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36 条记录 (耗时 0.036 秒)

    Pyrimidine-Substituted Benzimidazole Derivatives as Protein Kinase Inhibitors
    21.
    发明申请
    Pyrimidine-Substituted Benzimidazole Derivatives as Protein Kinase Inhibitors 失效
    嘧啶取代的苯并咪唑衍生物作为蛋白激酶抑制剂

    公开(公告)号：US20080255112A1

    公开(公告)日：2008-10-16

    申请号：US11915148

    申请日：2006-06-30

    申请人： Guobao Zhang ,  Pingda Ren ,  Xia Wang ,  Nathanael Gray ,  Taebo Sim

    发明人： Guobao Zhang ,  Pingda Ren ,  Xia Wang ,  Nathanael Gray ,  Taebo Sim

    IPC分类号： A61K31/5377 ,  C07D403/14 ,  C07D413/14 ,  A61K31/506

    CPC分类号： C07D413/14 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14

    摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of Alk, Abl, BRK, Blk, BMX, CSK, c-Src, c-Raf, EGFR, Fes, FGFR3, Fms, Fyn, IGF-IR, IR, IKKα, IKKβ, JAK2, JAK3, KDR, Lck, Met, p70S6k, Ros, Rsk1, SAPK2α, SAPK2β, SAPK3, SIK, Tie2, TrkB and/or WNK3 kinases.

    摘要翻译： 本发明提供了一类新颖的化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与异常或失调的激酶活性相关的疾病或病症的方法，特别是涉及Alk​​，Abl，BRK， 大肠杆菌，BMX，CSK，c-Src，c-Raf，EGFR，Fes，FGFR3，Fms，Fyn，IGF-IR，IR，IKKalpha，IKKbeta，JAK2，JAK3，KDR，Lck，Met，p70S6k，Ros，Rsk1， SAPK2alpha，SAPK2beta，SAPK3，SIK，Tie2，TrkB和/或WNK3激酶。

    Compounds and compositions as protein kinase inhibitors
    24.
    发明授权
    Compounds and compositions as protein kinase inhibitors 失效
    化合物和组合物作为蛋白激酶抑制剂

    公开(公告)号：US07868018B2

    公开(公告)日：2011-01-11

    申请号：US11997113

    申请日：2006-08-09

    申请人： Yongping Xie ,  Guobao Zhang ,  Xing Wang ,  Nathanael S. Gray ,  Yi Liu

    发明人： Yongping Xie ,  Guobao Zhang ,  Xing Wang ,  Nathanael S. Gray ,  Yi Liu

    IPC分类号： C07D471/04 ,  A61K31/4375 ,  A61P35/00 ,  A61P37/00 ,  A61P25/00 ,  A61K31/519 ,  C07D413/12 ,  A61K31/5355 ,  A61K31/4355 ,  C07D491/147

    CPC分类号： C07D471/14 ,  C07D471/04 ,  C07D491/14

    摘要： The invention provides compounds of Formula I: wherein R1-R6 are described in the Summary of the Invention; the pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, BMX, BTK, CHK2, b-RAF, c-RAF, CSK, c-SRC, Fes, FGFR3, Flt3, IKKα, IKKβ, JNK2α2, Lck, Met, MKK4, MKK6, MST2, NEK2, p70S6K, PDGFRβ, PKA, PKBα, PKD2, Rsk1, SAPK2α, SAPK2β, SAPK3, SGK, Tie2 and TrkB kinases.

    摘要翻译： 本发明提供式I化合物：其中R 1 -R 6在发明概述中描述; 包含这些化合物的药物组合物和使用这些化合物治疗或预防与异常或失调的激酶活性相关的疾病或病症的方法，特别是涉及Abl，Bcr-Abl，BMX，BTK，CHK2，b异常活化的疾病或病症 -RAF，c-RAF，CSK，c-SRC，Fes，FGFR3，Flt3，IKKα，IKK＆bgr;JNK2α2，Lck，Met，MKK4，MKK6，MST2，NEK2，p70S6K，PDGFR＆bgr; PKA，PKBα，PKD2，Rsk1 ，SAPK2α，SAPK2＆bgr，SAPK3，SGK，Tie2和TrkB激酶。

    Controlled release of thioamide moiety-containing therapeutic agents
    27.
    发明授权
    Controlled release of thioamide moiety-containing therapeutic agents 失效
    含硫酰胺部分的治疗剂的控制释放

    公开(公告)号：US06468522B1

    公开(公告)日：2002-10-22

    申请号：US09621109

    申请日：2000-07-21

    申请人： Stanley Stein ,  Guobao Zhang ,  Bo Qiu

    发明人： Stanley Stein ,  Guobao Zhang ,  Bo Qiu

    IPC分类号： A61K3174

    CPC分类号： A61K47/60 ,  Y10S424/16

    摘要： This invention pertains to disulfide-linked conjugates of therapeutic agents containing at least one thioamide group with polymer comprising at least one thiol group, so as to provide a controlled release pharmaceutical composition for administration to animals for the prophylaxis or treatment of various conditions or diseases. The therapeutic agent conjugate may comprise an inactive or weakly active prodrug form which may be converted into the original therapeutic compound by the natural action of reducing agents in vivo. The composition may comprise a mixture of polymers each with a different thioamide-containing agent attached, or a polymer conjugated with a mixture of thioamide-containing agents. Modified properties of the therapeutic compound potentially provided by the polymer itself, as well as by other compounds also appended to the polymer, include but are not limited to greater water solubility, longer in-vivo half-life (due to larger size of the conjugate), slower release from a sustained-release depot (due to larger size of the conjugate), better oral bioavailability and tissue-specific targeting.

    摘要翻译： 本发明涉及含有至少一种硫代酰胺基团的治疗剂与包含至少一种硫醇基团的聚合物的二硫键连接的缀合物，以提供用于预防或治疗各种病症或疾病的用于给予动物的控释药物组合物。 治疗剂缀合物可以包含无活性或弱活性的前药形式，其可以通过体内还原剂的天然作用转化为原始治疗化合物。 组合物可以包含各自与不同含硫代酰胺的试剂连接的聚合物的混合物，或与含硫代酰胺的试剂的混合物缀合的聚合物。 由聚合物本身以及也附加到聚合物上的其它化合物可以提供的治疗化合物的改性特征包括但不限于更大的水溶性，更长的体内半衰期（由于缀合物的较大尺寸 ），缓释片段的释放缓慢（由于缀合物的尺寸较大），更好的口服生物利用度和组织特异性靶向。