NOVEL COMPOUNDS OF REVERSE TURN MIMETICS AND THE USE THEREOF (1)
    9.
    发明公开
    NOVEL COMPOUNDS OF REVERSE TURN MIMETICS AND THE USE THEREOF (1) 有权
    反转新型化合物的新化合物及其用途(1)

    公开(公告)号:EP2212329A2

    公开(公告)日:2010-08-04

    申请号:EP08839568.6

    申请日:2008-10-15

    IPC分类号: C07D487/04

    CPC分类号: C07D487/04 A61K31/53

    摘要: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins as well as their prodrugs are disclosed. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds and prodrugs for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.

    摘要翻译: 公开了模拟生物活性肽和蛋白质的逆转区二级结构的构象约束化合物及其前药。 这种反转模拟结构和前药在广泛领域具有实用性,包括用作诊断剂和治疗剂。 还公开了含有本发明的反向模拟结构的文库以及筛选它们以鉴定生物活性成员的方法。 本发明还涉及这些化合物和前体药物用于抑制或治疗由Wnt信号传导途径调节的疾病例如癌症,特别是结直肠癌,与血管成形术相关的再狭窄,多囊肾病,异常血管生成疾病,类风湿性关节炎疾病,块状 硬化复合物,阿尔茨海默病,过量的头发生长或丧失或溃疡性结肠炎。

    NOVEL COMPOUNDS OF REVERSE TURN MIMETICS AND THE USE THEREOF (2)
    10.
    发明公开
    NOVEL COMPOUNDS OF REVERSE TURN MIMETICS AND THE USE THEREOF (2) 有权
    新的反向转角模拟物化合物及其用途

    公开(公告)号:EP2212328A2

    公开(公告)日:2010-08-04

    申请号:EP08839260.0

    申请日:2008-10-15

    IPC分类号: C07D487/04

    CPC分类号: C07D487/04 A61K31/53

    摘要: Conformationally constrained compounds that are novel and mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins and having bicyclic framework are disclosed, as well as their prodrugs. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. The invention also relates to the use of such compounds for the preparation of a medicament for treating or preventing cancer including an acute myeloid leukemia.