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    • 3. 发明授权
    • Purified form of streptogramines, preparation of same and pharmaceutical compositions containing them
    • 纯化形式的链球菌素,其制备物和含有它们的药物组合物
    • US06384014B1
    • 2002-05-07
    • US09522949
    • 2000-03-10
    • Pascal AngerJean-Claude BarriereBertrand BonnavaudPatrick LefevreJean-Marc ParisDenis Thibaut
    • Pascal AngerJean-Claude BarriereBertrand BonnavaudPatrick LefevreJean-Marc ParisDenis Thibaut
    • A61K3812
    • 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, 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.
    • 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。
    • 4. 发明授权
    • New process for the preparation of pristinamycin II.sub.B derivatives
    • 制备原始蛋白霉素IIB衍生物的新方法
    • US4775753A
    • 1988-10-04
    • US70389
    • 1987-07-07
    • Jean-Claude BarriereJean-Pierre BastartJean-Marc Paris
    • Jean-Claude BarriereJean-Pierre BastartJean-Marc Paris
    • C07D498/18A61K31/42A61P31/04C07D498/14C07K5/06C07K5/078
    • C07D498/14C07K5/06182
    • Pristinamycin II.sub.B derivatives of formula I in which R represents: ##STR1## either a 4- to 7-membered nitrogen-containing heterocyclic radical, optionally containing 1 or more other hetero atoms chosen from nitrogen, oxygen and sulphur in the sulphoxide or sulphone form, and unsubstituted or substituted by alkyl,or alkyl of 2 to 4 carbon atoms, substituted by 1 or 2 radicals chosen from phenyl, cycloalkylamino or N-alkyl-N-cycloalkylamino having 3 to 6 ring carbon atoms, alkylamino, dialkylamino or dialkylcarbamoyloxy (the alkyl parts of these last 2 radicals being optionally joined to form, with the nitrogen atom to which they are attached, a 4- to 7-membered saturated or unsaturated heterocycle optionally containing another hetero atom chosen from nitrogen, oxygen and sulphur in the sulphoxide or sulphone form, and unsubstituted or substituted by alkyl) or a said alkyl substituted by one or more 4- or 7-membered nitrogen-containing heterocycles optionally containing 1 or 2 other hetero atoms chosen from nitrogen, oxygen and sulphur in the sulphoxide or sulphone form and unsubstituted or substituted by an alkyl radical, the said heterocycles being attached to the alkyl via a carbon atom, at least one of the substituents carried by the alkyl being a nitrogen-containing substituent capable of forming salts,or a [(S)-1-methyl-2-pyrrolidinyl]methyl radical, the aforesaid alkyl radicals being straight-chain or branched and containing, unless otherwise stated, 1 to 10 carbon atoms each, including isomeric forms thereof and mixtures thereof, and the salts thereof, are made by oxidizing a pristinamycin II.sub.B derivative of formula II ##STR2## with potassium peroxymonosulphate.
    • 式I的普瑞霉素IIB衍生物,其中R表示:(I)4-元至7-元含氮杂环基,任选地含有1或多个选自亚砜中的氮,氧和硫的其它杂原子,或 砜基形式,未取代的或被烷基取代或被2至4个碳原子的烷基取代,被1或2个选自苯基,环烷基氨基或具有3至6个环碳原子的N-烷基-N-环烷基氨基的基团取代,烷基氨基,二烷基氨基或 二烷基氨基甲酰氧基(这些最后2个基团的烷基部分任选地连接形成与它们所连接的氮原子一起形成4-7元饱和或不饱和的杂环,任选地含有另外选自氮,氧和硫的杂原子) 亚砜或砜形式,未取代或被烷基取代)或被一个或多个4-或7-元含氮杂环取代的所述烷基,任选地含有1或2个其它h 选自氮,氧和硫的亚杂原子或未被取代或被烷基取代的杂原子,所述杂环经由碳原子连接到烷基上,烷基所携带的至少一个取代基是氮 (S)-1-甲基-2-吡咯烷基]甲基,上述烷基是直链或支链的并且除非另有说明,含有各自为1-10个碳原子, 包括其异构体形式及其混合物及其盐通过用过氧单硫酸钾与过氧化硫酸盐钾一起氧化式II的嘌呤霉素IIB衍生物来制备。
    • 8. 发明授权
    • Pristinamycin II.sub.B derivatives and compositions containing them
    • 普瑞霉素IIB衍生物和含有它们的组合物
    • US4668669A
    • 1987-05-26
    • US817548
    • 1986-01-10
    • Jean-Claude BarriereClaude CotrelJean-Marc Paris
    • Jean-Claude BarriereClaude CotrelJean-Marc Paris
    • C07D498/18A61K31/42A61P31/04C07D498/14C07K5/078C07K5/12
    • C07K5/06182Y10S930/19Y10S930/27
    • Pristinamycin II.sub.B derivatives of formula: ##STR1## in which R denotes a nitrogen-containing 4 to 7-membered heterocyclic ring optionally substituted by alkyl; or alkyl (2 to 4 C) substituted by 1 or 2 phenyl, cycloalkylamino or N-alkyl-N-cycloalkylamino (3 to 6 ring atoms), alkylamino, dialkylamino or dialkylcarbamoyloxy radicals (the dialkylamino moieties of these 2 latter radicals being capable of forming a 4 to 7-membered cyclic ring optionally substituted by alkyl) or substituted by 1 or 2 nitrogen-containing 4 to 7 membered heterocyclic rings, optionally substituted by alkyl, at least one of the above substituents being a nitrogen-containing substituent capable of forming salts and n is 1 or 2, all the alkyls being linear or branched and containing (unless stated otherwise) 1 to 10 carbon atoms, their isomers, their salts and their preparation. These compounds, optionally in combination with known synergistins or synergistins of formula: ##STR2## are useful as antimicrobial agents.
    • 其中R表示任选被烷基取代的含氮4〜7元杂环的普拉霉素IIB衍生物: 或被1或2个苯基,环烷基氨基或N-烷基-N-环烷基氨基(3至6个环原子),烷基氨基,二烷基氨基或二烷基氨基甲酰氧基取代的(2至4 C)烷基(这2个后基团的二烷基氨基部分能够 形成任选被烷基取代的4至7元环)或被1或2个含氮的4至7元杂环取代,任选被烷基取代,至少一个上述取代基是含氮取代基,其能够 形成盐,n为1或2,所有烷基均为直链或支链,并含有(除非另有说明)1至10个碳原子,它们的异构体及其盐及其制备。 这些化合物,任选地与已知的增效剂或下式的协同增效剂组合:可用作抗微生物剂。