Derivatives of antibiotic ge2270 factors c2a, d2 and e

Details Derivatives of antibiotic ge2270 factors c2a, d2 and e Derivatives of antibiotic ge2270 factors c2a, d2 and e

C - Chemistry, Metallurgy

07

K

C07K 5/078 (2006.01) A61K 38/05 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2242067

Mono- or di-substituted derivatives of GE2270 factors C2a, D2 and E of general formula (I), wherein W represents a moiety of formula (a), (b) or (c), R1 and R2 representing a variety of substituents, X1 is methyl, X2 is a -CH2-W1 moiety and X3 is methylamino or amino, or X1 is a -CH2-W1 moiety, X2 is methoxymethylene and X3 is methylamino, with the proviso that when X3 is amino, then W must be 2-(aminocarbonyl)-pyrrolidinyl; with the further proviso that when W is 2-(aminocarbonyl)-pyrrolidinyl, then W1 cannot be hydroxy; and the pharmaceutically acceptable salts thereof. The mono- or di-substituted derivatives of antibiotic GE 2270 of formula (I) are antimicrobial agents mainly active against gram positive bacteria.

L'invention concerne des dérivés mono ou bisubstitués des facteurs C¿2a?, D¿2? et E de l'antibiotique GE2270, de formule générale (I), où W représente une fraction de formule (a), (b) ou (c), R?1¿ et R?2¿ représentant toute une variété de substituants, X?1¿ est méthyle, X?2¿ est une fraction -CH¿2?-W?1¿, et X?3¿ est méthylamino ou amino, ou bien X?1¿ est une fraction -CH¿2?-W?1¿, X?2¿ est méthoxyméthylène et X?3¿ est méthylamino, à condition que quand X?3¿ est amino, W soit 2-(aminocarbonyl)-pyrrolidinyle, et à condition également que quand W est 2-(aminocarbonyl)-pyrrolidinyle, W?1¿ ne soit pas hydroxy. L'invention concerne également les sels pharmaceutiquement acceptables des dérivés mono ou bisubstitués de l'antibiotique GE2270 de formule (I). Ces dérivés sont des agents antimicrobiens principalement actifs contre les bactéries Gram positif.

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