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13 条记录 (耗时 0.084 秒)

    Method for producing and screening mass-coded combinatorial libraries for drug discovery and target validation
    8.
    发明申请
    Method for producing and screening mass-coded combinatorial libraries for drug discovery and target validation 审中-公开
    用于生产和筛选用于药物发现和目标验证的大规模组合文库的方法

    公开(公告)号：US20060063169A1

    公开(公告)日：2006-03-23

    申请号：US11061499

    申请日：2005-02-18

    申请人： Huw Nash ,  Seth Birnbaum ,  Edward Wintner ,  Krishna Kalghatgi ,  Gerald Shipps ,  Satish Jindal

    发明人： Huw Nash ,  Seth Birnbaum ,  Edward Wintner ,  Krishna Kalghatgi ,  Gerald Shipps ,  Satish Jindal

    IPC分类号： C40B40/08 ,  C40B40/10

    CPC分类号： G01N33/6845 ,  B01J19/0046 ,  B01J2219/00581 ,  B01J2219/00585 ,  B01J2219/00596 ,  B01J2219/00599 ,  B01J2219/00695 ,  B01J2219/00722 ,  B01J2219/00725 ,  C40B20/04 ,  C40B30/10 ,  C40B40/06 ,  C40B70/00 ,  G01N33/6848 ,  G01N2458/15

    摘要： The present invention provides a method for producing a mass-coded combinatorial library comprising a set of compounds having the general formula X(Y)n, where X is a scaffold, each Y is, independently, a peripheral moiety, and n is an integer greater than 1. The method comprises selecting a peripheral moiety precursor subset from a peripheral moiety precursor set. The subset includes a sufficient number of peripheral moiety precursors that at least about 50 distinct combinations of n peripheral moieties derived from the peripheral moiety precursors in the subset exist. The subset of peripheral moiety precursors is selected so that at least about 90% of all possible combinations of n peripheral moieties derived from the subset have a molecular mass sum which is distinct from the molecular mass sums of all of the other combinations of n peripheral moieties. The method further comprises contacting the peripheral moiety precursor subset with a scaffold precursor which has n reactive groups. Methods of use of the mass-coded combinatorial library produced by this method for identifying a ligand to a particular biomolecule are also disclosed.

    摘要翻译： 本发明提供一种生产大量编码的组合文库的方法，该组合文库包含一组具有通式X（Y）N n的化合物，其中X是支架，每个Y独立地是外周 部分，并且n是大于1的整数。该方法包括从外周部分前体组选择外周部分前体子集。 该子集包括足够数量的外周部分前体，其存在衍生自该子集中的外周部分前体的n个外周部分的至少约50个不同组合。 选择外周部分前体的子集，使得衍生自子集的n个外围部分的所有可能组合的至少约90％具有不同于n个外围部分的所有其它组合的分子质量和的分子质量和 。 该方法还包括使外周部分前体子集与具有n个反应性基团的支架前体接触。 还公开了通过该方法产生的用于鉴定特定生物分子的配体产生的批量编码的组合文库的方法。

    Pyrazolopyrimidines as protein kinase inhibitors
    9.
    发明申请
    Pyrazolopyrimidines as protein kinase inhibitors 有权
    吡唑并嘧啶作为蛋白激酶抑制剂

    公开(公告)号：US20060094706A1

    公开(公告)日：2006-05-04

    申请号：US11244628

    申请日：2005-10-06

    申请人： Kamil Paruch ,  Timothy Guzi ,  Michael Dwyer ,  Gerald Shipps

    发明人： Kamil Paruch ,  Timothy Guzi ,  Michael Dwyer ,  Gerald Shipps

    IPC分类号： A61K31/554 ,  A61K31/553 ,  A61K31/551 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/519 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions. The invention also relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compounds and methods for inhibiting HCV RNA-dependent RNA polymerase enzymatic activity. The invention also provides compositions and methods for the prophylaxis and treatment of HCV infection.

    摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的吡唑并[1,5-a]嘧啶化合物作为蛋白质和/或检查点激酶的抑制剂，制备此类化合物的方法，包含一种或多种这类化合物的药物组合物， 制备包括一种或多种这样的化合物的药物制剂，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与蛋白质或检查点激酶相关的一种或多种疾病的方法。 本发明还涉及丙型肝炎病毒（HCV）复制的抑制。 特别地，本发明的实施方案提供了用于抑制HCV RNA依赖性RNA聚合酶酶活性的化合物和方法。 本发明还提供了预防和治疗HCV感染的组合物和方法。