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    Method of Diagnosing Prodromal Forms of Diseases Associated With Amyloid Deposition
    1.
    发明申请
    Method of Diagnosing Prodromal Forms of Diseases Associated With Amyloid Deposition 审中-公开
    诊断与淀粉样蛋白沉积相关的疾病的原型形式的方法

    公开(公告)号：US20080286202A1

    公开(公告)日：2008-11-20

    申请号：US11666084

    申请日：2005-07-01

    Applicant: William E. Klunk ,  Chester A. Mathis Jr.

    Inventor： William E. Klunk ,  Chester A. Mathis Jr.

    IPC: A61K51/04 ,  A61K49/00 ,  A61K49/04 ,  C07D277/66 ,  A61K49/10

    CPC classification number: A61K51/0478

    Abstract: A method of identifying a patient as prodromal to a disease associated with amyloid deposition by imaging techniques is provided. In addition, a method of identifying amyloid deposition diseases in patients who present with a dementing disorder of questionable etiology by imaging techniques is provided. The methods discloses substances which are used for imaging and generating data which can be used to determine progress of an asymptomatic patient to a disease associated with amyloid deposition, or to identify amyloid deposition diseases in patients who present with a dementing disorder of questionable etiology.

    Abstract translation: 提供了通过成像技术将患者识别为与淀粉样蛋白沉积相关的疾病的前驱性的方法。 另外，提供了一种通过成像技术鉴定出具有可疑病因的痴呆病症的患者中淀粉样蛋白沉积疾病的方法。 该方法公开了用于成像和产生数据的物质，其可以用于确定无症状患者对与淀粉样蛋白沉积相关的疾病的进展，或鉴定存在具有可疑病因的痴呆病症的患者中的淀粉样蛋白沉积疾病。

    Isotopically-Labeled Benzofuran Compounds as Imaging Agents for Amyloidogenic Proteins
    2.
    发明申请
    Isotopically-Labeled Benzofuran Compounds as Imaging Agents for Amyloidogenic Proteins 有权
    同位素标记的苯并呋喃化合物作为淀粉样蛋白生成蛋白的成像剂

    公开(公告)号：US20080274058A1

    公开(公告)日：2008-11-06

    申请号：US12064146

    申请日：2006-10-10

    Applicant: William E. Klunk ,  Chester A. Mathis

    Inventor： William E. Klunk ,  Chester A. Mathis

    IPC: A61K49/10 ,  A61K49/00 ,  A61K31/343 ,  A61P25/28 ,  G01N33/53 ,  C07D307/79

    CPC classification number: C07D307/79

    Abstract: 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.

    Abstract translation: 含有至少一种可检测标记的苯并呋喃化合物，所述可检测标记选自131，第123，第124，第125， 76，Br，75 Br，18 F，19 F，11， 提供了用于检测脑淀粉样蛋白沉积物的淀粉样成像剂以及其他淀粉样变性的淀粉样蛋白沉积物 与全身或局部淀粉样变性相关的肽。 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。

    Rapid brain scanning radiopharmaceutical
    3.
    发明授权
    Rapid brain scanning radiopharmaceutical 失效
    快速脑扫描放射性药物

    公开(公告)号：US4647446A

    公开(公告)日：1987-03-03

    申请号：US732517

    申请日：1985-05-09

    Applicant: Thornton W. Sargent, III ,  Alexander T. Shulgin ,  Chester A. Mathis

    Inventor： Thornton W. Sargent, III ,  Alexander T. Shulgin ,  Chester A. Mathis

    IPC: A61K51/04 ,  A61K43/00 ,  A61K49/00 ,  A61K49/02

    CPC classification number: A61K51/0406 ,  A61K2123/00

    Abstract: A method for detecting the blood flow in animals, particularly in the brain, is provided wherein a detectable amount of a novel radioactive compound of the formula I is administered to one animal: ##STR1## wherein R.sub.1 and R.sub.2 are independently alkyl of 1 to 6 carbon atoms or benzyl;R.sub.3 is alkyl of 1 to 6 carbon atoms, benzyl, cyclopropylalkyl of 4 to 6 carbon atoms, or cyanoalkyl of 2 to 6 carbon atoms;R.sub.4 is hydrogen, benzyl or alkyl of 1 to 6 carbon atoms;with the provisos that R.sub.4 is not isopropyl and when R.sub.4 is methyl, R.sub.3 is not benzyl;and X is a radioactive halogen.

    Abstract translation: 提供了一种用于检测动物，特别是脑中血液流动的方法，其中向一种动物施用可检测量的式I的新型放射性化合物：其中R 1和R 2独立地为 1至6个碳原子或苄基; R3是1至6个碳原子的烷基，4至6个碳原子的苄基，环丙基烷基或2至6个碳原子的氰基烷基; R4是氢，苄基或1-6个碳原子的烷基; 条件是R 4不是异丙基，当R 4是甲基时，R 3不是苄基; X是放射性卤素。

    Amyloid imaging as a surrogate marker for efficacy of anti-amyloid therapies
    4.
    发明授权
    Amyloid imaging as a surrogate marker for efficacy of anti-amyloid therapies 有权
    淀粉样蛋白成像作为抗淀粉样蛋白疗法功效的替代标记物

    公开(公告)号：US08343457B2

    公开(公告)日：2013-01-01

    申请号：US13412823

    申请日：2012-03-06

    Applicant: William E. Klunk ,  Chester A. Mathis, Jr.

    Inventor： William E. Klunk ,  Chester A. Mathis, Jr.

    IPC: A61K49/00 ,  A61K51/00

    CPC classification number: A61K51/0453 ,  A61K49/0002 ,  A61K49/0438 ,  A61K49/10 ,  A61K51/0474

    Abstract: 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.

    Abstract translation: 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。

    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

    Applicant: William E. KLUNK ,  Chester A. MATHIS, JR.

    Inventor： William E. KLUNK ,  Chester A. MATHIS, JR.

    IPC: A61K51/04 ,  A61K49/10 ,  A61K49/00 ,  C07D307/79 ,  G01N33/566

    CPC classification number: C07D307/79

    Abstract: 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.

    Abstract translation: 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。

    THIOFLAVIN DERIVATES FOR USE IN THE ANTEMORTEM DIAGNOSIS OF ALZHEIMER'S DISEASE AND IN VIVO IMAGING AND PREVENTION OF AMYLOID DEPOSITION
    7.
    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

    Applicant: William E. KLUNK ,  Chester A. Mathis, JR. ,  Yanming Wang

    Inventor： William E. KLUNK ,  Chester A. Mathis, JR. ,  Yanming Wang

    IPC: C07D417/10 ,  C07D277/64

    CPC classification number: A61K31/5415 ,  A61K31/428 ,  A61K51/0497 ,  C07B2200/05 ,  C07D277/64 ,  C07D277/66

    Abstract: 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.

    Abstract translation: 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。

    Amyloid imaging as a surrogate marker for efficacy of anti-amyloid therapies
    8.
    发明授权
    Amyloid imaging as a surrogate marker for efficacy of anti-amyloid therapies 有权
    淀粉样蛋白成像作为抗淀粉样蛋白疗法功效的替代标记物

    公开(公告)号：US08147798B2

    公开(公告)日：2012-04-03

    申请号：US11666083

    申请日：2005-07-01

    Applicant: William E. Klunk ,  Chester A. Mathis, Jr.

    Inventor： William E. Klunk ,  Chester A. Mathis, Jr.

    IPC: A61K49/00 ,  A61K51/00

    CPC classification number: A61K51/0453 ,  A61K49/0002 ,  A61K49/0438 ,  A61K49/10 ,  A61K51/0474

    Abstract: 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.

    Abstract translation: 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。

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