Roussel Uclaf

Sanofi-aventis

Aventis Pharma S.a.

Hoechst Marion Roussel

Yannick Benedetti

Odile Le Martret

Alain Commercon

Alexis Denis

Constantin Agouridas

Jean-Francois Chantot

Jidong Zhang

Claude Fromentin

Alain Commerçon

Arielle Genevois-Borella

Anke Steinmetz

Andrees Bohme

Jacques Lagouardat

Odile Angouillant-Boniface

Jean-Francedillaois Chantot

François Clerc

Frederico Nardi

Jacques Scholl

Gaetan Touyer

Stéphanie Deprets

Daniel Bezard

Frédérico Nardi

The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide derivatives, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds, and to intermediate precursors to such compounds.

Derivatives of 2-alkoxy-3,4,5-trihydroxy-alkyl amides, preparation and use thereof, and compositions containing the same

The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide benzothiazepine compounds, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds and to intermediate precursors to such compounds.

2-alkoxy-3,4,5-trihydroxyalkylamide-benzothiazepines preparation thereof, compositions containing them and use thereof

The invention especially relates to novel chemical compounds, especially novel benzothiazole derivatives, to compositions containing said compounds, and to the use thereof as medicaments.

Benzothiazoles and the use thereof as medicaments

The invention relates to triazine derivatives of general formula (I): Wherein R, Rand Rare as defined herein. The invention also relates to a method for preparing these triazine derivatives and to the therapeutic application thereof.

Triazine derivatives, their preparation and therapeutic application thereof

Method for isomerising the 10-methyl radical of erythromycin derivatives

Compounds of the formula ##STR1## wherein X and X' form C.dbd.O or C.dbd.NOR, R is selected from the group consisting of hydrogen, heterocycle, alkyl, alkenyl, alkynyl, all optionally substituted, ##STR2## R.sub.a and R.sub.b are hydrogen or a hydrocarbon group or form together with the nitrogen a heterocycle, or with A forms a 9-N, 11-O ring, and X' is hydrogen, --Y and Y' have the same definition as X and X', b is hydrogen or OR.sub.4, R.sub.4 is hydrogen or forms together with A a carbonate or a carbamate, A forms with C a double bond or A is OR'.sub.4, R'.sub.4 is hydrogen or forms together with B a carbonate or ##STR3## R.sub.2 is alkyl or --CONH.sub.2, --CONHCOR.sub.11 or --CONHSO.sub.2 R.sub.11, R.sub.11 is a hydrocarbon up to 18 carbon atoms, R.sub.3 is hydrogen, ##STR4## and Z is hydrogen or a carboxylic acid remainder and their non-toxic, pharmaceutically acceptable acid addition salts, their preparation and intermediates useful as antibiotics.

Erythromycin compounds

A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and an optionally unsaturated hydrocarbon of up to 24 carbon atoms optionally interrupted by at least one heteroatom selected from the group consisting of oxygen, sulfur and nitrogen and optionally having at least one functional group or taken together form ##STR2## and R'.sub.1 and R'.sub.2 are individually selected from the group consisting of hydrogen and an optionally unsaturated hydrocarbon of up to 23 carbon atoms optionally interrupted by at least one heteroatom selected from the group consisting of nitrogen, oxygen and sulfur and optionally having at least one functional group, Z is hydrogen or acyl of an organic carboxylic acid of 1 to 18 carbon atoms and the wavy line indicates the 10-methyl may have R or S configuration or a mixture of R+S and their non-toxic, pharmaceutically acceptable acid addition salts having antibiotic properties.

Propanal derivatives

Erythromycin derivatives

Compounds of the formula ##STR1## wherein X and X' form C.dbd.O or C.dbd.NOR, R is selected from the group consisting of hydrogen, heterocycle, alkyl, alkenyl, alkynyl, all optionally substituted, or X is ##STR2## R.sub.a and R.sub.b are hydrogen or a hydrocarbon group or form together with the nitrogen a heterocycle, or with A forms a 9-N, 11-0 ring, and X' is hydrogen, --Y and Y' have the same definition as X and X', B is hydrogen or OR.sub.4, R.sub.4 is hydrogen or forms together with A a carbonate or a carbamate, A forms with C a double bond or A is OR'.sub.4, R'.sub.4 is hydrogen or forms together with B a carbonate or A is ##STR3## R.sub.2 is alkyl or --CONH.sub.2, --CONHCOR.sub.11 or --CONHSO.sub.2 R.sub.11, R.sub.11 is a hydrocarbon up to 18 carbon atoms, R.sub.3 is hydrogen, ##STR4## and Z is hydrogen or a carboxylic acid remainder and their non-toxic, pharmaceutically acceptable acid addition salts, their preparation and intermediates useful as antibiotics.

Compounds of the formula ##STR1## wherein X and X' form C.dbd.O or C.dbd.NOR, R is selected from the group consisting of hydrogen, heterocycle, alkyl, alkenyl, alkynyl, all optionally substituted, or X is ##STR2## R.sub.a and R.sub.b are hydrogen or a hydrocarbon group or form together with the nitrogen a heterocycle, or with A forms a 9-N, 11-O ring, and X' is hydrogen, --Y and Y' have the same definition as X and X', B is hydrogen or OR.sub.4, R.sub.4 is hydrogen or forms together with A a carbonate or a carbamate, A forms with C a double bond or A is OR'.sub.4, R'.sub.4 is hydrogen or forms together with B a carbonate or ##STR3## R.sub.2 is alkyl or --CONH.sub.2, --CONHCOR.sub.11 or --CONHSO.sub.2 R.sub.11, R.sub.11 is a hydrocarbon up to 18 carbon atoms, R.sub.3 is hydrogen, ##STR4## and Z is hydrogen or a carboxylic acid remainder and their non-toxic, pharmaceutically acceptable acid addition salts, their preparation and intermediates useful as antibiotics.

All possible stereoisomeric forms and mixtures thereof of a compound of the formula ##STR1## wherein the substituents are as defined in the specification and their non-toxic, pharmaceutically acceptable acid addition salts having antibiotic properties.

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Rosny Sous Bois, France

Yannick Benedetti