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15 条记录 (耗时 0.033 秒)

    1-Phenacyl-3-phenyl-3-(piperidylethyl)piperidine derivatives, process for the preparation thereof and pharmaceutical compositions containing them
    6.
    发明授权
    1-Phenacyl-3-phenyl-3-(piperidylethyl)piperidine derivatives, process for the preparation thereof and pharmaceutical compositions containing them 失效
    1-苯甲酰基-3-苯基-3-（哌啶基乙基）哌啶衍生物，其制备方法和含有它们的药物组合物

    公开(公告)号：US06642233B1

    公开(公告)日：2003-11-04

    申请号：US09913106

    申请日：2001-08-09

    申请人： Jean-Philippe Ducoux ,  Xavier Emonds-Alt ,  Patrick Gueule ,  Vincenzo Proietto

    发明人： Jean-Philippe Ducoux ,  Xavier Emonds-Alt ,  Patrick Gueule ,  Vincenzo Proietto

    IPC分类号： A61K31535

    CPC分类号： C07D211/34 ,  C07D211/26

    摘要： The invention relates to the compounds of formula: as well as to the salts thereof with inorganic or organic acids, to solvates thereof and/or to hydrates thereof, which have strong affinity and high selectivity for the human NK1 receptors of substance P. The invention also relates to the process for preparing them, to the intermediate compounds of formula (VII) which are useful for the preparation, to pharmaceutical compositions containing them and to their fuse for the manufacture of medicinal products intended for treating any pathology in which substance P and the human NK1 receptors are involved.

    摘要翻译： 本发明涉及对于物质P的人NK1受体具有强亲和力和高选择性的下式的化合物及其与无机或有机酸的盐，其溶剂合物和/或其水合物。本发明涉及 还涉及制备它们的方法，可用于制备的式（VII）的中间体化合物，含有它们的药物组合物及其保险丝，用于制造用于治疗任何病理学的药物，其中物质P和 涉及人NK1受体。

    Thiophene-2-carboxamide derivatives, preparation thereof and therapeutic use thereof
    8.
    发明授权
    Thiophene-2-carboxamide derivatives, preparation thereof and therapeutic use thereof 有权
    噻吩-2-甲酰胺衍生物，其制备及其治疗用途

    公开(公告)号：US08410137B2

    公开(公告)日：2013-04-02

    申请号：US13057043

    申请日：2009-07-30

    申请人： Francis Barth ,  Jean-Philippe Ducoux ,  Patrick Gueule ,  Murielle Rinaldi-Carmona ,  Arnaud Rouquette

    发明人： Francis Barth ,  Jean-Philippe Ducoux ,  Patrick Gueule ,  Murielle Rinaldi-Carmona ,  Arnaud Rouquette

    IPC分类号： A61K31/445 ,  C07D409/06

    CPC分类号： C07D409/06 ,  C07D409/14

    摘要： The subject matter of the invention is compounds corresponding to formula (I), in which: R1 and R2, together with the nitrogen atom to which they are attached, constitute a saturated heterocyclic radical containing from 4 to 7 atoms, which is preferably substituted; one of the two substituents R3 and R6 is a group Y-A-R9; Y is an oxygen atom or an —S(O)n′—, or —OSO2 group; A is an unsubstituted (C1-C4) alkylene group; R9 is an —OR19, —CH3, —NR19R20, —CONR19R20, —NR15COR19, —S(O)nR21, or —NR13SO2R21 group; —R10 is a hydrogen atom or a (C1-C4) alkyl group. The present invention also relates to the methods of preparation and the therapeutic uses of the compounds of formula (I).

    摘要翻译： 本发明的主题是对应于式（I）的化合物，其中：R 1和R 2与它们所连接的氮原子一起构成含有4至7个原子的饱和杂环基团，其优选被取代; 两个取代基R 3和R 6中的一个是Y-A-R 9基团; Y是氧原子或-S（O）n'-或-OSO 2基团; A是未取代的（C 1 -C 4）亚烷基; R9是-OR19，-CH3，-NR19R20，-CONR19R20，-NR15COR19，-S（O）nR21或-NR13SO2R21基团; -R10是氢原子或（C1-C4）烷基。 本发明还涉及式（I）化合物的制备方法和治疗用途。

    Derivatives of 3-alkoxy-4,5-diarylthiophene-2-carboxamide, preparation thereof, and therapeutic use thereof
    10.
    发明授权
    Derivatives of 3-alkoxy-4,5-diarylthiophene-2-carboxamide, preparation thereof, and therapeutic use thereof 有权
    3-烷氧基-4,5-二芳基噻吩-2-甲酰胺的衍生物及其治疗用途

    公开(公告)号：US08486971B2

    公开(公告)日：2013-07-16

    申请号：US13258933

    申请日：2010-03-25

    申请人： Jean-Philippe Ducoux ,  Murielle Rinaldi-Carmona ,  Arnaud Rouquette

    发明人： Jean-Philippe Ducoux ,  Murielle Rinaldi-Carmona ,  Arnaud Rouquette

    IPC分类号： A61K31/445 ,  C07D409/02

    CPC分类号： C07D409/06 ,  C07D409/12

    摘要： The invention relates to compounds of the formula (I), where: R1 is: a —NR5R6 group; an unsubstituted or substituted phenyl; R2 is: a (C1-C4)alkyl; an —X—R7 group; R3 and R4 each are independently a substituted phenyl; R5 is a hydrogen atom or a (C1-C4)alkyl; R6 is an unsubstituted or substituted (C1-C4)alkyl; or R5 and R6 together with the nitrogen atom to which they are bonded constitute an unsubstituted or substituted heterocyclic compound; X is a (C1-C5)alkylene; R7 is an —OR8 group, a —NR9R10 group, an —SO2—(C1-C4)alkyl group; R8 is a hydrogen atom or a (C1-C4)alkyl; R9 is a hydrogen atom or a (C1-C4)alkyl; R10 is a hydrogen atom, a —COR11 group, an —SO2R11 group or a —CO(CH2)mOH group; R11 is an unsubstituted or substituted (C1-C4)alkyl; m is 1, 2 or 3. The invention also relates to methods for preparing same and to the therapeutic use thereof.

    摘要翻译： 本发明涉及式（I）化合物，其中：R1为：-NR5R6基团; 未取代或取代的苯基; R2是：（C1-C4）烷基; -X-R7基团; R3和R4各自独立地是取代的苯基; R5是氢原子或（C1-C4）烷基; R6是未取代或取代的（C1-C4）烷基; 或R 5和R 6与它们所键合的氮原子一起构成未取代或取代的杂环化合物; X是（C 1 -C 5）亚烷基; R 7是-OR 8基，-NR 9 R 10基，-SO 2 - （C 1 -C 4）烷基; R8是氢原子或（C1-C4）烷基; R9是氢原子或（C1-C4）烷基; R 10为氢原子，-COR 11基，-SO 2 R 11基或-CO（CH 2）mOH基; R11是未取代或取代的（C1-C4）烷基; m是1,2或3.本发明还涉及其制备方法及其治疗用途。