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1. Compounds of the following formula I: wherein: X and X′ represent independently from each other O or S, and a) R1, R2, R3, R4, R5, R′1, R′2, R′3, R′4 and R′5 represent independently from each other:
H,a linear or branched (C1-C7)alkyl, if appropriate substituted by: a halogen, a hydroxyl group, a ORa or NRaRb, wherein Ra and Rb represent: H, a linear or branched (C1-C7)-alkyl, a (C3-C7)-cycloalkyl, an aryl substituted or not, CH2-aryl, CO—(C1-C7)-alkyl, CO-aryl, CO2—(C1-C7)-alkyl, CO2-aryl, wherein aryl is a substituted or not aromatic group or a substituted or not heteroaromatic group
a (C3-C7)-cycloalkyl, an aryl substituted or not, CH2-aryl, CO—(C1-C7)-alkyl, CO-aryl, CO2—(C1-C7)-alkyl, CO2-aryl, wherein aryl is a substituted or not aromatic group or a substituted or not heteroaromatic group,F, Cl, Br, I, CF3, OH, ORa, OCF3, COCF3, NH2, NHRa, NRaRb, wherein Ra and Rb represent: H, a linear or branched (C1-C2)-alkyl, a (C3-C2)-cycloalkyl, an aryl substituted or not, CH2-aryl, CO—(C1-C2)-alkyl, CO-aryl, CO2—(C1-C2)-alkyl, CO2-aryl, wherein aryl is a substituted or not aromatic group or a substituted or not heteroaromatic group,
CN and NO2 provided that R1, R2, R3, R4, R5, R′1 are different from CN and NO2.(CH2)n—Z, —(CH2)b—OH, —(CH2)n—CO2—(C1-C2)-alkyl, —(CH2)n—CO2 wherein n=2 to 12, Z is an halogen, and alkyl being as defined above. R represents H, a (C1-C2)-alkyl, CH2NHCO2—(C1-C2) CH2NHCO2—(C3-C2)-cycloalkyl, CO2H, CO2—(C1-C2)-alkyl, CO2—(C3-C7)-cycloalkyl, (CH2)nOH, CH2NH(CH2)b—OH, CH2NH(CH2)b—NRaRb, CONH—(C1-C7)-alkyl, CONH—(C3-C2)-cycloalkyl, CONH-aryl, CONH—(CH2)nOH, CONH—(CH2)nN. RaRn, wherein n=2 to 12 and Ra, Rb, aryl and alkyl being as defined above. R6 and R′6 represent independently from each other H, (C1-C2)-alkyl, SO2aryl, wherein aryl being as defined above, OH, O—(C1-C2)-alkyl, CO—(C1-C2)-alkyl, CO-aryl, CH2NH2, CH2NHRa, CH2NaRb, Si(Rc)3, the Rc groups being identical or different and representing independently of each other a linear or branched (C1-C7)-alkyl, a (C3-C7)-cycloalkyl, or an aryl, aryl and alkyl being as defined above, R7 represents H, OH, ORa, Ra being as defined above, or b) R and R7 are joined together to form a cycle of formula I-a: wherein Y represents:
N—R8 wherein R8 represents H, (C1-C7)-alkyl, (C3-C7)-cycloalkyl, CO—(C1-C7)-alkyl, CO—(C3-C7)-cycloalkyl, CO2—(C1-C7)-alkyl, CO2—(C3-C7)-cycloalkyl,O,S,CH2, CHR8 wherein R8 represents (C1-C7)-alkyl, (C3-C7)-cycloalkyl, CO—(C1-C7)-alkyl, CO—(C3-C7)-cycloalkyl, CO2—(C1-C7)-alkyl, CO2—(C3-C7)-cycloalkyl,m=0, 1 said cycle being optionally substituted by OH, a linear or branched O(C1-C7)-alkyl, a O(C3-C7)-cycloalkyl, NH2, or NRaRb, Ra and Rb being as defined above, R1, R2, R3, R4, R5, R′1, R′2, R′3, R′4, R′5, R6 and R′6 being as defined above, or c) R and R7 are joined together to form a cycle of formula I-b: wherein Y represents:
C, CR8 wherein R8 represents (C1-C7)-alkyl, (C3-C7)-cycloalkyl, CO—(C1-C7)-alkyl, CO—(C3-C7)-cycloalkyl, CO2—(C1-C7)-alkyl, CO2—(C3-C7)-cycloalkyl,m=1 R1, R2, R3, R4, R5, R′1, R′2, R′3, R′4, R′5, R6 and R′6 being as defined above, and their pharmaceutically acceptable salts, for use as a medicament, suitable especially for an antibacterial activity and/or NorA efflux pump inhibitor. |
