REVERSE-TURN MIMETICS AND METHOD RELATING THERETO
    4.
    发明申请
    REVERSE-TURN MIMETICS AND METHOD RELATING THERETO 有权
    反向转换和相关的方法

    公开(公告)号:US20100081655A1

    公开(公告)日:2010-04-01

    申请号:US12541388

    申请日:2009-08-14

    摘要: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures 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 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反转转区的二级结构的构象约束化合物。 这种反转模拟结构在广泛的领域中具有实用性,包括用作诊断和治疗剂。 还公开了包含本发明的反转模拟结构的文库以及用于筛选其的方法以鉴定生物活性成员。 本发明还涉及这种化合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,特别是结肠直肠癌,与血管成形术,多囊肾病,异常血管生成疾病,类风湿性关节炎疾病,结节性硬化综合征相关的再狭窄 ,阿尔茨海默氏病,过度毛发生长或损失,或溃疡性结肠炎。

    Guanosine-rich modified oligonucleotides and antiproliferative activity thereof
    6.
    发明授权
    Guanosine-rich modified oligonucleotides and antiproliferative activity thereof 有权
    富含肌氨酸的修饰的寡核苷酸及其抗增殖活性

    公开(公告)号:US09056886B2

    公开(公告)日:2015-06-16

    申请号:US13381326

    申请日:2010-06-29

    IPC分类号: C07H19/173 C07H21/00

    CPC分类号: C07H19/173 C07H21/00

    摘要: The present invention relates to a novel modified oligonucleotide comprising at least one guanosine molecule and a modified nucleic acid with therapeutic efficacies. The present invention also relates to a pharmaceutical composition having cell apoptotic activity against cancer cells for preventing or treating cancer comprising a guanosine-rich modified oligonucleotide with at least one therapeutically effective modified nucleic acid (N), or its pharmaceutically acceptable salt as active ingredient.

    摘要翻译: 本发明涉及包含至少一种鸟苷分子和具有治疗功效的修饰的核酸的新型修饰寡核苷酸。 本发明还涉及具有细胞凋亡活性的药物组合物,其具有用于预防或治疗癌症的细胞凋亡活性,其包含富含鸟嘌呤的修饰的寡核苷酸与至少一种治疗有效的修饰的核酸(N)或其药学上可接受的盐作为活性成分。

    Reverse-turn mimetics and method relating thereto
    7.
    发明授权
    Reverse-turn mimetics and method relating thereto 有权
    反转模拟物及其相关方法

    公开(公告)号:US08318738B2

    公开(公告)日:2012-11-27

    申请号:US13194428

    申请日:2011-07-29

    IPC分类号: C07D487/04 A61K31/53

    CPC分类号: C07D487/04

    摘要: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures 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 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反转转区的二级结构的构象约束化合物。 这种反转模拟结构在广泛的领域中具有实用性,包括用作诊断和治疗剂。 还公开了包含本发明的反转模拟结构的文库以及用于筛选其的方法以鉴定生物活性成员。 本发明还涉及这种化合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,特别是结肠直肠癌,与血管成形术,多囊肾病,异常血管生成疾病,类风湿性关节炎疾病,结节性硬化综合征相关的再狭窄 ,阿尔茨海默氏病,过度毛发生长或损失,或溃疡性结肠炎。

    Reverse-turn mimetics and method relating thereto
    8.
    发明授权
    Reverse-turn mimetics and method relating thereto 有权
    反转模拟物及其相关方法

    公开(公告)号:US08138337B2

    公开(公告)日:2012-03-20

    申请号:US12649161

    申请日:2009-12-29

    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转区域的二级结构及其前药的构象约束化合物。 这种反转模拟结构和前药在广泛的领域中具有实用性,包括用作诊断和治疗剂。 还公开了包含本发明的反转模拟结构的文库以及用于筛选其的方法以鉴定生物活性成员。 本发明还涉及这些化合物和前药用于抑制或治疗由Wnt信号传导途径调节的疾病如癌症,特别是结肠直肠癌,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,结节性 硬化综合征,阿尔茨海默氏病,过度头发生长或损失,或溃疡性结肠炎。

    Reverse-turn mimetics and method relating thereto
    9.
    发明授权
    Reverse-turn mimetics and method relating thereto 有权
    反转模拟物及其相关方法

    公开(公告)号:US07932384B2

    公开(公告)日:2011-04-26

    申请号:US12510107

    申请日:2009-07-27

    摘要: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures 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 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反转转区的二级结构的构象约束化合物。 这种反转模拟结构在广泛的领域中具有实用性,包括用作诊断和治疗剂。 还公开了包含本发明的反转模拟结构的文库以及用于筛选其的方法以鉴定生物活性成员。 本发明还涉及这种化合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,特别是结肠直肠癌,与血管成形术,多囊肾病,异常血管生成疾病,类风湿性关节炎疾病,结节性硬化综合征相关的再狭窄 ,阿尔茨海默氏病,过度毛发生长或损失,或溃疡性结肠炎。