Purified form of streptogramines, preparation of same and...

Details Purified form of streptogramines, preparation of same and... Purified form of streptogramines, preparation of same and...

C - Chemistry, Metallurgy

07

K

C07K 7/06 (2006.01) A61K 38/05 (2006.01) A61K 38/08 (2006.01) C07K 5/078 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2196450

Purified form of streptogramines, characterised in that it contains at least one component from group B streptogramines of general formula (I), wherein R1 is Me or Et, R2 is H or OH, and R3 is substituted benzyl of general formula (III), such that 1) if R2 is H, R is NR4R5, wherein one of R4 and R5 is H or an Me radical and the other is Me, and R' is Cl or Br, or R is (C3-5)alkenyl if R4 and R5 are Me, or 2) R is H and R' is halogen, alkylamino or dialkylamino, an ether-oxide residue, alkylthio, (C1-3)alkyl or trihalogenomethyl, or R is halogen, (C2-4)alkylamino, (C2-4)dialkylamino or methyl ethyl amino, pyrrolidino, alkenyl alkyl amino, dialkenylamino, an alkyl cycloalkylmethyl amino radical or an ether-oxide residue, alkylthio, alkylthiomethyl, (C1-6)alkyl, aryl or trihalogenomethyl, and R' is H, or R is halogen, amino, alkylamino or dialkylamino, an ether-oxide residue, an alkylthio radical, (C1-6)alkyl or trihalogenomethyl and R' is halogen, alkylamino or dialkylamino, an ether-oxide residue or alkylthio, (C1-3)alkyl, cocrystallised with one or more minor components of group A of general formula (II) wherein R'' is H, Me or Et.

Forme purifiée de streptogramines caractérisée en ce qu'elle comprend au moins une composante du groupe B des streptogramines de formule générale (I) dans laquelle R1 est Me ou Et, R2 est H ou OH, et R3 est benzyle substitué de formule générale (III) pour lequel 1) si R2 est H, R est NR4R5 pour lequel R4 et R5 sont l'un H ou un radical Me et l'autre Me et R' est Cl ou Br, ou R est alcényle (3 à 5C) si R4 et R5 sont Me, ou bien 2) R est H et R' est halogène, alcoylamino ou dialcoylamino, un reste éther-oxyde, alcoylthio, alcoyle (1 à 3C) ou trihalogénométhyle, ou R est halogène, alcoylamino (2 à 4C), dialcoylamino (2 à 4C) ou méthyl éthyl amino, pyrrolidino, alcényl alcoyl amino, dialcénylamino, un radical alcoyl cycloalcoylméthyl amino, ou bien un reste éther-oxyde, alcoylthio, alcoylthiométhyle, alcoyle (1 à 6C), aryle ou trihalogénométhyle, et R' est H ou bien R est d'halogène, amino, alcoylamino ou dialcoylamino, un reste éther-oxyde, un radical alcoylthio, alcoyle (1 à 6C) ou trihalogénométhyle et R' est halogène, alcoylamino ou dialcoylamino, un reste éther-oxyde ou alcoylthio, alcoyle (1 à 3C), cocristallisée avec au moins une composante "minoritaire" du groupe A de formule générale (II) dans laquelle R" est H, Me ou Et.

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