Aventis Pharma S.a.

Roussel Uclaf

Other

Hoechst Marion Roussel

Novexel

Claude Fromentin

Alexis Denis

Constantin Agouridas

Jozsef Aszodi

Maxime Lampilas

David Alan Rowlands

Odile Le Martret

Yannick Benedetti

Francois Bretin

Jean-Francois Chantot

Bertrand Heckmann

Jean-Francedillaois Chantot

David Alun Rowlands

The invention relates to new heterocyclic compounds of general formula (I), and their salts with a base or an acid:  The invention also relates to a process for the preparation of these compounds as well as their use as medicaments, in particular as anti-bacterial agents.

Heterocyclic compounds, their preparation and their use as medicaments, in particular as anti-bacterial agents

This invention discloses and claims methods for inhibiting bacterial &#x3b2;-lactamases and treating bacterial infections by inhibiting bacterial &#x3b2;-lactamases in man or an animal comprising administering a therapeutically effective amount to said man or said animal of a compound, or pharmaceutically acceptable salt thereof, of formula (I) either alone or in combination with a &#x3b2;-lactamine antibiotic wherein said combination can be administered separately, together or spaced out over time. Pharmaceutical compositions comprising a compound of formula (I), or a combination of a compound of formula (I) and a therapeutically effective amount of a &#x3b2;-lactamine antibiotic, and a pharmaceutically acceptable carrier are also disclosed and claimed. 

Heterocyclic compounds as inhibitors of beta-lactamases

Novel compounds of the formulawherein the substituents are defined as in the application having antibiotic properties.

2-halogenated derivatives of 5-0 desosaminyl-erythronolide a, their preparation process and their antibiotic use

A subject of the invention is a process for the preparation of the compounds of formula (I): Wherein the substituents are defined as in the application. The compounds of this invention exhibit antibiotic properties.

2-halogenated derivatives of 5-O-desosaminyl-erythronolide A, their preparation process and their antibiotic use

Azabicyclic compounds, preparation thereof and use as medicines, in particular as antibacterial agents

Derivatives . . . use as medicaments

Derivatives of erythromycin, their preparation process and their use as medicaments

2-halogenated derivatives of 5-0 desosaminyl-erythronolide A, their preparation process and their antibiotic use

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

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.

Growing community of inventors

Paris, France

Claude Fromentin