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    3-phenyl-2-propeneamine derivatives, their preparation and composition containing them
    2.
    发明授权
    3-phenyl-2-propeneamine derivatives, their preparation and composition containing them 失效
    3-苯基-2-丙烯胺衍生物，它们的制备方法和含有它们的组合物

    公开(公告)号：US4755599A

    公开(公告)日：1988-07-05

    申请号：US10558

    申请日：1987-02-03

    申请人： Jean-Claude Barriere ,  Jean-Pierre Corbet ,  Claude Cotrel ,  Daniel Farge ,  Jean-Marc Paris

    发明人： Jean-Claude Barriere ,  Jean-Pierre Corbet ,  Claude Cotrel ,  Daniel Farge ,  Jean-Marc Paris

    IPC分类号： A61K31/135 ,  A61K31/10 ,  A61K31/137 ,  A61K31/21 ,  A61K31/22 ,  A61P25/24 ,  A61P25/26 ,  C07C67/00 ,  C07C213/00 ,  C07C213/02 ,  C07C215/28 ,  C07C215/30 ,  C07C215/42 ,  C07C219/22 ,  C07C219/32 ,  C07C239/00 ,  C07C271/20 ,  C07C313/00 ,  C07C317/28 ,  C07C317/36 ,  C07C319/20 ,  C07C323/27 ,  C07C323/32 ,  C07C323/65 ,  C07D207/08 ,  C07D213/38 ,  C07D213/70 ,  C07D295/084 ,  C07D295/092 ,  C07D307/32 ,  C07F9/40 ,  C07D279/04 ,  C07C149/24 ,  C07D205/04 ,  C07D223/04 ,  C07D275/02 ,  C07D277/04 ,  C07D401/06

    CPC分类号： C07D207/08 ,  C07D213/38 ,  C07D213/70 ,  C07D295/092 ,  C07D307/32 ,  C07F9/4006

    摘要： The invention provides compounds of formula: ##STR1## in which R=H, halogen, alkyl, alkyloxy, alkythio, NH.sub.2, alkylamino, dialkylamino or CF.sub.3, R.sub.3 =H or alkyl,either R.sub.4 and R.sub.5 =H and R.sub.1 and R.sub.2 =H or alkyl, optionally substituted by alkenyl (2 to 4 C) or alternatively R.sub.1 and R.sub.2 form together a saturated heterocyclic ring containing 4 to 7 ring members and optionally containing another heteroatom such as O, S or N optionally substituted by alkyl,or R.sub.4 =H, R.sub.1 =H or alkyl and R.sub.2 and R.sub.5 together form an alkylene (3 to 4 C) radical and(i) either A=alkyl or phenyl which is unsubstituted or substituted by one or two substituents chosen from halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 or alternatively A=pyridyl, benzyl or cycloalkyl (3 to 6 C), Y=S, SO or SO.sub.2 or a radical: ##STR2## in which R.sub.6 =H or alkyl and R.sub.7 =H or alkylcarbonyl, alkyloxycarbonyl, alkylaminocarbonyl or benzoyl, optionally substituted by one or two halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 groups,(ii) or Y and A together form a 1-hydroxycycloalkyl radical, the ring of which contains 5 or 6 C, optionally joined to a benzene ring,it being understood that the alkyl radicals and alkyl parts contains 1 to 4 C as a straight or branched chain, and that the invention relates to all the possible geometric and optical isomers as well as their mixtures.These compounds are useful as antidepressants.

    摘要翻译： 本发明提供下式的化合物：其中R = H，卤素，烷基，烷氧基，链烯基，NH 2，烷基氨基，二烷基氨基或CF 3，R 3 = H或烷基，R 4和R 5 = H，R 1和 R 2 = H或烷基，任选被烯基（2至4 C）取代，或者R 1和R 2一起形成含有4至7个环成员的饱和杂环，并任选地含有另外的杂原子，例如任选被烷基取代的O，S或N， 或R4 = H，R1 = H或烷基，R2和R5一起形成亚烷基（3至4 C）基团，和（i）A =烷基或苯基，其未被取代或被一个或两个选自卤素，烷基 ，烷氧基，烷硫基，NH 2，烷基氨基，二烷基氨基，NO 2或CF 3，或者A =吡啶基，苄基或环烷基（3至6 C），Y = S，SO或SO 2或基团：其中R 6 = H或烷基，且R7 = H或烷基羰基，烷氧基羰基，烷基氨基羰基或苯甲酰基，任选被一个或两个卤素，烷基，烷氧基，烷硫基，NH 2， 烷基氨基，二烷基氨基，NO 2或CF 3基团，（ii）或Y和A一起形成1-羟基环烷基，其环包含5或6个C，任选地连接到苯环，应理解烷基和烷基 部分包含1至4 C作为直链或支链，本发明涉及所有可能的几何和光学异构体及其混合物。 这些化合物可用作抗抑郁药。

    3-phenyl-2-propeneamine derivatives, their preparation and compositions containing them
    3.
    发明授权
    3-phenyl-2-propeneamine derivatives, their preparation and compositions containing them 失效
    3-苯基-2-丙烯胺衍生物，它们的制备方法和含有它们的组合物

    公开(公告)号：US4686309A

    公开(公告)日：1987-08-11

    申请号：US702088

    申请日：1985-02-15

    申请人： Jean-Claude Barriere ,  Jean-Pierre Corbet ,  Claude Cotrel ,  Daniel Farge ,  Jean-Marc Paris

    发明人： Jean-Claude Barriere ,  Jean-Pierre Corbet ,  Claude Cotrel ,  Daniel Farge ,  Jean-Marc Paris

    IPC分类号： A61K31/135 ,  A61K31/10 ,  A61K31/137 ,  A61K31/21 ,  A61K31/22 ,  A61P25/24 ,  A61P25/26 ,  C07C67/00 ,  C07C213/00 ,  C07C213/02 ,  C07C215/28 ,  C07C215/30 ,  C07C215/42 ,  C07C219/22 ,  C07C219/32 ,  C07C239/00 ,  C07C271/20 ,  C07C313/00 ,  C07C317/28 ,  C07C317/36 ,  C07C319/20 ,  C07C323/27 ,  C07C323/32 ,  C07C323/65 ,  C07D207/08 ,  C07D213/38 ,  C07D213/70 ,  C07D295/084 ,  C07D295/092 ,  C07D307/32 ,  C07F9/40 ,  C07C91/16 ,  C07C67/02 ,  C07D211/70

    CPC分类号： C07D207/08 ,  C07D213/38 ,  C07D213/70 ,  C07D295/092 ,  C07D307/32 ,  C07F9/4006

    摘要： The invention provides compounds of formula: ##STR1## in which R=H, halogen, alkyl, alkyloxy, alkythio, NH.sub.2, alkylamino, dialkylamino or CF.sub.3, R.sub.3 =H or alkyl, either R.sub.4 and R.sub.5 =H and R.sub.1 and R.sub.2 =H or alkyl, optionally substituted by alkenyl (2 to 4 C) or alternatively R.sub.1 and R.sub.2 form together a saturated heterocyclic ring containing 4 to 7 ring members and optionally containing another heteroatom such as O, S or N optionally substituted by alkyl, or R.sub.4 =H, R.sub.1 =H or alkyl and R.sub.2 and R.sub.5 together form an alkylene (3 to 4 C) radical and (i) either A=alkyl or phenyl which is unsubstituted or substituted by one or two substituents chosen from halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 or alternatively A=pyridyl, benzyl or cycloalkyl (3 to 6C), Y=S, SO or SO.sub.2 or a radical: ##STR2## in which R.sub.6 =H or alkyl and R.sub.7 =H or alkylcarbonyl, alkyloxycarbonyl, alkylaminocarbonyl or benzoyl, optionally substituted by one or two halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 groups, (ii) or Y and A together form a 1-hydroxycycloalkyl radical, the ring of which contains 5 or 6 C, optionally joined to a benzene ring, it being understood that the alkyl radicals and alkyl parts contain 1 to 4 C as a straight or branched chain, and that the invention relates to all the possible geometric and optical isomers as well as their mixtures.These compounds are useful as antidepressants.

    摘要翻译： 本发明提供下式的化合物：其中R = H，卤素，烷基，烷氧基，链烯基，NH 2，烷基氨基，二烷基氨基或CF 3，R 3 = H或烷基，R 4和R 5 = H，R 1和 R 2 = H或烷基，任选被烯基（2至4 C）取代，或者R 1和R 2一起形成含有4至7个环成员的饱和杂环，并任选地含有另外的杂原子，例如任选被烷基取代的O，S或N， 或R4 = H，R1 = H或烷基，R2和R5一起形成亚烷基（3至4 C）基团，和（i）A =烷基或苯基，其未被取代或被一个或两个选自卤素，烷基 ，烷氧基，烷硫基，NH 2，烷基氨基，二烷基氨基，NO 2或CF 3，或者A =吡啶基，苄基或环烷基（3至6C），Y = S，SO或SO 2或基团：其中R 6 = H或烷基，R 7 = H或烷基羰基，烷氧基羰基，烷基氨基羰基或苯甲酰基，任选被一个或两个卤素，烷基，烷氧基，烷硫基，NH 2， 烷基氨基，二烷基氨基，NO 2或CF 3基团，（ii）或Y和A一起形成1-羟基环烷基，其环含有5或6个C，任选地连接到苯环，应理解烷基和烷基 部分含有1至4个C作为直链或支链，本发明涉及所有可能的几何和光学异构体及其混合物。 这些化合物可用作抗抑郁药。

    New process for the preparation of pristinamycin II.sub.B derivatives
    4.
    发明授权
    New process for the preparation of pristinamycin II.sub.B derivatives 失效
    制备原始蛋白霉素IIB衍生物的新方法

    公开(公告)号：US4775753A

    公开(公告)日：1988-10-04

    申请号：US70389

    申请日：1987-07-07

    申请人： Jean-Claude Barriere ,  Jean-Pierre Bastart ,  Jean-Marc Paris

    发明人： Jean-Claude Barriere ,  Jean-Pierre Bastart ,  Jean-Marc Paris

    IPC分类号： C07D498/18 ,  A61K31/42 ,  A61P31/04 ,  C07D498/14 ,  C07K5/06 ,  C07K5/078

    CPC分类号： C07D498/14 ,  C07K5/06182

    摘要： 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.

    摘要翻译： 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。

    Streptogramin derivatives, their preparation and pharmaceutical compositions which contain them
    7.
    发明授权
    Streptogramin derivatives, their preparation and pharmaceutical compositions which contain them 失效
    链球菌素衍生物，它们的制备和含有它们的药物组合物

    公开(公告)号：US5786449A

    公开(公告)日：1998-07-28

    申请号：US776665

    申请日：1997-01-31

    申请人： Jean-Claude Barriere ,  Jean-Marc Paris ,  Gerard Puchault

    发明人： Jean-Claude Barriere ,  Jean-Marc Paris ,  Gerard Puchault

    IPC分类号： A61K38/00 ,  A61P31/04 ,  A61P43/00 ,  C07K7/06 ,  C07K11/02 ,  A61K38/12 ,  C07K5/00 ,  C07K7/00 ,  C07K17/00

    CPC分类号： C07K7/06 ,  A61K38/00

    摘要： Streptogramine derivatives of general formula (I) below, wherein the radical R.sub.1 is a methyl or ethyl radical, the radical R.sub.2 is a bromine or chlorine atom, or is an alkenyl radical with 3 to 5 carbon atoms when R.sub.3 and R.sub.4 are methyl, and one of R.sub.3 and R.sub.4 is a hydrogen atom or a methyl radical and the other is a methyl radical are disclosed. The streptogramine derivatives of general formula (I) have particularly useful antibacterial properties, and may be used in combination with a pristinamycin II derivative. ##STR1##

    摘要翻译： PCT No.PCT / FR95 / 01025 Sec。 371日期1997年1月31日 102（e）日期1997年1月31日PCT提交1995年7月31日PCT公布。 第WO96 / 04299号公报 日期：1996年2月15日下面通式（I）的直链衍生物，其中基团R 1是甲基或乙基，基团R 2是溴或氯原子，或者当R 3和R 3是具有3至5个碳原子的烯基时 R4是甲基，R3和R4之一是氢原子或甲基，另一个是甲基。 通式（I）的链霉素衍生物具有特别有用的抗菌性质，并且可以与普瑞霉素II衍生物组合使用。

    Purified form of streptogramines, preparation of same and pharmaceutical compositions containing them
    10.
    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

    申请人： Pascal Anger ,  Jean-Claude Barriere ,  Bertrand Bonnavaud ,  Patrick Lefevre ,  Jean-Marc Paris ,  Denis Thibaut

    发明人： Pascal Anger ,  Jean-Claude Barriere ,  Bertrand Bonnavaud ,  Patrick Lefevre ,  Jean-Marc Paris ,  Denis Thibaut

    IPC分类号： A61K3812

    CPC分类号： C07K5/06182 ,  A61K38/00 ,  C07K7/06

    摘要： 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.

    摘要翻译： 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。