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1. 发明授权

US07563922B2 Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile 有权
标题翻译：制备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
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。

2. 发明授权

US07399856B2 Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-2pyrimidinyl]amino]benzonitrile 有权
标题翻译：制备4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基苯基]氨基] -2-2嘧啶基]氨基]苄腈的方法
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。

3. 发明申请

US20050085533A1 Novel mandelates salts of substituted tetracyclic tetrahydrofuran derivatives 失效
标题翻译：取代四环四氢呋喃衍生物的新型扁桃酸盐
公开(公告)号：US20050085533A1
公开(公告)日：2005-04-21
申请号：US10491799
申请日：2002-11-08
申请人： Bart Petrus Anna Maria Jozef Medaer , Sigrid Carl Maria Stokbroekx , Yves Ruysschaert , Joannes Josephus Maria Willems , Johan Erwin Edmond Weerts
发明人： Bart Petrus Anna Maria Jozef Medaer , Sigrid Carl Maria Stokbroekx , Yves Ruysschaert , Joannes Josephus Maria Willems , Johan Erwin Edmond Weerts
IPC分类号： A61K31/343 , A61P9/00 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/30 , C07D307/93
CPC分类号： C07D307/93
摘要： The object of the present invention is a novel mandelate salt of a substituted tetracyclic tetrahydrofuran derivative according to Formula (I) the N-oxide forms and the stereochemically isomeric forms thereof, wherein R1 and R2 each independently are hydrogen or C1-6alkyl and R3 and R4 each independently are hydrogen or halogen. In the foregoing definitions C1-6alkyl defines straight and branched saturated hydrocarbon radicals having from 1 to 6 carbon atoms such as, for example, methyl, ethyl, propyl, butyl, 1-methylpropyl, 1,1-dimethylethyl, pentyl or hexyl. The novel mandelate salt is not light-sensitive and is far more stable than the prior art salts at room temperature, enhanced temperature and at relative high humidities and in aqueous media. Also disclosed are pharmaceutical compositions comprising mandelate salts according to the invention, mandelate salts according to the invention for use as a medicine, a process for preparing the mandelate salts according to the invention and the use of the mandelate salts and pharmaceutical compositions comprising mandelate salts according to the invention for the treatment or the prevention of CNS disorders, cardiovascular disorders and gastrointestinal disorders.
摘要翻译：本发明的目的是根据式（I）的N-氧化物形式及其立体化学异构形式的取代四环四氢呋喃衍生物的新型扁桃酸盐，其中R 1和R 2， 2个独立地为氢或C 1-6烷基，R 3和R 4各自独立地为氢或卤素。在上述定义中，C 1-6烷基定义了具有1至6个碳原子的直链和支链饱和烃基，例如甲基，乙基，丙基，丁基，1-甲基丙基， 1-二甲基乙基，戊基或己基。新颖的扁桃酸盐盐不敏感，并且在室温，升高的温度和相对高的湿度和水性介质中比现有技术的盐更稳定。还公开了包含根据本发明的扁桃酸盐的药物组合物，根据本发明的用作药物的扁桃酸盐，根据本发明的扁桃酸盐的制备方法以及包含扁桃酸盐的扁桃酸盐和药物组合物的用途，所述扁桃酸盐包括扁桃酸盐涉及用于治疗或预防CNS疾病，心血管疾病和胃肠道疾病的本发明。

4. 发明授权

US07317115B2 Mandelates salts of substituted tetracyclic tetrahydrofuran derivatives 失效
标题翻译：取代四环四氢呋喃衍生物的盐
公开(公告)号：US07317115B2
公开(公告)日：2008-01-08
申请号：US10491799
申请日：2002-11-08
申请人： Bart Petrus Anna Maria Jozef Medaer , Sigrid Carl Maria Stokbroekx , Yves Georges Ruysschaert , Joannes Josephus Maria Willems , Johan Erwin Edmond Weerts
发明人： Bart Petrus Anna Maria Jozef Medaer , Sigrid Carl Maria Stokbroekx , Yves Georges Ruysschaert , Joannes Josephus Maria Willems , Johan Erwin Edmond Weerts
IPC分类号： C07D307/77
CPC分类号： C07D307/93
摘要： The object of the present invention is a novel mandelate salt of a substituted tetracyclic tetrahydrofuran derivative according to Formula (I) the N-oxide forms and the stereochemically isomeric forms thereof, wherein R1 and R2 each independently are hydrogen or C1-6alkyl and R3 and R4 each independently are hydrogen or halogen. In the foregoing definitions C1-6alkyl defines straight and branched saturated hydrocarbon radicals having from 1 to 6 carbon atoms such as, for example, methyl, ethyl, propyl, butyl, 1-methylpropyl, 1,1-dimethylethyl, pentyl or hexyl. The novel mandelate salt is not light-sensitive and is far more stable than the prior art salts at room temperature, enhanced temperature and at relative high humidities and in aqueous media. Also disclosed are pharmaceutical compositions comprising mandelate salts according to the invention, mandelate salts according to the invention for use as a medicine, a process for preparing the mandelate salts according to the invention and the use of the mandelate salts and pharmaceutical compositions comprising mandelate salts according to the invention for the treatment or the prevention of CNS disorders, cardiovascular disorders and gastrointestinal disorders.
摘要翻译：本发明的目的是根据式（I）的N-氧化物形式及其立体化学异构形式的取代四环四氢呋喃衍生物的新型扁桃酸盐，其中R 1和R 2， 2个独立地为氢或C 1-6烷基，R 3和R 4各自独立地为氢或卤素。在上述定义中，C 1-6烷基定义了具有1至6个碳原子的直链和支链饱和烃基，例如甲基，乙基，丙基，丁基，1-甲基丙基， 1-二甲基乙基，戊基或己基。新颖的扁桃酸盐盐不敏感，并且在室温，升高的温度和相对高的湿度和水性介质中比现有技术的盐更稳定。还公开了包含根据本发明的扁桃酸盐的药物组合物，根据本发明的用作药物的扁桃酸盐，根据本发明的扁桃酸盐的制备方法以及包含扁桃酸盐的扁桃酸盐和药物组合物的用途，所述扁桃酸盐包括扁桃酸盐涉及用于治疗或预防CNS疾病，心血管疾病和胃肠道疾病的本发明。

5. 发明授权

US07705148B2 Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile 有权
标题翻译：制备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
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。

6. 发明申请

US20080167464A1 PROCESSES FOR THE PREPARATION OF 4-[[4-[[4-(2-CYANOETHENYL)-2,6-DIMETHYLPHENYL]AMINO]-2-PYRIMIDINYL]AMINO]BENZONITRILE 有权
标题翻译：制备4 - [[4 - [[4-（2-氰基乙基）-2,6-二甲基苯基]氨基] -2-吡啶基]氨基]苯并噻唑的方法
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。

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