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139 条记录 (耗时 0.035 秒)

    Ligand libraries for screening GPCRs
    3.
    发明授权
    Ligand libraries for screening GPCRs 失效
    用于筛选GPCRs的配体文库

    公开(公告)号：US08618283B2

    公开(公告)日：2013-12-31

    申请号：US13289542

    申请日：2011-11-04

    申请人： David J Grainger ,  David John Fox

    发明人： David J Grainger ,  David John Fox

    IPC分类号： C40B30/00 ,  A61K38/00

    CPC分类号： C07D243/08 ,  C07D281/06

    摘要： The invention provides compounds of general formulae (I)-(IV) or pharmaceutically acceptable salts thereof: The invention also provides methods of preparing the compounds, pharmaceutical compositions comprising the compounds and use of the compounds for the preparation of medicaments intended to modulate the activity of one or more members of the G-protein coupled receptor (GPCR) class. Compounds of the invention may be used to create a compound library for use in screening for agents which modulate signalling through GPCRs.

    摘要翻译： 本发明提供通式（I） - （IV）的化合物或其药学上可接受的盐：本发明还提供了制备化合物的方法，包含该化合物的药物组合物和用于制备用于调节活性的药物 的一种或多种G蛋白偶联受体（GPCR）类成员。 本发明的化合物可用于产生用于筛选通过GPCRs调节信号传导的药剂的化合物文库。

    ANTI-INFLAMMATORY AGENTS
    4.
    发明申请
    ANTI-INFLAMMATORY AGENTS 审中-公开
    抗炎药物

    公开(公告)号：US20130172318A1

    公开(公告)日：2013-07-04

    申请号：US13702898

    申请日：2011-06-08

    申请人： David John Grainger ,  David John Fox

    发明人： David John Grainger ,  David John Fox

    IPC分类号： C07D223/12 ,  C07D211/76

    CPC分类号： C07D223/12 ,  C07D211/74 ,  C07D211/76 ,  C07D401/12

    摘要： Disclosed herein are methods of preventing or treating inflammatory diseases using 3-aminolactam compounds, each with aromatic “tail groups”. Compounds as defined by formulae (I) and (I′), and the medical uses of the compounds, are described herein.

    摘要翻译： 本文公开了使用具有芳族“尾组”的3-氨基内酰胺化合物预防或治疗炎性疾病的方法。 本文描述了式（I）和（I'）所定义的化合物以及化合物的医学用途。

    α-aminocyclolactam ligands for G-protein coupled receptors, and methods of using same
    5.
    发明授权
    α-aminocyclolactam ligands for G-protein coupled receptors, and methods of using same 失效
    G蛋白偶联受体的α-氨基环内酰胺配体及其使用方法

    公开(公告)号：US08389279B2

    公开(公告)日：2013-03-05

    申请号：US13193274

    申请日：2011-07-28

    申请人： David J. Grainger ,  David John Fox

    发明人： David J. Grainger ,  David John Fox

    IPC分类号： A61K31/55 ,  A61K31/439 ,  A61P9/12 ,  A61P9/10 ,  A61P11/06 ,  A61P3/04 ,  A61P37/06 ,  C12N5/07

    CPC分类号： C07D225/02 ,  C07D207/273 ,  C07D211/76 ,  C07D223/12 ,  C07D487/08

    摘要： The invention relates to the generation of a library of compounds enriched in agonist and antagonists for members of the G-protein coupled class of receptors (GPCRs).The library contains compounds of general formula (I) wherein y is any integer from 1 to 8; z is any integer from 0 to 8 with the proviso that y and z cannot simultaneously be 1; X is —CO—(Y)k—(R1)n or SO2—(Y)k—(R1)n; k is 0 or 1 Y is a cycloalkyl or polycyloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or Y is a cycloalkenyl or polycycloalkenyl group; each R1 is independently selected from hydrogen or an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl, alkylamino, alkylaminoalkyl, alkylaminodialkyl, charged alkylaminotrialkyl or charged alkylcarboxylate radical of 1 to 20 carbon atoms; or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl, aminodialkyl, charged aminotrialkyl, or carboxylate radical; and n is any integer from 1 to m, where m is the maximum number of substitutions permissible on the cyclo-group Y; or alternatively R1 may be selected from a peptido radical, for example having from 1 to 4 peptidic moieties linked together by peptide bonds (for example a peptido radical of 1 to 4 amino acid residues).

    摘要翻译： 本发明涉及产生富含G-蛋白偶联受体类（GPCR）成员的激动剂和拮抗剂的化合物文库。 该文库含有通式（I）的化合物，其中y为1至8的整数; z是0至8的任何整数，条件是y和z不能同时为1; X是-CO-（Y）k-（R1）n或SO2-（Y）k-（R1）n; k是0或1，Y是环烷基或聚环烷基（例如金刚烷基，金刚烷甲基，双环辛基，环己基，环丙基）; 或Y是环烯基或多环烯基; 每个R 1独立地选自氢或具有1至20个碳原子的烷基，卤代烷基，烷氧基，卤代烷氧基，烯基，炔基，烷基氨基，烷基氨基烷基，烷基氨基二烷基，带电荷的烷基氨基三烷基或带电荷的烷基羧酸根。 或每个R 1独立地选自氟，氯，溴，碘，羟基，氧烷基，氨基，氨基烷基，氨基二烷基，带电荷的氨基三烷基或羧酸根; n为1〜m的整数，m为环基Y上允许的最大取代数; 或者R1可以选自肽基，例如具有通过肽键连接在一起的1至4个肽部分（例如1至4个氨基酸残基的肽基）。

    Antenna arrangement
    7.
    发明授权
    Antenna arrangement 有权
    天线布置

    公开(公告)号：US08106826B2

    公开(公告)日：2012-01-31

    申请号：US11996419

    申请日：2006-07-21

    申请人： Andrew John Fox

    发明人： Andrew John Fox

    IPC分类号： H01Q3/00

    CPC分类号： H01Q25/00 ,  H01Q3/2652 ,  H01Q3/40

    摘要： An antenna has multiple antenna elements, with a beam forming Butler matrix, having antenna ports and input/output ports, with each of said antenna elements being connected to a respective port of the beam forming Butler matrix. Transceiver circuitry is connected to each of the input/output ports of the beam forming matrix by means of respective distinct transmit and receive paths and a respective duplexer. Individually controllable gain control elements are located in each of the transmit and receive paths. These can be controlled in response to signal strength measurements made by the antenna.

    摘要翻译： 天线具有多个天线元件，具有波束形成Butler矩阵，具有天线端口和输入/输出端口，其中每个天线元件连接到波束形成Butler矩阵的相应端口。 收发器电路通过相应的不同的发射和接收路径和相应的双工器连接到波束形成矩阵的每个输入/输出端口。 单独控制的增益控制元件位于每个发送和接收路径中。 这些可以根据由天线进行的信号强度测量来控制。