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    Novel Ether Linked Compounds and Improved Treatments for Cardiac and Cardiovascular Disease
    1.
    发明申请
    Novel Ether Linked Compounds and Improved Treatments for Cardiac and Cardiovascular Disease 审中-公开

    公开(公告)号：US20140094493A1

    公开(公告)日：2014-04-03

    申请号：US13983462

    申请日：2012-02-06

    申请人： Jillian G. Baker ,  Peter M. Fischer ,  Christophe Fromont ,  Sheila M. Gardiner ,  Stephen J. Hill ,  Gopal Jadhav ,  Barrie Kellam ,  Shailesh Mistry ,  Jeanette Woolard

    发明人： Jillian G. Baker ,  Peter M. Fischer ,  Christophe Fromont ,  Sheila M. Gardiner ,  Stephen J. Hill ,  Gopal Jadhav ,  Barrie Kellam ,  Shailesh Mistry ,  Jeanette Woolard

    IPC分类号： C07D405/14 ,  C07D319/20 ,  C07D211/38

    CPC分类号： C07D405/14 ,  C07C217/34 ,  C07D209/46 ,  C07D211/38 ,  C07D215/20 ,  C07D217/24 ,  C07D241/40 ,  C07D309/06 ,  C07D319/20 ,  C07D405/12

    摘要： A compound of Formula (I), and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein R1 is independently selected from F, Cl, Br, CN, NH2, OH, CHO, COOH, oxo, C1-4alkyl, C1-4alkoxy, CONH2 (optionally mono- or di-substituted by C1-4alkyl) and SO2NH2, R2 is independently selected from C1-6allkyl substituted by R3 wherein the C1-6alkyl chain optionally comprises one or two heteroatoms select from O; R3 is selected from aryl, C3-6cycloalkyl, C3-6heterocyclyl and C3-6heteroaryl, wherein the heterocyclyl and heteroaryl rings are nitrogen containing; and wherein R3 is optonally substituted by one or more groups selected from R1; n1 is zero or an integer from 1 to 2; n2 is an integer from 1 to 2; and the sum of n1 and 2 is less than or equal to 2; R5 is selected from any group defined for R1 and R2; R6a and R6b are independently selected from H or C1-4alkyl; R7 is independently selected from F, Cl, Br, CN, NH2, OH, CHO, COOH, oxo, C1-4alkyl, C1-4alkoxy, CONH2 (optionally mono- or di-substituted by C1-4alkyl) and SO2NH2, Q1, Q2 and Q3 are independently selected from H or any group defined for R1 and R2; or Q1 and Q2 or Q2 and Q3 together form a C5-6heteroaryl or C5-6heterocylclic ring; optionally containing one or two heteroatoms selected from N and O optionally substituted by any group selected from R5; Z is selected from linear C2-3 alkylene; X3 is O; X4 is selected from aryl, a 9-10 membered heteroaryl ring or a 9-10 membered heterocyclic ring, wherein the heteroaryl and heterocyclic rings contain one or more heteroatoms selected from N, and optionally additionally O, and wherein X4 is optionally substituted by one or two oxo moieties and is optionally substituted by one or more groups selected from R7; with the proviso that (i) when X4 is phenyl then Q1 and Q2 or Q2 and Q3—together form an optionally substituted heteroaryl or heterocylclic ring as defined above; and (ii) when Q1, Q2 and Q3 are independently selected from H or any group defined for R1 and R2 then X4 is not phenyl except when R2 is C1-5alkyl substituted by R3 wherein R3 is C3-6heterocyclyl as defined above, their preparation and novel intermediates, compositions thereof and their use in the prevention or treatment of cardiac and cardiovascular disease and methods for the treatment thereof.

    High content screening
    3.
    发明授权
    High content screening 失效
    高含量筛选

    公开(公告)号：US08349571B2

    公开(公告)日：2013-01-08

    申请号：US11576035

    申请日：2005-09-26

    申请人： Stephen John Hill ,  Barrie Kellam ,  Stephen John Briddon

    发明人： Stephen John Hill ,  Barrie Kellam ,  Stephen John Briddon

    IPC分类号： G01N33/53 ,  G01N31/00

    CPC分类号： G01N33/5026 ,  G01N33/5008 ,  G01N33/566

    摘要： A high content screening (HCS) assay for rapidly screening one or more compounds to determine functional response or pharmacological properties thereof, comprising: i) priming a cell or cell material with a sensor for a biological response; ii) contacting the compound(s) to be tested with the primed cell or cell material or contacting a cell or cell material which has been contacted with the compound(s) with the primed cell or cell material; iii) simultaneously or subsequently contacting with a fluorescent agonist or a fluorescent neutral antagonist wherein the binding of the fluorescent agonist or antagonist and its associated biological response are detected or monitored in the same cell and are distinct allowing separate readout.

    摘要翻译： 用于快速筛选一种或多种化合物以确定其功能反应或药理学性质的高含量筛选（HCS）测定法，其包括：i）用用于生物反应的传感器引发细胞或细胞材料; ii）使待测化合物与引发细胞或细胞材料接触或使与化合物接触的细胞或细胞材料与引发细胞或细胞材料接触; iii）同时或随后与荧光激动剂或荧光中性拮抗剂接触，其中在相同细胞中检测或监测荧光激动剂或拮抗剂及其相关生物反应的结合，并且是不同的，允许单独读出。

    Method for Generating a Recombinant Clonal Cell Line and Novel Reagents for Use in the Method
    4.
    发明申请
    Method for Generating a Recombinant Clonal Cell Line and Novel Reagents for Use in the Method 审中-公开
    用于生成重组克隆细胞系的方法和用于该方法的新型试剂

    公开(公告)号：US20110300116A1

    公开(公告)日：2011-12-08

    申请号：US13133366

    申请日：2008-09-29

    申请人： Stephen John Hill ,  Barrie Kellam ,  Richard John Middleton

    发明人： Stephen John Hill ,  Barrie Kellam ,  Richard John Middleton

    IPC分类号： A61K35/12 ,  C07D487/14 ,  A61K35/00 ,  C07F5/02 ,  A61P43/00 ,  G01N21/64 ,  C07D223/16

    CPC分类号： C12N15/1075 ,  C07F5/022

    摘要： A method for generating a recombinant clonal cell line expressing a target cell surface receptor at a specific level of expression from a cell population comprising cells transfected with a plasmid encoding the cDNA sequence of the target receptor and expressing the target cell surface receptor, the method comprising (c) incubating the cell population with a receptor specific fluorescent ligand (d) selecting single cells from step (c) expressing the target cell surface receptor by monitoring the specific binding of the fluorescent ligand using flow cytometry; and novel fluorescent ligands.

    摘要翻译： 一种生成表达靶细胞表面受体的重组克隆细胞系的方法，所述重组克隆细胞系来自包含用编码靶受体的cDNA序列的质粒转染并表达靶细胞表面受体的细胞的细胞群，所述方法包括 （c）用受体特异性荧光配体孵育细胞群体（d）通过使用流式细胞术监测荧光配体的特异性结合来选择表达靶细胞表面受体的步骤（c）中的单个细胞; 和新型荧光配体。

    Fluorescently tagged ligands
    5.
    发明申请
    Fluorescently tagged ligands 审中-公开

    公开(公告)号：US20060211045A1

    公开(公告)日：2006-09-21

    申请号：US10551475

    申请日：2004-03-31

    申请人： Michael George ,  Stephen Hill ,  Barrie Kellam ,  Richard Middleton

    发明人： Michael George ,  Stephen Hill ,  Barrie Kellam ,  Richard Middleton

    IPC分类号： C40B40/04 ,  C40B40/10

    CPC分类号： C07D209/56 ,  C07D333/02 ,  C07D473/00 ,  C07H19/16 ,  C07H19/20 ,  C40B20/04 ,  C40B30/04 ,  C40B40/04 ,  C40B50/08 ,  C40B70/00 ,  G01N33/533

    摘要： Library comprising a plurality of tagged non-peptide ligands of formula I (LigJL)mL(JTTag)m(JTL(JLLig)m)p including and salts thereof comprising one or a plurality of same or different ligand moieties Lig each linked to a one or a plurality of same or different tag moieties Tag via same or different linker moieties L and same or different linking site or linking functionality JT and JL wherein Lig comprises a GPCR ligand, an inhibitor of an intracellular enzyme or a substrate or inhibitor of a drug transporter; L is a single bond or is any linking moiety selected from a heteroatom such as N, O, S, P, branched or straight chain saturated or unsaturated, optionally heteroatom containing, C1-600 hydrocarbyl and combinations thereof, which may be monomeric, oligomeric having oligomeric repeat of 2 to 30 or polymeric having polymeric repeat in excess of 30 up to 300; Tag is any known or novel tagging substrate; m are each independently selected from a whole number integer from 1 to 3; p is 0 to 3 characterised in that linking is at same or different linking sites in compounds comprising different Lig, JL, L JT and/or -Tag and is at different linking sites in compounds comprising same Lig, JL, L JT and/or -Tag; process for the preparation thereof; process for the preparation of a library compound of formula I or a precursor of formula IV; method for selecting a compound of formula I from a library thereof; compound of formula I associated with information relating to its pharmacological properties; a novel compound of formula I or precursor of formula IV; uses thereof; methods for binding or inhibition therewith; use of a fluorescent target therewith; a modified cell surface GPCR and cells expressing the same; and a kit comprising a compound of formula I and a target therefor.

    HIGH CONTENT SCREENING
    6.
    发明申请
    HIGH CONTENT SCREENING 失效
    高内容筛选

    公开(公告)号：US20090093001A1

    公开(公告)日：2009-04-09

    申请号：US11576035

    申请日：2005-09-26

    申请人： Stephen John Hill ,  Barrie Kellam ,  Stephen John Briddon

    发明人： Stephen John Hill ,  Barrie Kellam ,  Stephen John Briddon

    IPC分类号： G01N33/533 ,  C07H19/167

    CPC分类号： G01N33/5026 ,  G01N33/5008 ,  G01N33/566

    摘要： A high content screening (HCS) assay for rapidly screening one or more compounds to determine functional response or pharmacological properties thereof, comprising: i) priming a cell or cell material with a sensor for a biological response; ii) contacting the compound(s) to be tested with the primed cell or cell material or contacting a cell or cell material which has been contacted with the compound(s) with the primed cell or cell material; iii) simultaneously or subsequently contacting with a fluorescent agonist or a fluorescent neutral antagonist wherein the binding of the fluorescent agonist or antagonist and its associated biological response are detected or monitored in the same cell and are distinct allowing separate readout.

    摘要翻译： 用于快速筛选一种或多种化合物以确定其功能反应或药理学性质的高含量筛选（HCS）测定法，其包括：i）用用于生物反应的传感器引发细胞或细胞材料; ii）使待测化合物与引发细胞或细胞材料接触或使与化合物接触的细胞或细胞材料与引发细胞或细胞材料接触; iii）同时或随后与荧光激动剂或荧光中性拮抗剂接触，其中在相同细胞中检测或监测荧光激动剂或拮抗剂及其相关生物反应的结合，并且是不同的，允许单独读出。