Romainville, France
Romainville, France

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The invention relates to the compounds (I) and their acids and bases salts: wherein: Formula (I) the dotted line indicates a double bond; X is N or C-R1 and Y is N or C-R2, X and Y not being simultaneously N; A is selected from the group consisting of phenyl, naphthyl and (5-11) membered monocyclic or bicyclic unsaturated cycle or heterocycle possibly substituted as defined in the application, and A can also comprise either a further (4-7) membered heterocycle, said heterocycle being a monocycle, fused, saturated or unsaturated, the polycyclic system then comprising up to 14 members and up to 5 heteroatoms selected from N, O and S; B is selected from the group of substituents as defined in the application, or B is a 4 or (6-10) membered mono or bicyclic saturated or unsaturated heterocycle containing 1-3 heteroatoms selected from N, O and S, linked by a carbon atom, and possibly substituted as defined in the application; R1 is Hydrogen or a substituent as defined in the application; R2 is Hydrogen or Halogen; their preparation, their use in the antibacterial prevention and therapy, alone or in association with antibacterials, antivirulence agents or drugs reinforcing the host innate immunity, and pharmaceutical compositions and associations containing them.


Lee T.-W.,McMaster University | Verhey T.B.,McMaster University | Antiperovitch P.A.,McMaster University | Atamanyuk D.,MUTABILIS | And 17 more authors.
Journal of Medicinal Chemistry | Year: 2013

As an essential constituent of the outer membrane of Gram-negative bacteria, lipopolysaccharide contributes significantly to virulence and antibiotic resistance. The lipopolysaccharide biosynthetic pathway therefore serves as a promising therapeutic target for antivirulence drugs and antibiotic adjuvants. Here we report the structural-functional studies of d-glycero-β-d-manno-heptose 7-phosphate kinase (HldA), an absolutely conserved enzyme in this pathway, from Burkholderia cenocepacia. HldA is structurally similar to members of the PfkB carbohydrate kinase family and appears to catalyze heptose phosphorylation via an in-line mechanism mediated mainly by a conserved aspartate, Asp270. Moreover, we report the structures of HldA in complex with two potent inhibitors in which both inhibitors adopt a folded conformation and occupy the nucleotide-binding sites. Together, these results provide important insight into the mechanism of HldA-catalyzed heptose phosphorylation and necessary information for further development of HldA inhibitors. © 2012 American Chemical Society.


The present invention relates to heterocyclic compounds of formula (I), their process of preparation, pharmaceutical compositions comprising these compounds and use thereof, optionally in combination with other antibacterial agents and/or beta-lactam compounds, for the prevention or treatment of bacterial infections. The present invention also relates to the use of these compounds as -lactamase inhibitors and/or as antibacterial agents.


The present invention relates to heterocyclic compounds, their process of preparation, pharmaceutical compositions comprising these compounds and use thereof, optionally in combination with other antibacterial agents and/or beta-lactam compounds, for the prevention or treatment of bacterial infections. The present invention also relates to the use of these compounds as -lactamase inhibitors and/or as antibacterial agents.


The present invention relates to heterocyclic compounds, their process of preparation, pharmaceutical compositions comprising these compounds and use thereof, optionally in combination with other antibacterial agents and/or beta-lactam compounds, for the prevention or treatment of bacterial infections. The present invention also relates to the use of these compounds as -lactamase inhibitors and/or as antibacterial agents.


The present invention relates to heterocyclic compounds of formula (I), their process of preparation, pharmaceutical compositions comprising these compounds and use thereof, optionally in combination with other antibacterial agents and/or beta-lactam compounds, for the prevention or treatment of bacterial infections. The present invention also relates to the use of these compounds as -lactamase inhibitors and/or as antibacterial agents.


The invention relates to the compounds (I) and their acids and bases salts: wherein: Formula (I) the dotted line indicates a double bond; X is N or CR_(1 )and Y is N or CR_(2), X and Y not being simultaneously N; A is selected from the group consisting of phenyl, naphthyl and (5-11) membered monocyclic or bicyclic unsaturated cycle or heterocycle possibly substituted as defined in the application, and A can also comprise either a further (4-7) membered heterocycle, said heterocycle being a monocycle, fused, saturated or unsaturated, the polycyclic system then comprising up to 14 members and up to 5 heteroatoms selected from N, O and S; B is selected from the group of substituents as defined in the application, or B is a 4 or (6-10) membered mono or bicyclic saturated or unsaturated heterocycle containing 1-3 heteroatoms selected from N, O and S, linked by a carbon atom, and possibly substituted as defined in the application; R_(1 )is Hydrogen or a substituent as defined in the application; R_(2 )is Hydrogen or Halogen; their preparation, their use in the antibacterial prevention and therapy, alone or in association with antibacterials, antivirulence agents or drugs reinforcing the host innate immunity, and pharmaceutical compositions and associations containing them.


The invention relates to new 1,2,4-triazine derivatives of formula (I):their preparation and intermediates, their use as drugs and pharmaceutical compositions and associations containing them. The compounds of formula (I) are capable of inhibiting bacterial heptose synthesis.


The invention relates to compositions of polypeptides specific to pathogenic strains comprising at least one polypeptide of a first group, having a sequence selected in the group comprising the sequences of SEQ ID No 159, or homologous sequences of polypeptides of the first group and/or the second group with a minimum of 25% of identity with the whole sequences of said polypeptides. Application for the preparation of vaccine compositions specific to E. coli extra-intestinal infections.

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