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    NOVEL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME, AND METHODS OF USE FOR SAME
    2.
    发明申请
    NOVEL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME, AND METHODS OF USE FOR SAME 审中-公开
    新化合物，含有它们的药物组合物及其使用方法

    公开(公告)号：WO2007014249A3

    公开(公告)日：2007-05-31

    申请号：PCT/US2006028981

    申请日：2006-07-26

    申请人： UNIV JOHNS HOPKINS ,  FASGEN INC ,  KUHAJDA FRANCIS P ,  TOWNSEND CRAIG A ,  MEDGHALCHI SUSAN M ,  MCFADDEN JILL M

    发明人： KUHAJDA FRANCIS P ,  TOWNSEND CRAIG A ,  MEDGHALCHI SUSAN M ,  MCFADDEN JILL M

    IPC分类号： C07D333/02 ,  C07D333/32 ,  C07D333/34

    CPC分类号： C07D333/38 ,  C07D409/12

    摘要： A pharmaceutical composition containing a pharmaceutical diluent and a compound of formula II: wherein: R 8 = H, C 1 -C 20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, -C(O)R 4 , where R 4 is H, C 1 -C 20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing halogen atoms, or -OH, -OR 7 or -NR 7 , where R 7 is H, C 1 -C 20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing halogen atoms; R 9 = -OR 5 , -NR 5 , -NH-NH-R 5 where R 5 is H, C 1 -C 20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, allyl, or alkylaryl, optionally containing halogen atoms; R 10 = H, C 1 -C 20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, or- CH 2 C(O)R 6 , where R 6 is OR 7 and NR 7 , where R 7 = H, C 1 -C 20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, allyl, or alkylaryl and can optionally contain halogen atoms. Also included in the invention are methods of using the pharmaceutical compositions and the chemical compounds used in the compositions.

    摘要翻译： 含有药物稀释剂和式II化合物的药物组合物：其中：R 8 = H，C 1 -C 20烷基，环烷基 ，烯基，芳基，芳基烷基或烷基芳基，-C（O）R 4，其中R 4是H，C 1 -C 3烷基， 或任选地含有卤素原子的烷基，芳基，芳基烷基或烷基芳基，或-OH，-OR 7或-NR 7， 其中R 7为H，C 1 -C 20烷基，环烷基，烯基，芳基，芳基烷基或烷基芳基，任选地含有卤素原子 ; R 9 = -OR 5，-NR 5，-NH-NH-R 5，其中R 0 任选地含有卤素原子的烷基，环烷基，链烯基，芳基，芳基烷基，烯丙基或烷基芳基; R 10 = H，C 1 -C 20烷基，环烷基，烯基，芳基，芳烷基或烷基芳基，或 - 2 C（O）R 6，其中R 6为OR 7和NR 7， 其中R 7 = H，C 1 -C 20烷基，环烷基，烯基，芳基，芳基烷基，烯丙基或烷基芳基，并且可任选地含有 卤原子。 本发明还包括使用组合物中使用的药物组合物和化合物的方法。

    FLUORESCENTLY TAGGED LIGANDS
    3.
    发明申请
    FLUORESCENTLY TAGGED LIGANDS 审中-公开
    荧光标签配置

    公开(公告)号：WO2004088312A3

    公开(公告)日：2005-03-24

    申请号：PCT/GB2004001418

    申请日：2004-03-31

    申请人： UNIV NOTTINGHAM ,  GEORGE MICHAEL ,  HILL STEPHEN JOHN ,  KELLAM BARRIE ,  MIDDLETON RICHARD JOHN

    发明人： GEORGE MICHAEL ,  HILL STEPHEN JOHN ,  KELLAM BARRIE ,  MIDDLETON RICHARD JOHN

    IPC分类号： C07D209/56 ,  C07D333/02 ,  C07D473/00 ,  C07H19/16 ,  C07H19/20 ,  G01N33/533 ,  A61K38/25 ,  C07B61/00

    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): (Lig JL)m L(JT Tag) 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, CI-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.

    摘要翻译： 包含多个标记的式（I）所示的非肽配体：（Lig JL）m L（JT Tag）m（JTL（JLLig）m）p包括其盐及其盐，其包含一个或多个相同或不同的配体部分 每个连接到一个或多个相同或不同标签部分的标签通过相同或不同的接头部分L和相同或不同的连接位点或连接官能团JT和JL标记，其中Lig包含GPCR配体，细胞内酶的抑制剂或 药物转运蛋白的底物或抑制剂; L是单键或者是选自杂原子如N，O，S，P，支链或直链饱和或不饱和的任选的连接部分，任选地是杂原子，含有C 1-6的烃基及其组合，其可以是单体的，低聚的 具有2至30的寡聚重复或具有超过30至300的聚合物重复的聚合物; 标签是任何已知或新颖的标签底物; m各自独立地选自1至3的整数; p为0至3，其特征在于连接在包含不同的Lig，JL，L JT和/或 - Tag的化合物中的相同或不同的连接位点，并且在包含相同的Lig，JL，L JT和/或 - 标签; 制备方法; 用于制备式（I）的文库化合物或式（IV）的前体的方法; 从其文库中选择式（I）化合物的方法; 与其药理学性质有关的信息相关的式（I）化合物; 式（I）的新化合物或式（IV）的前体; 用途; 用于结合或抑制的方法; 使用荧光目标; 修饰的细胞表面GPCR和表达其的细胞; 和包含式（I）化合物及其靶标的试剂盒。