THIOFLAVIN DERIVATES FOR USE IN THE ANTEMORTEM DIAGNOSIS OF ALZHEIMER'S DISEASE AND IN VIVO IMAGING AND PREVENTION OF AMYLOID DEPOSITION
    2.
    发明申请
    THIOFLAVIN DERIVATES FOR USE IN THE ANTEMORTEM DIAGNOSIS OF ALZHEIMER'S DISEASE AND IN VIVO IMAGING AND PREVENTION OF AMYLOID DEPOSITION 审中-公开
    用于阿尔茨海默病和体内成像和预防淀粉样沉积症的手术诊断中的三唑衍生物

    公开(公告)号:US20120095235A1

    公开(公告)日:2012-04-19

    申请号:US13310243

    申请日:2011-12-02

    IPC分类号: C07D417/10 C07D277/64

    摘要: This invention relates to novel thioflavin derivatives, methods of using the derivatives in, for example, in vivo imaging of patients having neuritic plaques, pharmaceutical compositions comprising the thioflavin derivatives and method of synthesizing the compounds. The compounds find particular use in the diagnosis and treatment of patients having diseases where accumulation of neuritic plaques are prevalent. The disease states or maladies include but are not limited to Alzheimer's Disease, familial Alzheimer's Disease, Down's Syndrome and homozygotes for the apolipoprotein E4 allele.

    摘要翻译: 本发明涉及新型硫黄素衍生物,在例如具有神经炎斑块的患者的体内成像中使用衍生物的方法,包含硫代黄素衍生物的药物组合物和合成该化合物的方法。 该化合物特别用于诊断和治疗患有神经炎斑块积聚的疾病的患者。 疾病状态或疾病包括但不限于阿尔茨海默病,家族性阿尔茨海默氏病,唐氏综合征和载脂蛋白E4等位基因的纯合子。

    ISOTOPICALLY-LABELED BENZOFURAN COMPOUNDS AS IMAGING AGENTS FOR AMYLOIDOGENIC PROTEINS
    5.
    发明申请
    ISOTOPICALLY-LABELED BENZOFURAN COMPOUNDS AS IMAGING AGENTS FOR AMYLOIDOGENIC PROTEINS 审中-公开
    同位素标记的苯甲醚化合物作为淀粉样蛋白成像剂

    公开(公告)号:US20120148494A1

    公开(公告)日:2012-06-14

    申请号:US13359040

    申请日:2012-01-26

    CPC分类号: C07D307/79

    摘要: Benzofuran compounds which contain at least one detectable label selected from the group consisting of 131I, 123I, 124I, 76Br, 75Br, 18F, 19F, 11C, 13C, 14C and 3H are provided as amyloid imaging agents for detecting brain amyloid deposits as well as other amyloidogenic peptides associated with systemic or localized amyloidosis. Additionally, the compounds are useful for determining if patients, presenting with clinically confusing cases of dementia or presenting with mild cognitive impairment, have Alzheimer's disease. The compounds are additionally useful as surrogate markers for monitoring the efficacy of anti-amyloidosis therapies.

    摘要翻译: 提供含有选自131I,123I,124I,76Br,75Br,18F,19F,11C,13C,14C和3H中的至少一种可检测标记的苯并呋喃化合物作为用于检测脑淀粉样沉积物的淀粉样成像剂 与全身或局部淀粉样变性相关的其他淀粉样变性肽。 此外,这些化合物可用于确定呈现临床上混淆的痴呆病例或呈现轻度认知障碍的患者是否患有阿尔茨海默氏病。 该化合物另外可用作用于监测抗淀粉样变性治疗功效的替代标志物。

    ISOTOPICALLY-LABELED BENZOFURAN COMPOUNDS AS IMAGING AGENTS FOR AMYLOIDOGENIC PROTEINS
    6.
    发明申请
    ISOTOPICALLY-LABELED BENZOFURAN COMPOUNDS AS IMAGING AGENTS FOR AMYLOIDOGENIC PROTEINS 审中-公开
    同位素标记的苯甲醚化合物作为淀粉样蛋白成像剂

    公开(公告)号:US20120189545A1

    公开(公告)日:2012-07-26

    申请号:US13359077

    申请日:2012-01-26

    CPC分类号: C07D307/79

    摘要: Benzofuran compounds which contain at least one detectable label selected from the group consisting of 131I, 123I, 124I, 125I, 76Br, 75Br, 18F, 19F, 11C, 13C, 14C and 3H are provided as amyloid imaging agents for detecting brain amyloid deposits as well as other amyloidogenic peptides associated with systemic or localized amyloidosis. Additionally, the compounds are useful for determining if patients, presenting with clinically confusing cases of dementia or presenting with mild cognitive impairment, have Alzheimer's disease. The compounds are additionally useful as surrogate markers for monitoring the efficacy of anti-amyloidosis therapies.

    摘要翻译: 提供含有选自131I,123I,124I,125I,76Br,75Br,18F,19F,11C,13C,14C和3H中的至少一种可检测标记的苯并呋喃化合物作为用于检测脑淀粉样沉积物的淀粉样蛋白显像剂 以及与全身或局部淀粉样变性相关的其他淀粉样变性肽。 此外,这些化合物可用于确定呈现临床上混淆的痴呆病例或呈现轻度认知障碍的患者是否患有阿尔茨海默氏病。 该化合物另外可用作用于监测抗淀粉样变性治疗功效的替代标志物。

    AMYLOID IMAGING AS A SURROGATE MARKER FOR EFFICACY OF ANTI-AMYLOID THERAPIES
    7.
    发明申请
    AMYLOID IMAGING AS A SURROGATE MARKER FOR EFFICACY OF ANTI-AMYLOID THERAPIES 有权
    AMYLOID成像作为抗肿瘤治疗效能的标记

    公开(公告)号:US20120177572A1

    公开(公告)日:2012-07-12

    申请号:US13412823

    申请日:2012-03-06

    IPC分类号: A61K51/04 A61P25/28

    摘要: The present method for determining the efficacy of therapy in the treatment of amyloidosis involves administering to a patient in need thereof a compound of formula (I) or formula (II) or structures 1-45 and imaging the patient. After said imaging, at least one anti-amyloid agent is administered to said patient. Then, an effective amount of a compound of formula (I) or formula (II) or structures 1-45 is administered to the patient and the patient is imaged again. Finally, baseline levels of amyloid deposition in the patient before treatment with the anti-amyloid agent are compared with levels of amyloid deposition in the patient following treatment with the anti-amyloid agent.

    摘要翻译: 用于确定治疗淀粉样变性的疗效的本方法涉及向有需要的患者施用式(I)或式(II)化合物或结构1-45并使患者成像。 在所述成像之后,向所述患者施用至少一种抗淀粉样蛋白剂。 然后,向患者施用有效量的式(I)或式(II)或结构1-45的化合物,并再次对患者进行成像。 最后,将用抗淀粉样蛋白剂治疗之前患者淀粉样蛋白沉积的基线水平与用抗淀粉样蛋白剂治疗后患者淀粉样沉积的水平进行比较。

    THIOFLAVIN DERIVATIVES FOR USE IN THE ANTEMORTEM DIAGNOSIS OF ALZHEIMERS DISEASE AND IN VIVO IMAGING AND PREVENTION OF AMYLOID DEPOSITION
    8.
    发明申请
    THIOFLAVIN DERIVATIVES FOR USE IN THE ANTEMORTEM DIAGNOSIS OF ALZHEIMERS DISEASE AND IN VIVO IMAGING AND PREVENTION OF AMYLOID DEPOSITION 审中-公开
    用于治疗ALZHEIMERS疾病和VIVO成像和防止淀粉样沉积的ANTEMORTEM诊断中的三氟衍生物

    公开(公告)号:US20080154042A1

    公开(公告)日:2008-06-26

    申请号:US12046070

    申请日:2008-03-11

    IPC分类号: C07D277/66 C07D417/02

    摘要: This invention relates to novel thioflavin derivatives, methods of using the derivatives in, for example, in vivo imaging of patients having neuritic plaques, pharmaceutical compositions comprising the thioflavin derivatives and method of synthesizing the compounds. The compounds find particular use in the diagnosis and treatment of patients having diseases where accumulation of neuritic plaques are prevalent. The disease states or maladies include but are not limited to Alzheimer's Disease, familial Alzheimer's Disease, Down's Syndrome and homozygotes for the apolipoprotein E4 allele.

    摘要翻译: 本发明涉及新型硫黄素衍生物,在例如具有神经炎斑块的患者的体内成像中使用衍生物的方法,包含硫代黄素衍生物的药物组合物和合成该化合物的方法。 该化合物特别用于诊断和治疗患有神经炎斑块积聚的疾病的患者。 疾病状态或疾病包括但不限于阿尔茨海默病,家族性阿尔茨海默氏病,唐氏综合征和载脂蛋白E4等位基因的纯合子。