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    Pyridinoylpiperidines as 5-HT1F agonists
    1.
    发明授权
    Pyridinoylpiperidines as 5-HT1F agonists 有权
    吡啶基哌啶作为5-HT1F激动剂

    公开(公告)号：US08748459B2

    公开(公告)日：2014-06-10

    申请号：US13363895

    申请日：2012-02-01

    申请人： Michael Philip Cohen ,  Daniel Timothy Kohlman ,  Sidney Xi Liang ,  Frantz Victor ,  Yao-Chang Xu ,  Bai-Ping Ying ,  DeAnna Piatt Zacherl ,  Deyi Zhang

    发明人： Michael Philip Cohen ,  Daniel Timothy Kohlman ,  Sidney Xi Liang ,  Frantz Victor ,  Yao-Chang Xu ,  Bai-Ping Ying ,  DeAnna Piatt Zacherl ,  Deyi Zhang

    IPC分类号： A61K31/445 ,  C07D401/06

    CPC分类号： C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

    摘要： The present invention relates to compounds of formula I: or pharmaceutically acceptable acid addition salts thereof, where; R1 is C1-C6 alkyl, substituted C1-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, C3-C7 cycloalkyl-C1-C3 alkyl, substituted C3-C7 cycloalkyl-C1-C3 alkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II R3 is hydrogen or C1-C3 alkyl; R4 is hydrogen, halo, or C1-C3 alkyl; R5 is hydrogen or C1-C3 alkyl; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5-HTlF receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. The present invention also relates to a process for the synthesis of intermediates in the synthesis of compounds of Formula I.

    摘要翻译： 本发明涉及式I化合物或其药学上可接受的酸加成盐，其中： R 1是C 1 -C 6烷基，取代的C 1 -C 6烷基，C 3 -C 7环烷基，取代的C 3 -C 7环烷基，C 3 -C 7环烷基-C 1 -C 3烷基，取代的C 3 -C 7环烷基-C 1 -C 3烷基，苯基，取代的苯基， 杂环或取代的杂环; R 2是氢，C 1 -C 3烷基，C 3 -C 6环烷基-C 1 -C 3烷基或式II的基团R 3是氢或C 1 -C 3烷基; R4是氢，卤素或C1-C3烷基; R5是氢或C1-C3烷基; R6是氢或C1-C6烷基; n为1〜6的整数。 本发明的化合物可用于激活5-HT1F受体，抑制神经元蛋白质外渗，以及用于治疗或预防哺乳动物偏头痛。 本发明还涉及合成式I化合物中的中间体的方法。

    Vision measuring system having vision measuring apparatus
    2.
    发明授权
    Vision measuring system having vision measuring apparatus 有权
    具有视力测量装置视力测量系统

    公开(公告)号：US07809105B2

    公开(公告)日：2010-10-05

    申请号：US11550802

    申请日：2006-10-19

    申请人： Chih-Kuang Chang ,  Sen Zhang ,  Xi-Liang Feng

    发明人： Chih-Kuang Chang ,  Sen Zhang ,  Xi-Liang Feng

    IPC分类号： G01N23/04

    CPC分类号： G01B11/005

    摘要： A vision measuring system includes a vision measuring apparatus. The apparatus includes a first body mechanism, a carrying stage movably mounted in the first mechanism for supporting an article thereon, a second body mechanism spanning the first mechanism, a third body mechanism movably mounted on the second mechanism, and an imaging device movably mounted to the third mechanism for picking up images of the article. Adjusting structures are installed on the apparatus for ensuring the device to be movable relative to the article in three directions perpendicular to one another. The system further includes a motion controller for controlling movements of the stage, the third mechanism, and the device, an input unit, a computer system for converting operating orders from the input unit into electronic signals and sending the electronic signals to the controller, and analyzing image data from the device, and an output unit for displaying analyzing results.

    摘要翻译： 一种图像测定系统，包括视力测量装置。 该装置包括第一主体机构，可移动地安装在第一机构中用于在其上支撑物品的承载台，跨越第一机构的第二主体机构，可移动地安装在第二机构上的第三主体机构，以及可移动地安装到 第三个机制用于拾取物品的图像。 调整结构被安装在用于确保所述装置彼此垂直是相对于物品移动，在三个方向上设备。 该系统还包括用于控制舞台，第三机构和装置的移动的运动控制器，输入单元，用于将来自输入单元的操作命令转换为电子信号并将电子信号发送到控制器的计算机系统，以及 从设备，以及用于显示分析结果的输出单元，分析图像数据。

    Pyridinoylpiperidines as 5-HT1F agonists
    4.
    发明申请
    Pyridinoylpiperidines as 5-HT1F agonists 审中-公开
    吡啶基哌啶作为5-HT1F激动剂

    公开(公告)号：US20090209563A1

    公开(公告)日：2009-08-20

    申请号：US12221919

    申请日：2008-08-07

    申请人： Michael Philip Cohen ,  Daniel Timothy Kohlman ,  Sidney Xi Liang ,  Vincent Mancuso ,  Yao-Chang Xu

    发明人： Michael Philip Cohen ,  Daniel Timothy Kohlman ,  Sidney Xi Liang ,  Vincent Mancuso ,  Yao-Chang Xu

    IPC分类号： A61K31/4545 ,  C07D401/06 ,  C07D409/14 ,  C07D405/14 ,  C07D401/14 ,  C07D417/14 ,  A61K31/506 ,  A61P25/06

    CPC分类号： C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

    摘要： The present invention relates to compounds of formula I: or pharmaceutically acceptable acid addition salts thereof, where; R1 is C1-C6 alkyl, substituted C1-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, C3-C7 cycloalkyl-C1-C3 alkyl, substituted C3-C7 cycloalkyl-C1-C3 alkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II R3 is hydrogen or C1-C3 alkyl; R4 is hydrogen, halo, or C1-C3 alkyl; R5 is hydrogen or C1-C3 alkyl; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. The present invention also relates to a process for the synthesis of intermediates in the synthesis of compounds of Formula I.

    摘要翻译： 本发明涉及式I化合物或其药学上可接受的酸加成盐，其中： R 1是C 1 -C 6烷基，取代的C 1 -C 6烷基，C 3 -C 7环烷基，取代的C 3 -C 7环烷基，C 3 -C 7环烷基-C 1 -C 3烷基，取代的C 3 -C 7环烷基-C 1 -C 3烷基，苯基，取代的苯基， 杂环或取代的杂环; R 2是氢，C 1 -C 3烷基，C 3 -C 6环烷基-C 1 -C 3烷基或式II的基团R 3是氢或C 1 -C 3烷基; R4是氢，卤素或C1-C3烷基; R5是氢或C1-C3烷基; R6是氢或C1-C6烷基; n为1〜6的整数。 本发明的化合物可用于激活5-HT1F受体，抑制神经元蛋白质外渗，以及治疗或预防哺乳动物偏头痛。 本发明还涉及合成式I化合物中的中间体的方法。

    VISION MEASURING SYSTEM HAVING VISION MEASURING APPARATUS
    5.
    发明申请
    VISION MEASURING SYSTEM HAVING VISION MEASURING APPARATUS 有权
    具有视觉测量装置的视觉测量系统

    公开(公告)号：US20070262211A1

    公开(公告)日：2007-11-15

    申请号：US11550802

    申请日：2006-10-19

    申请人： CHIH-KUANG CHANG ,  SEN ZHANG ,  XI-LIANG FENG

    发明人： CHIH-KUANG CHANG ,  SEN ZHANG ,  XI-LIANG FENG

    IPC分类号： A47F5/00

    CPC分类号： G01B11/005

    摘要： A vision measuring system includes a vision measuring apparatus. The apparatus includes a first body mechanism, a carrying stage movably mounted in the first mechanism for supporting an article thereon, a second body mechanism spanning the first mechanism, a third body mechanism movably mounted on the second mechanism, and an imaging device movably mounted to the third mechanism for picking up images of the article. Adjusting structures are installed on the apparatus for ensuring the device to be movable relative to the article in three directions perpendicular to one another. The system further includes a motion controller for controlling movements of the stage, the third mechanism, and the device, an input unit, a computer system for converting operating orders from the input unit into electronic signals and sending the electronic signals to the controller, and analyzing image data from the device, and an output unit for displaying analyzing results.

    摘要翻译： 视觉测量系统包括视觉测量装置。 该装置包括第一主体机构，可移动地安装在第一机构中用于在其上支撑物品的承载台，横跨第一机构的第二主体机构，可移动地安装在第二机构上的第三主体机构，以及可移动地安装到 第三种拾取文章图像的机制。 调整结构安装在设备上，以确保设备相对于物品在彼此垂直的三个方向上是可移动的。 该系统还包括用于控制舞台，第三机构和装置的运动的运动控制器，输入单元，用于将来自输入单元的操作命令转换成电子信号并将电子信号发送到控制器的计算机系统，以及 分析来自设备的图像数据，以及用于显示分析结果的输出单元。

    Piperidine derivatives as serotonine reuptake inhibitors
    6.
    发明授权
    Piperidine derivatives as serotonine reuptake inhibitors 失效
    哌啶衍生物作为血清素再摄取抑制剂

    公开(公告)号：US06664274B1

    公开(公告)日：2003-12-16

    申请号：US10070183

    申请日：2002-07-16

    申请人： Sidney Xi Liang ,  Yao-Chang Xu

    发明人： Sidney Xi Liang ,  Yao-Chang Xu

    IPC分类号： A61K31444

    CPC分类号： C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14

    摘要： The present invention provides compounds of formula I and a method of inhibiting the reuptake of serotonin, antagonizing the 5-HT1A receptor and antagonizing the 5-HT2A receptor which comprises administering to a subject in need of such treatment an effective amount of a compound of formula I.

    摘要翻译： 本发明提供了式I化合物和抑制5-羟色胺再摄取，拮抗5-HT 1A受体和拮抗5-HT 2A受体的方法，其包括向需要这种治疗的受试者施用有效量的式I化合物 。

    Pyridinoylpiperidines as 5-HT1F agonists
    8.
    发明授权
    Pyridinoylpiperidines as 5-HT1F agonists 有权
    吡啶基哌啶作为5-HT1F激动剂

    公开(公告)号：US07423050B2

    公开(公告)日：2008-09-09

    申请号：US10509770

    申请日：2003-03-27

    申请人： Michael Philip Cohen ,  Daniel Timothy Kohlman ,  Sidney Xi Liang ,  Vincent Mancuso ,  Yao-Chang Xu ,  Bai-Ping Ying ,  DeAnna Piatt Zacherl ,  Deyi Zhang ,  Frantz Victor

    发明人： Michael Philip Cohen ,  Daniel Timothy Kohlman ,  Sidney Xi Liang ,  Vincent Mancuso ,  Yao-Chang Xu ,  Bai-Ping Ying ,  DeAnna Piatt Zacherl ,  Deyi Zhang ,  Frantz Victor

    IPC分类号： A61K31/445 ,  C07D401/06

    CPC分类号： C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

    摘要： The present invention relates to compounds of formula I: or pharmaceutically acceptable acid addition salts thereof, where; R1 is C1-C6 alkyl, substituted C1-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, C3-C7 cycloalkyl-C1-C3 alkyl, substituted C3-C7 cycloalkyl-C1-C3 alkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle;R2 is hydrogen, C1-C3 alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II R3 is hydrogen or C1-C3 alkyl;R4 is hydrogen, halo, or C1-C3 alkyl;R5 is hydrogen or C1-C3 alkyl;R6 is hydrogen or C1-C6 alkyl; andn is an integer from 1 to 6 inclusively.The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. The present invention also relates to a process for the synthesis of intermediates in the synthesis of compounds of Formula I.

    摘要翻译： 本发明涉及式I化合物或其药学上可接受的酸加成盐，其中： R 1是C 1 -C 6烷基，取代的C 1 -C 6亚烷基 烷基，C 3 -C 7环烷基，取代的C 3 -C 7环烷基，C 1 -C 3烷基， 取代的C 3 -C 3烷基，取代的C 3 -C 3烷基，C 1 -C 3烷基，C 3 -C 3 - 苯基，取代的苯基，杂环或取代的杂环; R 2是氢，C 1 -C 3烷基，C 3 -C 6烷基，C 3 -C 3烷基，C 3 -C 3烷基， 或者式II的基团R 3是氢或C 1 -C 6烷基， C 1 -C 3烷基; R 4是氢，卤素或C 1 -C 3烷基; R 5是氢或C 1 -C 3烷基; R 5是氢或C 1 -C 3烷基; R 6是氢或C 1 -C 6烷基; n为1〜6的整数。 本发明的化合物可用于激活5-HT 1F受体，抑制神经元蛋白质外渗，以及治疗或预防哺乳动物偏头痛。 本发明还涉及合成式I化合物中的中间体的方法。

    Indole-type derivatives as inhibitors of p38 kinase
    9.
    发明授权
    Indole-type derivatives as inhibitors of p38 kinase 有权
    吲哚型衍生物作为p38激酶的抑制剂

    公开(公告)号：US07238712B2

    公开(公告)日：2007-07-03

    申请号：US10156997

    申请日：2002-05-28

    申请人： Babu J. Mavunkel ,  Sarvajit Chakravarty ,  John J. Perumattam ,  Sundeep Dugar ,  Qing Lu ,  Xi Liang

    发明人： Babu J. Mavunkel ,  Sarvajit Chakravarty ,  John J. Perumattam ,  Sundeep Dugar ,  Qing Lu ,  Xi Liang

    IPC分类号： A61K31/445 ,  C07D401/06

    CPC分类号： C07D209/24 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

    摘要： The invention is directed to methods to inhibit p38-α kinase using compounds of the formula and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein represents a single or double bond; one Z2 is CA or CR8A and the other is CR1, CR12, NR6 or N wherein each R1, R6 and R8 is independently hydrogen or noninterfering substituent; A is —Wi—COXjY wherein Y is COR2 or an isostere thereof and R2 is hydrogen or a noninterfering substituent, each of W and X is a spacer of 2–6 Å, and each of i and j is independently 0 or 1; Z3 is NR7 or O; each R3 is independently a noninterfering substituent; n is 0–3; each of L1 and L2 is a linker; each R4 is independently a noninterfering substituent; m is 0–4; Z1 is CR5 or N wherein R5 is hydrogen or a noninterfering substituent; each of l and k is an integer from 0–2 wherein the sum of l and k is 0–3; Ar is an aryl group substituted with 0–5 noninterfering substituents, wherein two noninterfering substituents can form a fused ring; and the distance between the atom of Ar linked to L2 and the center of the α ring is 4.5–24 Å.

    摘要翻译： 本发明涉及使用下式的化合物及其药学上可接受的盐或其药物组合物来抑制p38-α激酶的方法，其中表示单键或双键; 一个Z 2是CA或CR 8 A，另一个是CR 1，CR 1，2， 其中每个R 1，R 6和R 8独立为氢，NR 6，N 6， 或非干扰取代基; A是其中Y是COR 2或其等同体和R 2的-Wi-i-X 氢或非干扰取代基，W和X各自为2-6的间隔基，i和j各自独立地为0或1; Z 3是NR 7或O; 每个R 3独立地是非干扰取代基; n为0-3; L 1和L 2各自为连接体; 每个R 4独立地是非干扰取代基; m为0-4; Z 1是CR 5或N，其中R 5是氢或非干扰取代基; l和k中的每一个是0-2的整数，其中l和k的和为0-3; Ar是被0-5个非直链取代基取代的芳基，其中两个非干扰取代基可以形成稠环; 并且与L 2连接的Ar原子和α环的中心之间的距离为4.5-24埃。