2-heteroaryl substituted benzothiophenes and benzofuranes 709
    5.
    发明授权
    2-heteroaryl substituted benzothiophenes and benzofuranes 709 有权
    2-杂芳基取代的苯并噻吩和苯并呋喃709

    公开(公告)号:US07772256B2

    公开(公告)日:2010-08-10

    申请号:US12042795

    申请日:2008-03-05

    IPC分类号: A61K31/443 C07D405/04

    摘要: The present invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives, precursors thereof, and therapeutic uses of such compounds, having the structural formula (Ia) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents.

    摘要翻译: 本发明涉及新的2-杂芳基取代的苯并噻吩和苯并呋喃衍生物及其前体,以及具有以下结构式(Ia)的这类化合物及其药学上可接受的盐,组合物和使用方法的治疗用途。 此外,本发明涉及适用于生活患者淀粉样蛋白沉积物成像,其组成,使用方法和制备这些化合物的方法的新型2-杂芳基取代的苯并噻吩和苯并呋喃衍生物。 更具体地说,本发明涉及一种在体内淀粉样蛋白沉积物在体内成像以使阿尔茨海默病的止血诊断成为可能并测量阿尔茨海默病治疗剂的临床疗效的方法。

    Spirooxindole derivatives that act as analgesics
    6.
    发明授权
    Spirooxindole derivatives that act as analgesics 失效
    作为镇痛药的螺氧吲哚衍生物

    公开(公告)号:US06774132B1

    公开(公告)日:2004-08-10

    申请号:US09674373

    申请日:2000-10-27

    IPC分类号: A61K31437

    摘要: The present invention relates to certain spirooxindole derivatives and to pharmaceutically acceptable salts thereof, which exhibit good analgesic properties and are effective in the treatment of chronic pain. The derivatives have the structure of formula I: wherein: Ar is benzene or pyridine; X is NHCO—; —CONH—; or —NH—SO2—; Y is a single bond; and Z is —CH═CHCH2.

    摘要翻译: 本发明涉及某些螺恶唑衍生物及其药学上可接受的盐,它们具有良好的止痛特性并且有效治疗慢性疼痛。 衍生物具有式I的结构:其中:Ar为苯或吡啶; X为NHCO-; -CONH-; 或-NH-SO 2 - ; Y是单键; Z为-CH = CHCH 2。

    Compounds and their use as BACE inhibitors
    9.
    发明申请
    Compounds and their use as BACE inhibitors 审中-公开
    化合物及其作为BACE抑制剂的用途

    公开(公告)号:US20120165346A1

    公开(公告)日:2012-06-28

    申请号:US13331231

    申请日:2011-12-20

    CPC分类号: C07D401/14 C07D403/14

    摘要: The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.

    摘要翻译: 本发明涉及新的式(I)化合物及其药物组合物。 此外,本发明涉及用于治疗和/或预防与疾病相关的病症如唐氏综合征和淀粉样血管病变的治疗方法,例如但不限于脑淀粉样血管病或遗传性脑出血,与 认知障碍,例如但不限于MCI(“轻度认知障碍”),阿尔茨海默病,记忆丧失,与阿尔茨海默病相关的注意力缺陷症状,与诸如阿尔茨海默氏病或​​痴呆症的疾病相关的神经变性,包括混合血管和退行性来源的痴呆, 老年性痴呆,老年性痴呆和与帕金森病相关的痴呆,进行性核上性麻痹或皮质基底变性。

    Novel Heteroaryl Substituted Benzoxazoles
    10.
    发明申请
    Novel Heteroaryl Substituted Benzoxazoles 失效
    新型杂芳基取代苯并恶唑

    公开(公告)号:US20080027051A1

    公开(公告)日:2008-01-31

    申请号:US11763151

    申请日:2007-06-14

    CPC分类号: C07D413/04

    摘要: The present invention relates to novel heteroaryl substituted benzoxazole derivatives and therapeutic uses for such compounds, having the structural formula (Ia) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzoxazole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measureing clinical efficacy of Alzheimer's disease therapeutic agents.

    摘要翻译: 本发明涉及新颖的杂芳基取代的苯并恶唑衍生物和具有以下结构式(Ia)的化合物及其药学上可接受的盐,组合物和使用方法的治疗用途。 此外,本发明涉及适用于在活体患者中成像淀粉样蛋白沉积物的新型杂芳基取代的苯并恶唑衍生物,其组合物,使用方法和制备此类化合物的方法。 更具体地说,本发明涉及在体内淀粉样蛋白沉积物在体内成像以使阿尔茨海默病的抗原异常诊断以及阿尔茨海默病治疗剂的临床疗效的测定方法。