公开(公告)号：US20060167253A1

公开(公告)日：2006-07-27

申请号：US10523753

申请日：2003-08-07

申请人： Didier Philippe Schils ,  Joannes Josephus Willems ,  Bart Petrus Anna Medaer ,  Elisabeth Pasquier ,  Paul Janssen ,  Jan Heeres ,  Ruben Gerardus Leenders ,  Jerome Guillemont

发明人： Didier Philippe Schils ,  Joannes Josephus Willems ,  Bart Petrus Anna Medaer ,  Elisabeth Pasquier ,  Paul Janssen ,  Jan Heeres ,  Ruben Gerardus Leenders ,  Jerome Guillemont

IPC分类号： C07D239/48

CPC分类号： C07D239/48 ,  C07C253/20 ,  C07C253/30 ,  C07C255/42

摘要： Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: a) reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate of formula (III) in the presence of a suitable solvent; b) reacting an intermediate of formula (IV) with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent; c) dehydrating the corresponding amide of the compound of formula (I).

摘要翻译： 用于制备式（I）的4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基苯基] - 氨基] -2-嘧啶基]氨基]苄腈的方法，N-氧化物， 提供药学上可接受的酸加成盐，季胺或其立体化学异构形式，所述方法包括：a）使4-（2-氰基乙烯基）-2,6-二甲基苯胺与式（III）的中间体在 合适的溶剂; b）在合适的钯催化剂，合适的碱和合适的溶剂的存在下使式（Ⅳ）的中间体与丙烯腈反应; c）使相应的式（I）化合物的酰胺脱水。

公开(公告)号：US08101752B2

公开(公告)日：2012-01-24

申请号：US11913200

申请日：2006-05-24

申请人： Didier Philippe Robert Schils ,  Alfred Elisabeth Stappers

发明人： Didier Philippe Robert Schils ,  Alfred Elisabeth Stappers

IPC分类号： C07D239/47

CPC分类号： C07D239/47

摘要： This invention relates to a process for preparing 4-[(1,6-dihydro-6-oxo-2-pyrimidinyl)-amino]benzonitrile (I) starting from a 4-oxo-1,6-dihydro-pyrimidinylcarboxylic acid ester (II) or starting from a guanidine derivative which is reacted with an alkoxy-methylene malonic acid ester to an ester (II) which is converted to (I), which reaction sequence may be a one-pot procedure.

摘要翻译： 本发明涉及从4-氧代-1,6-二氢 - 嘧啶基羧酸酯制备4 - [（1,6-二氢-6-氧代-2-嘧啶基） - 氨基]苄腈（I）的方法 II）或从与烷氧基 - 亚甲基丙二酸酯反应的胍衍生物转化为（I）的酯（II），该反应顺序可以是一锅法。

公开(公告)号：US07563922B2

公开(公告)日：2009-07-21

申请号：US11738688

申请日：2007-04-23

申请人： Didier Philippe Robert Schils ,  Joannes Josephus Maria Willems ,  Bart Petrus Anna Maria Jozef Medaer ,  Elisabeth Therese Jeanne Pasquier ,  Paul Adriaan Jan Janssen ,  Jan Heeres ,  Ruben Gerardus George Leenders ,  Jérôme Emile Georges Guillemont

发明人： Didier Philippe Robert Schils ,  Joannes Josephus Maria Willems ,  Bart Petrus Anna Maria Jozef Medaer ,  Elisabeth Therese Jeanne Pasquier ,  Paul Adriaan Jan Janssen ,  Jan Heeres ,  Ruben Gerardus George Leenders ,  Jérôme Emile Georges Guillemont

IPC分类号： C07C255/42 ,  C07C253/30 ,  C07C253/20 ,  C07D239/48 ,  A61K31/505 ,  A61P31/18

CPC分类号： C07D239/48 ,  C07C253/20 ,  C07C253/30 ,  C07C255/42

摘要： Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: a) reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate of formula (III)  in the presence of a suitable solvent; b) reacting an intermediate of formula (IV)  with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent; c) dehydrating the corresponding amide of the compound of formula (I).

摘要翻译： 用于制备式（I）的4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基苯基] - 氨基] -2-嘧啶基]氨基]苄腈的方法，N-氧化物， 提供药学上可接受的酸加成盐，季胺或其立体化学异构形式，所述方法包括：a）使4-（2-氰基乙烯基）-2,6-二甲基苯胺与式（III）的中间体在 合适的溶剂; b）在合适的钯催化剂，合适的碱和合适的溶剂的存在下使式（Ⅳ）的中间体与丙烯腈反应; c）使相应的式（I）化合物的酰胺脱水。

公开(公告)号：US07399856B2

公开(公告)日：2008-07-15

申请号：US10523753

申请日：2003-08-07

申请人： Didier Philippe Robert Schils ,  Joannes Josephus Maria Willems ,  Bart Petrus Anna Maria Jozef Medaer ,  Elisabeth Therese Jeanne Pasquier ,  Paul Adriaan Jan Janssen ,  Jan Heeres ,  Ruben Gerardus George Leenders ,  Jérôme Emile Georges Guillemont

发明人： Didier Philippe Robert Schils ,  Joannes Josephus Maria Willems ,  Bart Petrus Anna Maria Jozef Medaer ,  Elisabeth Therese Jeanne Pasquier ,  Paul Adriaan Jan Janssen ,  Jan Heeres ,  Ruben Gerardus George Leenders ,  Jérôme Emile Georges Guillemont

IPC分类号： C07D239/48 ,  C07C255/42 ,  C07C253/30 ,  C07C253/20 ,  A61K31/505 ,  A61P31/18

CPC分类号： C07D239/48 ,  C07C253/20 ,  C07C253/30 ,  C07C255/42

摘要： Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: a) reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate of formula (III)  in the presence of a suitable solvent; b) reacting an intermediate of formula (IV)  with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent; c) dehydrating the corresponding amide of the compound of formula (I).

摘要翻译： 用于制备式（I）的4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基苯基] - 氨基] -2-嘧啶基]氨基]苄腈的方法，N-氧化物， 提供药学上可接受的酸加成盐，季胺或其立体化学异构形式，所述方法包括：a）使4-（2-氰基乙烯基）-2,6-二甲基苯胺与式（III）的中间体在 合适的溶剂; b）在合适的钯催化剂，合适的碱和合适的溶剂的存在下使式（Ⅳ）的中间体与丙烯腈反应; c）使相应的式（I）化合物的酰胺脱水。

公开(公告)号：US08618291B2

公开(公告)日：2013-12-31

申请号：US13325621

申请日：2011-12-14

申请人： Didier Philippe Robert Schils ,  Alfred Elisabeth Stappers

发明人： Didier Philippe Robert Schils ,  Alfred Elisabeth Stappers

IPC分类号： C07D239/47

CPC分类号： C07D239/47

摘要： This invention relates to a process for preparing 4-[(1,6-dihydro-6-oxo-2-pyrimidinyl)-amino]benzonitrile (I) starting from a 4-oxo-1,6-dihydro-pyrimidinylcarboxylic acid ester (II) or starting from a guanidine derivative which is reacted with an alkoxy-methylene malonic acid ester to an ester (II) which is converted to (I), which reaction sequence may be a one-pot procedure.

摘要翻译： 本发明涉及从4-氧代-1,6-二氢 - 嘧啶基羧酸酯制备4 - [（1,6-二氢-6-氧代-2-嘧啶基） - 氨基]苄腈（I）的方法 II）或从与烷氧基 - 亚甲基丙二酸酯反应的胍衍生物转化成（I）的酯（II），该反应顺序可以是一锅法。

公开(公告)号：US07705148B2

公开(公告)日：2010-04-27

申请号：US12031011

申请日：2008-02-14

申请人： Didier Philippe Robert Schils ,  Joannes Josephus Maria Willems ,  Bart Petrus Anna Maria Jozef Medaer ,  Elisabeth Therese Jeanne Pasquier ,  Paul Adriaan Jan Janssen ,  Jan Heeres ,  Ruben Gerardus George Leenders ,  Jérôme Emile Georges Guillemont

发明人： Didier Philippe Robert Schils ,  Joannes Josephus Maria Willems ,  Bart Petrus Anna Maria Jozef Medaer ,  Elisabeth Therese Jeanne Pasquier ,  Paul Adriaan Jan Janssen ,  Jan Heeres ,  Ruben Gerardus George Leenders ,  Jérôme Emile Georges Guillemont

IPC分类号： C07D239/48 ,  C07C255/42 ,  C07C253/30 ,  C07C253/20 ,  A61K31/505 ,  A61P31/18

CPC分类号： C07D239/48 ,  C07C253/20 ,  C07C253/30 ,  C07C255/42

摘要： Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: a) reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate of formula (III) in the presence of a suitable solvent; b) reacting an intermediate of formula (IV) with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent; c) dehydrating the corresponding amide of the compound of formula (I).

摘要翻译： 用于制备式（I）的4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基苯基] - 氨基] -2-嘧啶基]氨基]苄腈的方法，N-氧化物， 提供药学上可接受的酸加成盐，季胺或其立体化学异构形式，所述方法包括：a）使4-（2-氰基乙烯基）-2,6-二甲基苯胺与式（III）的中间体在 合适的溶剂; b）在合适的钯催化剂，合适的碱和合适的溶剂的存在下使式（Ⅳ）的中间体与丙烯腈反应; c）使相应的式（I）化合物的酰胺脱水。

公开(公告)号：US20080171878A1

公开(公告)日：2008-07-17

申请号：US11913200

申请日：2006-05-24

申请人： Didier Philippe Robert Schils ,  Alfred Elisabeth Stappers

发明人： Didier Philippe Robert Schils ,  Alfred Elisabeth Stappers

IPC分类号： C07D239/47

CPC分类号： C07D239/47

摘要： This invention relates to a process for preparing 4-[(1,6-dihydro-6-oxo-2-pyrimidinyl)-amino]benzonitrile (I) starting from a 4-oxo-1,6-dihydro-pyrimidinylcarboxylic acid ester (II) or starting from a guanidine derivative which is reacted with an alkoxy-methylene malonic acid ester to an ester (II) which is converted to (I), which reaction sequence may be a one-pot procedure.

摘要翻译： 本发明涉及从4-氧代-1,6-二氢 - 嘧啶基羧酸酯制备4 - [（1,6-二氢-6-氧代-2-嘧啶基） - 氨基]苄腈（I）的方法 II）或从与烷氧基 - 亚甲基丙二酸酯反应的胍衍生物转化为（I）的酯（II），该反应顺序可以是一锅法。

公开(公告)号：US20080167464A1

公开(公告)日：2008-07-10

申请号：US12031011

申请日：2008-02-14

申请人： Didier Philippe Robert Schils ,  Joannes Josephus Maria Willems ,  Bart Petrus Anna Maria Jozef Medaer ,  Elisabeth Therese Jeanne Pasquier ,  Paul Adriaan Jan Janssen ,  Jan Heeres ,  Ruben Gerardus George Leenders ,  Jerome Emile Georges Guillemont

发明人： Didier Philippe Robert Schils ,  Joannes Josephus Maria Willems ,  Bart Petrus Anna Maria Jozef Medaer ,  Elisabeth Therese Jeanne Pasquier ,  Paul Adriaan Jan Janssen ,  Jan Heeres ,  Ruben Gerardus George Leenders ,  Jerome Emile Georges Guillemont

IPC分类号： C07D239/48

CPC分类号： C07D239/48 ,  C07C253/20 ,  C07C253/30 ,  C07C255/42

摘要： Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: a) reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate of formula (III) in the presence of a suitable solvent; b) reacting an intermediate of formula (IV) with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent; c) dehydrating the corresponding amide of the compound of formula (I).

摘要翻译： 用于制备式（I）的4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基苯基] - 氨基] -2-嘧啶基]氨基]苄腈的方法，N-氧化物， 提供药学上可接受的酸加成盐，季胺或其立体化学异构形式，所述方法包括：a）使4-（2-氰基乙烯基）-2,6-二甲基苯胺与式（III）的中间体在 合适的溶剂; b）在合适的钯催化剂，合适的碱和合适的溶剂的存在下使式（Ⅳ）的中间体与丙烯腈反应; c）使相应的式（I）化合物的酰胺脱水。

公开(公告)号：US06231405B1

公开(公告)日：2001-05-15

申请号：US09273710

申请日：1999-03-22

申请人： Robert Diconne ,  Bernard Lepretre ,  Didier Philippe

发明人： Robert Diconne ,  Bernard Lepretre ,  Didier Philippe

IPC分类号： H01R922

CPC分类号： H01R4/62 ,  H01H2001/5861 ,  H01R4/26 ,  H01R4/36 ,  H01R4/489

摘要： The present invention relates to a connection accessory and to a terminal equipped with such an accessory. This accessory is designed to perform connection of an electrical conductor such as an aluminum cable to a contact strip of an electrical apparatus such as a circuit breaker. This accessory is characterized in that it comprises a pad made of a conducting material and presenting an appreciably U-shaped transverse cross section, said pad being able to be fixed in removable manner onto the contact strip and to receive a conductor designed to be clamped against the pad by a clamping means in order to establish the electrical contact between the contact strip and the cable.

摘要翻译： 本发明涉及连接附件和配备有这种附件的终端。该附件被设计成执行诸如铝电缆的电导体与例如断路器的电气设备的接触条的连接。 该附件的特征在于它包括由导电材料制成并且呈现明显的U形横截面的垫，所述垫能够以可移除的方式固定在接触条上并接收被设计成抵抗的导体 该垫通过夹紧装置来建立接触片与电缆之间的电接触。

公开(公告)号：US20120083606A1

公开(公告)日：2012-04-05

申请号：US13325621

申请日：2011-12-14

申请人： DIDIER PHILIPPE ROBERT SCHILS ,  ALFRED ELISABETH STAPPERS

发明人： DIDIER PHILIPPE ROBERT SCHILS ,  ALFRED ELISABETH STAPPERS

IPC分类号： C07D239/47

CPC分类号： C07D239/47

摘要： This invention relates to a process for preparing 4-[(1,6-dihydro-6-oxo-2-pyrimidinyl)-amino]benzonitrile (I) starting from a 4-oxo-1,6-dihydro-pyrimidinylcarboxylic acid ester (II) or starting from a guanidine derivative which is reacted with an alkoxy-methylene malonic acid ester to an ester (II) which is converted to (I), which reaction sequence may be a one-pot procedure.

摘要翻译： 本发明涉及从4-氧代-1,6-二氢 - 嘧啶基羧酸酯制备4 - [（1,6-二氢-6-氧代-2-嘧啶基） - 氨基]苄腈（I）的方法 II）或从与烷氧基 - 亚甲基丙二酸酯反应的胍衍生物转化为（I）的酯（II），该反应顺序可以是一锅法。