Purified form of streptogramins, its preparation and pharmaceutical
compositions containing it
    1.
    发明授权
    Purified form of streptogramins, its preparation and pharmaceutical compositions containing it 失效
    纯化形式的链霉素,其制剂和含有它的药物组合物

    公开(公告)号:US5726151A

    公开(公告)日:1998-03-10

    申请号:US472767

    申请日:1995-06-07

    CPC classification number: C07K5/06182 C07K5/06139 C07K7/06 A61K38/00

    Abstract: This invention relates to a purified form of streptogramins, having of a combination of one or more group B components of streptogramins, of general formula: ##STR1## in which A.sub.1 is a radical of general formula: ##STR2## for which R' is H or OH and Y is H, a methylamino radical or a dimethylamino radical, R is an ethyl radical or, when R' is H, R can also represent--CH.sub.3, andR.sub.1 and R.sub.2 are H, or alternatively A.sub.1 is a radical of formula: ##STR3## R is an isobutyl radical, and R.sub.1 is OH and R.sub.2 is --CH.sub.3, and one or more group A minority components of streptogramins, of general formula: ##STR4## in which R" is H or a methyl or ethyl radical, in the state of cocrystallizate, of a coprecipitate or of a physical mixture of the powders.

    Abstract translation: 本发明涉及一种纯化形式的链霉素,其具有一种或多种链霉素的一种或多种B组分组合,其通式如下:其中A1是通式如下的基团:,其中 R'是H或OH,Y是H,甲基氨基或二甲基氨基,R是乙基,或当R'是H时,R也可以表示-CH 3,R 1和R 2是H,或者A1是 式的基团:R 1是异丁基,R 1是OH,R 2是-CH 3,以及一个或多个通式为:其中R“是H的链霉素的少数成分,其中R”是H或 以共沉淀物或粉末的物理混合物的共结晶状态的甲基或乙基。

    Purified form of streptogramines, preparation of same and pharmaceutical compositions containing them
    2.
    发明授权
    Purified form of streptogramines, preparation of same and pharmaceutical compositions containing them 失效
    纯化形式的链球菌素,其制备物和含有它们的药物组合物

    公开(公告)号:US06384014B1

    公开(公告)日:2002-05-07

    申请号:US09522949

    申请日:2000-03-10

    CPC classification number: C07K5/06182 A61K38/00 C07K7/06

    Abstract: 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, dialkylamino, an alkyl cycloalkylmethyl amino radical or in 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.

    Abstract translation: 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,吡咯烷基链烯基烷基氨基,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,芳基或三卤代甲基,R' ,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,醚氧化物 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。

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