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    • 10. 发明申请
    • PURIFIED FORM OF STREPTOGRAMINES, PREPARATION OF SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
    • 结构形式的纯化形式,其制备方法和含有其的药物组合物
    • WO1996004298A1
    • 1996-02-15
    • PCT/FR1995001026
    • 1995-07-31
    • RHONE-POULENC RORER S.A.ANGER, PascalBARRIERE, Jean-ClaudeBONNAVAUD, BertrandLEFEVRE, PatrickPARIS, Jean-MarcTHIBAUT, Denis
    • RHONE-POULENC RORER S.A.
    • C07K05/078
    • C07K5/06182A61K38/00C07K7/06
    • 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.
    • 其特征在于,其含有至少一种通式(I)的B组链霉素的组分,其中R 1是Me或Et,R 2是H或OH,R 3是通式(III)的取代的苄基, 使得1)如果R 2是H,R 4是NR 4 R 5,其中R 4和R 5之一是H或Me基团,而另一个是Me,R'是Cl或Br,或R 4是(C 3-5)烯基,如果R 4 和R 5是Me,或2)R是H,R'是卤素,烷基氨基或二烷基氨基,醚氧化物残基,烷硫基,(C 1-3)烷基或三卤代甲基,或R是卤素,(C 2-4)烷基氨基, (C 2-4)二烷基氨基或甲基乙基氨基,吡咯烷子基,烯基烷基氨基,二烷基氨基,烷基环烷基甲基氨基或醚氧化物残基,烷硫基,烷硫基甲基,(C 1-6)烷基,芳基或三卤甲基,R' H或R是卤素,氨基,烷基氨基或二烷基氨基,醚氧化物残基,烷硫基,(C 1-6)烷基或三卤代甲基,R'是卤素,烷基氨基或二烷基氨基,醚 - 氧基 残基或烷硫基,(C 1-3)烷基,与通式(II)的基团A的一种或多种次要组分共结晶,其中R“为H,Me或Et。