C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 498/14 (2006.01) A61K 31/4745 (2006.01) A61P 31/04 (2006.01) C07D 401/04 (2006.01) C07D 401/12 (2006.01) C07F 7/00 (2006.01)
Patent
CA 2616977
The invention relates to novel chimeric antibiotics of formula (I) Wherein R1 is CH2NHCOR5, heteroarylmethyl, heteroaryloxymethyl or heteroarylaminomethyl; R2 is H, OH, OSO3H, OPO3H2, OCH2OPO3H2, OCOCH2CH2COOH, OCOR6; R3 is H or halogen; R4 is (C1-C3)alkyl, (C1-C3)haloalkyl or cycloalkyl; R5 is alkyl or haloalkyl; and R6 is the residue of a naturally occurring amino acid or of dimethylaminoglycine. These chimeric compounds are useful in the manufacture of medicaments for the treatment of infections (e.g. bacterial infections).
L'invention concerne de nouveaux antibiotiques chimériques représentés par la formule (I), dans laquelle R1 représente CH2NHCOR5, hétéroarylméthyle, hétéroaryloxyméthyle ou hétéroarylaminométhyle ; R2 représente H, OH, OSO3H, OPO3H2, OCH2OPO3H2, OCOCH2CH2COOH, OCOR6; R3 représente H ou halogène ; R4 représente (C1-C3)alkyle, (C1-C3)haloalkyle ou cycloalkyle ; R5 représente alkyle ou haloalkyle ; et R6 représente le résidu d'un acide aminé naturel ou de diméthylaminoglycine. Ces composés chimériques conviennent pour la fabrication de médicaments destinés au traitement d'infections (par exemple, les infections bactériennes).
Hubschwerlen Christian
Panchaud Philippe
Sigwalt Christine
Specklin Jean-Luc
Actelion Pharmaceuticals Ltd
Gowling Lafleur Henderson Llp
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