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    Pyrazolopyrimidine compounds and their use in medicine
    1.
    发明申请
    Pyrazolopyrimidine compounds and their use in medicine 审中-公开

    公开(公告)号：US20070179161A1

    公开(公告)日：2007-08-02

    申请号：US10551177

    申请日：2004-03-18

    申请人： Martin Parratt ,  Justin Bower ,  Douglas Williamson ,  Andrew Cansfield

    发明人： Martin Parratt ,  Justin Bower ,  Douglas Williamson ,  Andrew Cansfield

    IPC分类号： A61K31/519 ,  C07D487/02

    CPC分类号： C07D487/04 ,  A61K31/519

    摘要： Compounds of formula (I) or salts, N-oxides, hydrates or solvates thereof are inhibitors of kinase activity, and useful for the treatment of, for example, cancer, psoriasis or restenosis: wherein ring A is an optionally substituted carbocyclic or heterocyclic radical. Alk represents an optionally substituted divalent C1-C6 alkylene radical. n is 0 or 1. Q represents a radical of formula -(Alk1)p (X)r-(Alk2)s-Z wherein in any compatible combination Z is hydrogen or an optionally substituted carbocyclic or heterocyclic ring; Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene radicals which may contain a —O—, —S— or —NRA— link, wherein RA is hydrogen or C1-C6 alkyl; X represents —O—, —S—, —(C═O)—, —(C═S)—, —SO2—, —SO—, —C(═O)O—, —OC(═O)—, —C(═O)NRA—, —NR AC(═O)—, —C(═S)NRA, —NRAC(═S)—, —SO2NRA—, —NRASO2—, —OC(═O)NRA—, —NRAC(═O)O—, or —NRA— wherein RA is hydrogen or C1-C6 alkyl. p, r and s are independently 0 or 1. R1 represents a radical -(Alk3)a-(Y)b-(Alk4)d-B wherein a, b and d are independently 0 or 1; Alk3 and Alk4 are optionally substituted divalent C,-C3 alkylene radicals; Y represents a monocyclic divalent carbocyclic or heterocyclic radical having from 5 to 8 ring atoms, —O—, —S—, or —NRA— wherein RA is hydrogen or C1-C6 alkyl; B represents hydrogen or halo, or an optionally substituted monocyclic carbocyclic or heterocyclic ring having from 5 to 8 ring atoms, or in the case where Y is —NRA— and b is 1, then RA and the radical -(Alk4)d-B taken together with the nitrogen to which they are attached may form an optionally substituted heterocyclic ring. R represents hydrogen, halo, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, phenyl, benzyl, cycloalkyl with 3 to 6 ring atoms, or a monocyclic heterocyclic group having 5 or 6 ring atoms.

    Triazolo ' 1, 5-A ! Pyrimidines and Their Use in Medicine
    2.
    发明申请
    Triazolo ' 1, 5-A ! Pyrimidines and Their Use in Medicine 审中-公开
    Triazolo'1，5-A！ 嘧啶及其在医学中的应用

    公开(公告)号：US20070275961A1

    公开(公告)日：2007-11-29

    申请号：US10558694

    申请日：2004-06-02

    申请人： Justin Bower ,  Andrew Cansfield ,  Allan Jordan ,  Martin Parratt ,  Lee Walmsley ,  Douglas Williamson

    发明人： Justin Bower ,  Andrew Cansfield ,  Allan Jordan ,  Martin Parratt ,  Lee Walmsley ,  Douglas Williamson

    IPC分类号： A61K31/519 ,  A61K31/496 ,  A61K31/5377 ,  A61P17/06 ,  A61P35/00 ,  A61P9/00 ,  C07D413/14 ,  C07D487/04

    CPC分类号： A61K31/519 ,  C07D487/04

    摘要： Compounds of formula (IA) or (AB) are kinase inhibitors, especially of CDK2, and/or PDK1 and/or CHK1: wherein Ring A is an optionally substituted aryl, heteroaryl, carbocyclic or heterocyclic radical, Alk represents an optionally substituted clivaient C1-C6 alkylene radical; n is 0 or 1; Q represents a radical of formula -(Alk1)p-(X),(Alk2)s-Z wherein in any compatible combination Z is hydrogen or an optionally substituted carbocyclic or heterocyclic ring, p, r and s are 0 or 1, and Alk1, Alk2, X, are as described in the specification, and R1 represents a radical 3 4 3 (CYC)k-(Alk3)a-(Y)b-(Alk4)d-B wherein k, a, b and d are 0 or 1, and Cyc, Alk3, Alk4 and B are as described in the specification.

    摘要翻译： 式（IA）或（AB）的化合物是激酶抑制剂，特别是CDK2和/或PDK1和/或CHK1的激酶抑制剂：其中环A是任选取代的芳基，杂芳基，碳环或杂环基，Alk表示任选取代的亲水性C C 1 -C 6亚烷基; n为0或1; Q表示式 - （Alk-1）对 - （X），（Alk 2 O 3）-SZ的基团，其中以任何相容的组合 Z是氢或任选取代的碳环或杂环，p，r和s是0或1，并且Alk 1，Alk 2 X，如 规格，R 1表示基团3 4 3（CYC）3 - （烷基） （Y）b - 其中k，a，b和d分别为0或1，并且Cyc，Alk 3号，3号，4号和B号如说明书中所述。

    METHODS FOR THE IDENTIFICATION OF PI3K INTERACTING MOLECULES AND FOR THE PURIFICATION OF PI3K
    3.
    发明申请
    METHODS FOR THE IDENTIFICATION OF PI3K INTERACTING MOLECULES AND FOR THE PURIFICATION OF PI3K 失效

    公开(公告)号：US20100055711A1

    公开(公告)日：2010-03-04

    申请号：US12375979

    申请日：2007-08-03

    申请人： Giovanna Bergamini Moore ,  Andrew Cansfield ,  Nigel Ramsden ,  Gitte Neubauer

    发明人： Giovanna Bergamini Moore ,  Andrew Cansfield ,  Nigel Ramsden ,  Gitte Neubauer

    IPC分类号： G01N33/53

    CPC分类号： C12Q1/485 ,  G01N2500/02

    摘要： The present invention relates to a method for the identification of a PI3K interacting compound, comprising the steps of a) providing a protein preparation containing PI3K, b) contacting the protein preparation with phenylthiazole ligand 1 immobilized on a solid support under conditions allowing the formation of a phenylthiazole ligand 1-PI3K complex, c) incubating the phenylthiazole ligand 1-PI3K complex with a given compound, and d) determining whether the compound is able to separate PI3K from the immobilized phenylthiazole ligand 1. Furthermore, the present invention relates to a method for the identification of a PI3K interacting compound, comprising the steps of a) providing a protein preparation containing PI3K, b) contacting the protein preparation with phenylthiazole ligand 1 immobilized on a solid support and with a given compound under conditions allowing the formation of a phenylthiazole ligand 1-PI3K complex, and c) detecting the phenylthiazole ligand 1-PI3K complex formed in step b). Furthermore, the present invention relates to a method for the identification of a PI3K interacting compound, comprising the steps of a) providing two aliquots of a protein preparation containing PI3K, b) contacting one aliquot with the phenylthiazole ligand 1 immobilized on a solid support under conditions allowing the formation of a phenylthiazole ligand 1-PI3K complex, c) contacting the other aliquot with the phenylthiazole ligand 1 immobilized on a solid support and with a given compound under conditions allowing the formation of a phenylthiazole ligand 1-PI3K complex, and d) determining the amount of the phenylthiazole ligand 1-PI3K complex formed in steps b) and c). Furthermore, the present invention relates to a method for the identification of a PI3K interacting compound, comprising the steps of a) providing two aliquots comprising each at least one cell containing PI3K, b) incubating one aliquot with a given compound, c) harvesting the cells of each aliquot, d) lysing the cells in order to obtain protein preparations, e) contacting the protein preparations with the phenylthiazole ligand 1 immobilized on a solid support under conditions allowing the formation of a phenylthiazole ligand 1-PI3K complex, and f) determining the amount of the phenylthiazole ligand 1-PI3K complex formed in each aliquot in step e).