Roussel Uclaf

Hoechst Marion Roussel

Other

Jean-Francois Chantot

Jozsef Aszodi

Constantin Agouridas

Alexis Denis

Solange Gouin d'Ambrieres

Daniel Humbert

Odile Le Martret

Patrick Fauveau

Christophe Dini

Solange G D'Ambrieres

Yannick Benedetti

Jean-Georges Teutsch

Claude Fromentin

Alain Bonnefoy

Alain Bonnet

Nicole Tessot

Daniel Hunbert

Odile L Martret

Jean-Marie Pejac

A compound having the formula selected from the group consisting of

Cephalosporins

Erythromycin derivatives, method for preparing same and use thereof as

Intermediates for the preparation of compounds selected from the group consisting of a compound of the formula ##STR1## wherein R is ##STR2## n is an integer from 3 to 5, Ar is an optionally substituted heterocyclic selected from the group consisting of

Erythromycin compounds

Erythromycin derivatives, method for preparing same, and use thereof as

A compound selected from the group consisting of a syn isomer of a compound of the formula ##STR1## in the R or S form or in the form of an R, S mixture wherein R us selected from the group consisting of ##STR2## R and R' are individually selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen, CO.sub.2 --Q, ##STR3## CH.sub.2 --SQ, Q and Q' are individually hydrogen or alkyl of 1 to 4 carbon atoms, P, P' and P' are individually alkyl of 1 to 4 carbon atoms optionally substituted by one of the substituents R and R' the dotted line indicating that P and P' can optionally form with the nitrogen atom to which they are linked a heterocycle with 5 or 6 links, R.sub.b and R.sub.c are individually selected from the group consisting of an equivalent of an alkali metal, an alkaline earth metal, magnesium, ammonium and an amine organic base or A and A' are the remainder of an easily cleavable ester group or CO.sub.2 A is CO.sub.2 --and the wavy line indicates that CH.sub.2 R.sub.1 is in the E or Z position and their non-toxic, pharmaceutically acceptable acid addition salts having anti-bacterial activity.

Novel intermediates of the formula ##STR1## wherein the substituents are defined in the specification.

A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## syn isomer, in the (R) or (S) form or in the form of an (R,S) mixture, in the form of an integral salt or their salts with organic or mineral acids wherein the substituents are as defined in the application and having antibacterial properties.

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

A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## syn isomer, in the (R) or (S) form or in the form of an (R,S) mixture, in the form of an internal salt or their salts with organic or mineral acids wherein the substituents are as set forth below.

A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## syn isomer, in the (R) or (S) form or in the form of an (R,S) mixture, in the form of an internal salt or their salts with organic or mineral acids wherein the substituents are defined as in the application having anti-bacterial properties.

Erythromycin derivatives

An erythromycin compound of Formula I or its non-toxic acid addition salt having antibiotic activity.

Novel intermediates for the preparation of the compounds of Formula I wherein the substituents are as defined in the specification.

Eryhromycin derivatives

A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## syn isomer, in the (R) or (S) form or in the form of an (R,S) mixture, in the form of an internal salt or their salts with organic or mineral acids, wherein the variables are herein below defined, having antibacterial properties.

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.

Growing community of inventors

Gressy en France, France

Jean-Francois Chantot