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    Carbamoyl esters that inhibit cholinesterase and release pharmacologically active agents
    1.
    发明授权
    Carbamoyl esters that inhibit cholinesterase and release pharmacologically active agents 失效
    抑制胆碱酯酶并释放药理学活性剂的氨基甲酰酯

    公开(公告)号：US07795307B2

    公开(公告)日：2010-09-14

    申请号：US10576861

    申请日：2004-10-19

    申请人： Jeroen C. Verheijen ,  ShouCheng Du

    发明人： Jeroen C. Verheijen ,  ShouCheng Du

    IPC分类号： A61K31/216

    CPC分类号： C07C271/42 ,  C07C271/44 ,  C07C271/48 ,  C07D213/64 ,  C07D487/04

    摘要： Carbamoyl esters inhibit cholinesterase activity and, upon hydrolysis release a pharmacologically active agent. In one embodiment, the carbamoyl ester has the following structure: Formula (I) wherein A is selected from the group consisting of an unsubstituted aryl, a substituted aryl, an unsubstituted heteroaryl and a substituted heteroaryl. The carbamoyl esters are employed in methods to treat an individual. The pharmacologically active agent obtained by hydrolysis of the carbamoyl esters can treat, for example, a nervous system condition, a cholinergic deficiency and conditions or diseases associated with a deficiency in a pharmacologically active agent, such as acetylcholine.

    摘要翻译： 氨基甲酰酯抑制胆碱酯酶活性，并且在水解时释放药理活性剂。 在一个实施方案中，氨基甲酰酯具有以下结构：式（I）其中A选自未取代的芳基，取代的芳基，未取代的杂芳基和取代的杂芳基。 氨基甲酰酯用于治疗个体的方法。 通过水解氨基甲酰酯获得的药理学活性剂可以治疗例如神经系统状况，胆碱能缺乏以及与药理活性剂如乙酰胆碱缺乏相关的病症或疾病。

    Carbamoyl esters that inhibit cholinesterase and release pharmacologically active agents
    4.
    发明授权
    Carbamoyl esters that inhibit cholinesterase and release pharmacologically active agents 失效
    抑制胆碱酯酶并释放药理学活性剂的氨基甲酰酯

    公开(公告)号：US07897639B2

    公开(公告)日：2011-03-01

    申请号：US10969796

    申请日：2004-10-19

    申请人： Jeroen C. Verheijen ,  ShouCheng Du

    发明人： Jeroen C. Verheijen ,  ShouCheng Du

    IPC分类号： A61K31/325 ,  C07C271/44

    CPC分类号： C07C271/42 ,  C07C271/44 ,  C07C271/48 ,  C07D213/64 ,  C07D487/04

    摘要： Carbamoyl esters inhibit cholinesterase activity and, upon hydrolysis release a pharmacologically active agent. In one embodiment, the carbamoyl ester has the following structure: wherein A is selected from the group consisting of an unsubstituted aryl, a substituted aryl, an unsubstituted heteroaryl and a substituted heteroaryl. The carbamoyl esters are employed in methods to treat an individual. The pharmacologically active agent obtained by hydrolysis of the carbamoyl esters can treat, for example, a nervous system condition, a cholinergic deficiency and conditions or diseases associated with a deficiency in a pharmacologically active agent, such as acetylcholine.

    摘要翻译： 氨基甲酰酯抑制胆碱酯酶活性，并且在水解时释放药理活性剂。 在一个实施方案中，氨基甲酰酯具有以下结构：其中A选自未取代的芳基，取代的芳基，未取代的杂芳基和取代的杂芳基。 氨基甲酰酯用于治疗个体的方法。 通过水解氨基甲酰酯获得的药理学活性剂可以治疗例如神经系统状况，胆碱能缺乏以及与药理活性剂如乙酰胆碱缺乏相关的病症或疾病。

    Compositions and methods of synthesis of pyridinolypiperidine 5-HT1F agonists
    8.
    发明授权
    Compositions and methods of synthesis of pyridinolypiperidine 5-HT1F agonists 有权
    吡啶基哌啶5-HT1F激动剂的组合物和合成方法

    公开(公告)号：US08697876B2

    公开(公告)日：2014-04-15

    申请号：US13637566

    申请日：2011-03-31

    申请人： Jean-Francois Carniaux ,  Jonathan Cummins

    发明人： Jean-Francois Carniaux ,  Jonathan Cummins

    IPC分类号： C07D401/06

    CPC分类号： C07D401/06

    摘要： The present invention provides a novel polymorph of the hemisuccinate salt of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide (Form A) characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure. This polymorph is useful in pharmaceutical compositions, for example, for the treatment and prevention of migraine. The invention also provides a process for the synthesis of pyridinoylpiperidine compounds of Formula I in high yield and high purity. In particular, the provides a process for the preparation of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide, its hemisuccinate salt and polymorph (Form A).

    摘要翻译： 本发明提供2,4,6-三氟-N- [6-（1-甲基 - 哌啶-4-羰基） - 吡啶-2-基] - 苯甲酰胺（形式A）的半琥珀酸盐的新颖多晶型物 通过独特的X射线衍射图和差示扫描量热法分析，以及独特的晶体结构。 该多晶型物可用于药物组合物，例如用于治疗和预防偏头痛。 本发明还提供以高产率和高纯度合成式I的吡啶基哌啶化合物的方法。 特别地，本发明提供了制备2,4,6-三氟-N- [6-（1-甲基 - 哌啶-4-羰基） - 吡啶-2-基] - 苯甲酰胺及其半琥珀酸盐和多晶型物 （表A）。

    COMPOSITIONS OF CHOLINESTERASE INHIBITORS
    9.
    发明申请
    COMPOSITIONS OF CHOLINESTERASE INHIBITORS 审中-公开
    胆碱酯酶抑制剂的组成

    公开(公告)号：US20100256229A1

    公开(公告)日：2010-10-07

    申请号：US12753567

    申请日：2010-04-02

    申请人： Shoucheng Du ,  Marc W. Andersen ,  Daniel Coughlin ,  Alexander Kolchinski

    发明人： Shoucheng Du ,  Marc W. Andersen ,  Daniel Coughlin ,  Alexander Kolchinski

    IPC分类号： A61K31/27 ,  C07C271/44 ,  A61P27/06 ,  A61P25/16 ,  A61P25/28 ,  A61P1/00 ,  A61P9/10 ,  A61P25/34

    CPC分类号： C07C271/44 ,  C07C57/15

    摘要： The present invention is directed to compositions, methods of use, and processes for the synthesis related to 3-((S)-1-(dimethylamino)ethyl)phenyl methyl-((R)-1-phenylpropan-2 yl)carbamate, and its pharmaceutically acceptable salt forms, including the hydrogen fumarate salt. The present invention also relates to a novel form polymorph of 3-((S)-1-(dimethylamino)ethyl)phenylmethyl-((R)-1-phenylpropan-2 yl)carbamate, characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well a unique crystalline structure.

    摘要翻译： 本发明涉及与3 - （（S）-1-（二甲基氨基）乙基）苯基甲基 - （（R）-1-苯基丙烷-2-基）氨基甲酸酯相关的组合物，使用方法和合成方法， 及其药学上可接受的盐形式，包括富马酸氢盐。 本发明还涉及3 - （（S）-1-（二甲基氨基）乙基）苯基甲基 - （（R）-1-苯基丙烷-2-基）氨基甲酸酯的新型多晶型物，其特征在于独特的X射线衍射图 和差示扫描量热法，以及独特的晶体结构。