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US 2012/0232079 A1Published application
Novel acylpiperazinones and their use as pharmaceuticals
AssigneeFab Pharma S.A.S.
InventorsVincent Gerusz, Sonia Escaich, Mayalen Oxoby, Francois Moreau
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Abstract
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.
Claims25
A compound of formula (I):
- wherein:
- W, X and Y independently represent CH2 or C=0, wherein said CH2 group may be optionally independently substituted by a fluorine or (C1-C6) alkyl group, wherein said (C1-C6) alkyl group may be further substituted by one or two R5 groups;
- R1 represents H, (C1-C6) alkyl optionally substituted by a CONRaRb group, (C2-C6) alkenyl, (C2-C6) alkynyl, phenyl or a —Z-Het group, such that Z represents a bond or a linker selected from CO, (C1-C6) alkylene or —CO—(C1-C6) alkylene and Het represents a 4-6 membered monocyclic saturated or unsaturated heterocycle containing 1-3 heteroatoms selected from N, O and S, wherein said phenyl or heterocycle group of R1 may be optionally substituted by one or more (e.g. 1, 2 or 3) R5 groups;
- R2 represents H, CO2Ra, CORa, CONRaRb, CH2ORc, CH2NRaRb, SO2NRaRb or P(O)ORaORb;
- R3 represents halogen, (C1-C6) alkyl, (C2-C6) alkenyl or (C2-C6) alkynyl;
- R4 represents H, halogen, CN or CH3;
- Ra, Rb and Rc independently represent H, (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, or an NRaR group may optionally form a 3- to 7-membered nitrogen containing saturated heterocycle optionally containing 1 to 3 additional heteroatoms selected from N, O or S wherein said heterocycle may be optionally substituted by one or more (C1-C6) alkyl groups;
- R5 represents halogen, CN, (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, CO2Ra, CORa, CONRaRb OCORa, ORa, NRaRb, ON═CRaRb, NRcCORa, NRcCOORa, OCONRaRb, NRcCONRaRb, NRcSO2Ra, S(O)nRa, or SO2NRaRb;
- n represents an integer selected from 0 to 2;
- or a pharmaceutically acceptable salt or solvate thereof.
7 more elements
Dependencies are inferred from the claim text.