir DF are provided as a multicomponent unitary oral dosage form, component 1 comprising tenofovir DF (and, optionally, emtricitabine) and component 2 comprising efavirenz, wherein components 1 and 2 are in a stabilizing configuration. In preferred embodiments component 1 is made by dry granulation.

Unitary pharmaceutical dosage form

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&#xae;) and (2R,5S,cis)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (emtricitabine, Emtriva&#x2122;, (&#x2212;)-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.

The present invention relates to formulations of nucleotide reverse transcriptase inhibitors (NRTIs), preferably [2-(6-Amino-purin-9-yl)-1-methyl-ethoxymethyl]-phosphonic acid (tenofovir, PMPA), or a physiologically functional derivative thereof, suitable for topical application and their use in the prevention of HIV infections.

Topical antiviral formulations

In accordance with this invention a novel pharmaceutical product containing efavirenz, emtricitabine and tenofovir DF are provided as a multicomponent unitary oral dosage form, componentcomprising tenofovir DF (and, optionally, emtricitabine) and componentcomprising efavirenz, wherein componentsandare in a stabilizing configuration. In preferred embodiments componentis made by dry granulation.

This invention is directed to a composition comprising dry granulated tenofovir DF and emtricitabine, and a method for making same. Dry granulation was unexpectedly found to be important in preparing a tenofovir DF containing composition suitable for inclusion in a combination dosage form containing emtricitabine, efavirenz and tenofovir DF.

Method and composition for pharmaceutical product

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&#xae;) and (2R, 5S, cis)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one(emtricitabine, Emtriva&#x2122;, (-)-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.

A compound of formula (1) and its salts and solvates are provided for the treatment or prophylaxis of hepatitis C virus infections. Methods of making and formulating compound (1) are provided. 

Pyridazine compound and use thereof

A compound of formula (1) and its salts and solvates are provided for the treatment or prophylaxis of hepatitis C virus infections Methods of making and formulating compound (1) are provided.

The invention provides compositions comprising the nucleotide analog 9-&lsqb;2-&lsqb;&lsqb;bis&lsqb;(pivaloyloxy)methyl&rsqb;phosphono&rsqb;methoxy&rsqb;ethyl&rsqb;adenine and an alkaline excipient with or without L-carnitine-L-tartrate. The compositions are more stable those previously described. The invention also provides methods to make the compositions and their intermediates.

Growing community of inventors

Sunnyvale, CA, United States of America

Terrence C Dahl