Fab Pharma S.a.s.

Mutabilis

Debiopharm International, S.a.

Laboratoire Biodim

Fab Pharma

Vincent Gerusz

Alexis Denis

Mayalen Oxoby

Yannick Bonvin

Heinz W Pauls

Mihiro Sunose

Sonia Escaich

Francois Moreau

Fabien Faivre

Dmytro Atamanyuk

Francis Chevreuil

Christophe Simon

Nicolas Lecointe

Vivien Henryon

Benoît Ledoussal

Chrystelle Oliveira

Etienne Airiau

Jerome Monbrun

François Moreau

Judd Berman

Juan Bravo

Terry Finn

Vasileios Tatsis

Danig Pohin

Pierre-Michel Regenass

Jérôme Monbrun

The present invention provides compounds of the general formula (I) or a pharmaceutically acceptable prodrugs, salts and/or solvates thereof, wherein LHS is selected from the group consisting of LHSa and LHSb And wherein, the asterisk (*) marks the point of attachment; These compounds exhibit antibacterial activity against Gram-negative and Gram-positive bacteria, especiallyand. Pharmaceutical compositions containing these compounds, therapeutic uses thereof and methods for manufacturing the same are also provided.

Compounds and their use

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&#x2014;Rand Y is N or C&#x2014;R, 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; Ris Hydrogen or a substituent as defined in the application; Ris 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. 

Heteroaromatic derivatives and their use as pharmaceuticals

The invention relates to compounds of formulae (Ia), (Ib) or (Ic) wherein, Aand A, identical or different, are H, (C-C) alkyl, (C-C) fluoroalkyl, (C-C) alkenyl, (C-C) alkynyl, (C-C) alkyl-OR, (C-C) alkyl-SR, (C-C) alkyl-NRR, OR, SR, NRR, or COR; Ais H, OH or form a carbonyl with A; Ais H, OH or form a carbonyl with A; Ais H, CRROH, F, OH or forms a double bond with X in the case where X is CH; Ais H or F; X is CH, CHF, CF, CHOH, O, S, NRor a simple bond, or X is CH in the case where Aforms with X a double bond; Y is P(O)(OR)(OR) or P(O)(OR)(NRR); V is O or S; Ais H, (C-C) alkyl, (C-C) fluoroalkyl, (C-C) alkenyl, (C-C) alkynyl or (C-C) alkyl-OR; Ais OH or H, Rand R, identical or different, are H, (C-C) alkyl, (C-C) fluoroalkyl, (C-C) alkyl-OH or (C-C) alkyl-O&#x2014;(C-C) alkyl; and their addition salts thereof with acids and bases, their preparation and their use in the antibacterial prevention and therapy, used alone or in association with antibacterials, antivirulence agents or drugs reinforcing the host innate immunity. 

Antibacterial compounds and biological applications thereof

The invention relates to novel heterocyclic acrylamide compounds (I), to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.

Heterocyclic acrylamides and their use as pharmaceuticals

The invention relates to hydroxyphenyl derivatives of formula (I); and uses thereof as anti-bacterial and/or anti-parasitic agents.

Hydroxyphenyl derivatives and biological applications thereof

The invention relates to a novel hydroxyphenyl compound, to the preparation of the compound and intermediates used therein, to the use of the compound as an antibacterial medicament and pharmaceutical compositions containing the compound.

Antibacterial hydroxyphenyl compound

The invention relates to novel heterocyclic acrylamide compounds (I), to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds. 

The invention relates to hydroxyphenyl derivatives of formula (I); and uses thereof as anti-bacterial and/or anti-parasitic agents. 

The invention relates to novel acylpiperazinone compounds, to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.

Acylpiperazinones and their use as pharmaceuticals

The invention relates to Imidazolo-heteroaryl derivatives of formula (I). The compounds inhibit the activity of the Dlta enzyme of Gram-positive bacteria and are useful to treat Gram-positive bacterial infections. Furthermore the application discloses method for assessing the Dlta inhibitory activity of tested molecules and a method for measuring the efficacy of molecules in inhibiting bacteria proliferation in vitro. 

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Paris, France

Vincent Gerusz