Centre National De La Recherche Scientifique

Other

Idenix Pharmaceuticals, Inc.

L'université Montpellier Ii

Emory University

Commissariat a L'energie Atomique

Isis Pharmaceuticals, Inc.

The Uab Research Foundation

Cnrs

Novartis Ag

The University of Alabama

Agence Nationale De Valorisation De La Recherche (anvar)

Synthelabo

University of Montpellier Ii

Centre National De La Recherche Scientifique-cnrs

Jean-Louis Imbach

Gilles J Gosselin

Martin L Bryant

Raymond F Schinazi

Jean-Pierre Sommadossi

Joel Oiry

Christian Perigaud

Pascal Clayette

Bernard Rayner

Philippe Fretier

Jean-Yves Puy

Muthiah Manoharan

Jean-Jacques Vasseur

Gilles Gosselin

Albert Meyer

Anne-Marie Aubertin

Jean-Claude Madelmont

Cécile Dueymes

Fritz Link

Jean De Rudder

Denise Godeneche

Daniel Parry

Marie-France Moreau

Meinolf Lange

Gustin Meyniel

Joël Oiry

Jean-Louis Barascut

Jean-Pierre Sommmadossi

Andreas Schonberger

Ilaria Adamo

Andreas Schönberger

This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2'-deoxy-&#x3b2;-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2&#x2032;-deoxy-&#x3b2;-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2&#x2032;-deoxy-&#x3b2;-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2&#x2032;-deoxy-&#x3b2;-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.

&#x3b2;-L-2'-deoxy-nucleosides for the treatment of hepatitis B

A solution phase synthesis method for preparing an oligonucleotide, wherein at least some of the reagents are solid supported. The method suitable for large-scale synthesis comprises coupling a protected compound with a nucleotide derivative having a protection group in the presence of a solid supported activator to give an elongated oligonucleotide with a P(III)-internucleotide bond; optionally processing the elongated oligonucleotide by capping by reaction with a solid supported capping agent and/or by oxidizing or sulfurizing by reaction of the oligonucleotide with a solid supported oxidizing or sulfurization reagent; and removing the protection group. The coupling may include reacting a 3'-protected compound of formula: with a nucleotide derivative having a 5&#x2032;-protection group, or reacting a 5&#x2032;-protected compound of formula with a nucleotide derivative having a 3&#x2032;-protection group.

Method for preparing oligonucleotides

The present invention relates to compounds, compositions and methods for the treatment of a host infected with a hepatitis B virus. Specifically, compound and compositions of 3'-esters of 2&#x2032;-deoxy-&#x3b2;-L-pyrimidine nucleosides are disclosed, which can be administered either alone or in combination with other anti-hepatitis B agents. Compound and compositions of 3&#x2032;,5&#x2032;-diesters of 2&#x2032;-deoxy-&#x3b2;-L-pyrimidine nucleosides are also disclosed, which can be administered either alone or in combination with other anti-hepatitis B agents.

3'-prodrugs of 2&#x2032;-deoxy-&#x3b2;-L-nucleosides

A method for the treatment of a host, and in particular, a human, infected with hepatitis B virus (HBV) is provided that includes administering an effective amount of a &#x3b2;-L-nucleotide, optionally in combination therapy with other drugs for the treatment of HBV or human immuno-deficiency virus (HIV).

Nucleosides with anti-hepatitis B virus activity

Method for the sterospecific preparation of 2' or 3&#x2032; deoxy and 2&#x2032;,3&#x2032;-dideoxy-&#x3b2;-L-pentafuranonucleoside compounds. 2&#x2032; or 3&#x2032; deoxy and 2&#x2032;,3&#x2032;-dideoxy-&#x3b2;-L-pentofuranonucleoside compounds are also described. Finally, the invention concerns the use of these compounds, and particularly 2&#x2032;,3&#x2032;dideoxy-&#x3b2;-L-fluorocytidine, as drugs, and especially as anti-viral agents.

2' or 3&#x2032; -deoxy and 2&#x2032;, 3&#x2032;-dideoxy-&#x3b2;-L-pentofuranonucleo-side compounds, method of preparation and application in therapy, especially as anti-viral agents

This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2'-deoxy-&#x3b2;-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2&#x2032;-deoxy-&#x3b2;-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2&#x2032;-deoxy-&#x3b2;-L-eythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2&#x2032;-deoxy-&#x3b2;-L-erythro pentofuranonucleoside or in combination with another anti-hepatitis B agent.

A compound, method and composition for treating a host infected with a hepatitis C viral comprising administering an effective hepatitis C treatment amount of a described 4'-disubstituted nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.

Methods and compositions for treating hepatitis C virus using 4'-modified nucleosides

The invention concerns compounds of general formula (I) (wherein R and R' represent an alkyl radical or an aryl group and R&#x2033; is hydrogen or a CO&#x2014;Rgroup wherein Ris an alkyl radical or an aryl group; and the dimers formed by the disulphide bond from one and/or the other of the two sulphur atoms of the compounds of general formula (I); and the corresponding thiazolidin forms), the methods for preparing them and uses thereof. More particularly, it concerns the use of said compounds as antioxidant agents, in particular for preparing medicines designed to increase the intracellular and/or extracellular level of glutathione (GSH).

Antioxidants, preparation methods and uses

The invention concerns a process for preparing compounds of general formula (I)wherein R and R' represent an alkyl radical or an aryl group; and R&#x2033; is hydrogen or a CO&#x2014;Rgroup wherein Ris an alkyl radical or an aryl group; and wherein these compounds are or not in the thiazolidine form; by protecting the N-acyl-L-cysteine to form an intermediate compound; and then by coupling said intermediate compound with S-acylcysteamine hydrochloride or with thiazolidine.

Antioxidants, preparation processes and their uses

This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2'-deoxy-&#x3b2;-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2&#x2032;-deoxy-&#x3b2;-L-erythro-pentofuranonucleoside has the formula:wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2&#x2032;-deoxy-&#x3b2;-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2&#x2032;-deoxy-&#x3b2;-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.

Compounds and pharmaceutical compositions active against HIV are provided, as is a method for the treatment of HIV infection in humans and other host animals is provided comprising administering an effective amount of a &#x3b2;-L-(2' or 3&#x2032;-azido)-2&#x2032;,3&#x2032;-dideoxy-5-fluorocytosine of the formulawherein R is H, acyl, monophosphate, diphosphate, or triphosphate, or a stabilized phosphate derivative (to form a stabilized nucleotide prodrug), and R&#x2032; is H, acyl, or alkyl.

&#x3b2;-L-2'-deoxy-nucleosides for the treatment of HIV infection

The present invention relates to compounds, compositions and methods for the treatment of a host infected with a hepatitis B virus. Specifically, compound and compositions of 3'-esters of 2&#x2032;-deoxy-&#x3b2;-L-nucleosides are disclosed, which can be administered either alone or in combination with other anti-hepatitis B agents. Compound and compositions of 3&#x2032;,5&#x2032;-diesters of 2&#x2032;-deoxy-&#x3b2;-L-nucleosides are disclosed, which can be administered either alone or in combination with other anti-hepatitis B agents, are also disclosed.

&bgr;-L-2&prime;-deoxy pyrimidine nucleosides for the treatment of hepatitis B

&bgr;-L-2&prime;-deoxy-nucleosides for the treatment of hepatitis B

Growing community of inventors

Montpellier, France

Jean-Louis Imbach