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US 8,618,100 B2Granted
Compounds with antibacterial activity against Clostridium
AssigneeElanco Animal Health Ireland Limited
InventorsJerome Emile Georges Guillemont, Pierre Jean-Marie Bernard Raboisson, Nacer Lounis
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Abstract
The present invention is related to novel compounds of formula (I) having antibacterial activity against Clostridium bacteria, in particular Clostridium perfringens, pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
Claims15
A compound of formula (I)
- including any stereochemically isomeric form and tautomer thereof, wherein:
- R1 and R2 are each independently selected from hydrogen, halo, hydroxy, C1 -6alkyl, polyhaloC1-6alkyl, C1-6alkyloxy, or polyhaloC1-6alkyloxy;
- R3 is hydroxy, amino, mono- or di(C1-4alkyl)amino;
- R4 is hydrogen or C1-4alkyl;
- X is nitrogen or CR5 wherein R5 is hydrogen, halo or C1-4alkyl;
- provided that when R3 is hydroxy then X is CH and R4 is hydrogen;
- or a pharmaceutically acceptable acid addition salt thereof, or a solvate thereof.
4 more elements
A process for preparing a compound of formula (I)
- including any stereochemically isomeric form and tautomer thereof, or a pharmaceutically acceptable acid addition salt thereof, or a solvate thereof, comprising:
- N-alkylating a compound of formula (II) with a compound of formula (III)
- wherein R1 and R2 are each independently selected from hydrogen, halo, hydroxy, C1-6alkyl, polyhaloC1-6alkyl, C1-6alkyloxy, or polyhaloC1-6alkyloxy;
- R3 is hydroxy, amino, mono- or di(C1-4alkyl)amino;
- R4 is hydrogen or C1-4alkyl;
- X is nitrogen or CR5 wherein R5 is hydrogen, halo or C1-4alkyl;
- provided that when R3 is hydroxy then X is CH and R4 is hydrogen.
4 more elements
Dependencies are inferred from the claim text.