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US 2014/0275191 A1Published application
Novel 1,2,4- oxadiazol compounds active against gram-positive pathogens
AssigneesIstituto Euro Mediterraneo Di Scienza E Tecnologia, Universita Degli Studi Di Milano-Bicocca
InventorsRosario MUSUMECI, Clementina Elvezia Anna COCUZZA, Cosimo Gianluca FORTUNA, Andrea PACE, Antonio PALUMBO PICCIONELLO
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Abstract
The present invention relates to novel oxazolidinone compounds of general formula (I) having antibiotic activity also against multiresistant bacterial strains.
Claims27
Compounds of general formula (I):
- as racemic mixtures or pure enantiomers or mixtures enriched with one of the S or R enantiomer,
- where:
- X, Y, Z are independently:
- CH, O, N, S, with at least two heteroatoms;
- R=H, F, Cl, Br, I, (C1-C3)alkyl (methyl, ethyl, n-propyl, iso-propyl), (C3-C6)cyclo-alkyl, aryl, heteroaryl, NH2, OH, SH, NHR6, N(R6)2, OR6 with R6=(C1-C3)alkyl, (C3-C6)cyclo-alkyl, aryl, heteroaryl, (C1-C4)acyl;
- R1-4=independently H or F or Cl or Br;
- R5=—NH2;
- —OH;
- —NHC(X)CH3 with X=O or S;
- —NHC(X)CH2Z with X=O, S and Z=F, Cl;
- —NHC(X)CHZ2 with X=O, S, Z=F, Cl;
- —NHC(X)CZ3 with X=O, S, Z=F, Cl;
- —NHC(X)NHR7 with X=O, S, R7=H, (C1-C3)alkyl, (C3-C6)cyclo-alkyl, aryl, heteroaryl, (C1-C3)acyl, or N-substituted azoles such as 1,2,3-triazole for the use in the treatment of infections caused by Gram-positive bacteria.
10 more elements
A pharmaceutical composition containing a compound having the general formula (I):
- as racemic mixtures or pure enantiomers or mixtures enriched with one of the S or R enantiomer,
- where:
- X, Y, Z are independently:
- CH, O, N, S, with at least two heteroatoms;
- R=H, F, Cl, Br, I, (C1-C3)alkyl (methyl, ethyl, n-propyl, iso-propyl), (C3-C6)cyclo-alkyl, aryl, heteroaryl, NH2, OH, SH, NHR6, N(R6)2, OR6 with R6=(C1-C3)alkyl, (C3-C6)cyclo-alkyl, aryl, heteroaryl, (C1-C4)acyl;
- R1-4=independently H or F or Cl or Br;
- R5=—NH2;
- —OH;
- —NHC(X)CH3 with X=O or S;
- —NHC(X)CH2Z with X=O, S and Z=F, Cl;
- —NHC(X)CHZ2 with X=O, S, Z=F, Cl;
- —NHC(X)CZ3 with X=O, S, Z=F, Cl;
- —NHC(X)NHR7 with X=O, S, R7=H, (C1-C3)alkyl, (C3-C6)cyclo-alkyl, aryl, heteroaryl, (C1-C3)acyl, or N-substituted azoles such as 1,2,3-triazole for the use in the treatment of infections caused by Gram-positive bacteria, and a pharmaceutically acceptable excipient.
10 more elements
Dependencies are inferred from the claim text.