ALZHEIMER'S DISEASE ASSAY IN A LIVING PATIENT
    1.
    发明申请
    ALZHEIMER'S DISEASE ASSAY IN A LIVING PATIENT 审中-公开
    ALZHEIMER在生活中的疾病测定

    公开(公告)号:US20160266149A1

    公开(公告)日:2016-09-15

    申请号:US15167370

    申请日:2016-05-27

    IPC分类号: G01N33/68

    摘要: An assay for Alzheimer's disease pathology (AD) in a living patient is disclosed wherein an amount of α7nAChR or TLR4 in a FLNA-captured protein complex or α7nAChR in an Aβ-captured protein complex or α7nAChR-FLNA, TLR4-FLNA and/or α7nAChR-Aβ42 complex present as a protein-protein complex in a sample is determined and compared to the amount in a standard sample from a person free of AD pathology. An amount greater than in the standard sample indicates AD pathology. Also disclosed is an assay predictive of prognosis for treatment with a medicament in which the amount of an above protein or protein complex is determined and compared to an amount determined in the presence of a medicament that binds to a FLNA pentapeptide and contains at least four of the six pharmacophores of FIGS. 7-12. An amount of protein or protein complex determined in the presence of the medicament less than the first determined amount indicates a favorable treatment prognosis.

    摘要翻译: 公开了一种活体患者中阿尔茨海默病病理学(AD)的测定法,其中在被捕获的FLNA捕获的蛋白质复合物中的α7nAChR或TLR4或Aβ捕获的蛋白质复合物或α7nAChR-FLNA,TLR4-FLNA和/或α7nAChR中的α7nAChR 确定样品中作为蛋白质 - 蛋白质复合物存在的-Aβ42复合物,并与来自不存在AD病理学的人的标准样品中的量进行比较。 大于标准样品的量表示AD病理学。 还公开了一种预测用于治疗药物的预测的方法,其中确定上述蛋白质或蛋白质复合物的量并将其与在与FLNA五肽结合并且含有至少四种 图6的六个药效团。 7-12。 在小于第一确定量的药物存在下测定的蛋白质或蛋白质复合物的量表明有利的治疗预后。

    Alzheimer's disease assay in a living patient
    2.
    发明授权
    Alzheimer's disease assay in a living patient 有权
    阿尔茨海默病测定在一个活的病人

    公开(公告)号:US09354223B2

    公开(公告)日:2016-05-31

    申请号:US13942326

    申请日:2013-07-15

    IPC分类号: G01N33/50 G01N33/94 G01N33/68

    摘要: An assay for Alzheimer's disease (AD) pathology in a living patient is disclosed wherein an amount of α7nAChR or TLR4 in a FLNA-captured protein complex or α7nAChR in an Aβ-captured protein complex or α7nAChR-FLNA, or TLR4-FLNA and/or α7nAChR-Aβ42 complex present as a protein-protein complex in a sample is compared to the amount in a standard sample from a person free of AD pathology. An amount greater than in the standard sample indicates AD pathology. Also disclosed is an assay predictive of prognosis for treatment with a medicament in which the amount of an above protein or protein complex is compared to an amount in the presence of a medicament that binds to a FLNA pentapeptide and contains at least four pharmacophores of FIGS. 7-12. An amount of protein or protein complex determined in the presence of medicament that is less than the first amount indicates a favorable treatment prognosis.

    摘要翻译: 公开了一种活体患者的阿尔茨海默氏病(AD)病理学测定法,其中在被捕获的蛋白质复合物或α7nAChR-FLNA或TLR4-FLNA中的α7nAChR或TLR4或α7nAChR或TLR4-FLNA和/ 或作为样品中蛋白质 - 蛋白质复合物存在的α7nAChR-A&bgr; 42复合物与来自不具有AD病理学的人的标准样品中的量进行比较。 大于标准样品的量表示AD病理学。 还公开了一种预测用于用药物进行治疗的预测的测定法,其中将上述蛋白质或蛋白质复合物的量与结合FLNA五肽并含有至少四种图1和2的药效学的药物存在下的量进行比较。 7-12。 在小于第一量的药物存在下测定的蛋白质或蛋白质复合物的量表明有利的治疗预后。

    FILAMIN A BINDING ANTI-INFLAMMATORY AND ANALGESIC
    3.
    发明申请
    FILAMIN A BINDING ANTI-INFLAMMATORY AND ANALGESIC 有权
    菲林蛋白结合抗炎和毒理学

    公开(公告)号:US20140113895A1

    公开(公告)日:2014-04-24

    申请号:US14137374

    申请日:2013-12-20

    摘要: A compound or its pharmaceutically acceptable salt, optionally including both individual enantiomeric forms, a racemate, diastereomers and mixtures thereof, composition and method are disclosed that can provide analgesia and reduce inflammation. A contemplated compound has a structure that corresponds to Formula A, wherein the R group substituents, d, e, f, k, n, m, D, E, F, K, G, P, Q, W, and Z are defined within.

    摘要翻译: 公开了可以提供止痛和减轻炎症的化合物或其药学上可接受的盐,任选地包括单独的对映体形式,外消旋物,非对映异构体及其混合物。 考虑的化合物具有对应于式A的结构,其中R基团取代基d,e,f,k,n,m,D,E,F,K,G,P,Q,W和Z被定义 中。

    BENZAZOCINE-RING COMPOUND INHIBITION OF TAU HYPERPHOSPHORYLATION
    4.
    发明申请
    BENZAZOCINE-RING COMPOUND INHIBITION OF TAU HYPERPHOSPHORYLATION 审中-公开
    苯并噻吩化合物抑制TAO高磷酸化

    公开(公告)号:US20140094482A1

    公开(公告)日:2014-04-03

    申请号:US13968078

    申请日:2013-08-15

    IPC分类号: A61K31/485 C12N5/079

    摘要: A method of inhibiting hyperphosphorylation of the tau protein and/or a TLR4-mediated immune response is disclosed. The method contemplates administering to cells in recognized need thereof such as cells of the central nervous system a FLNA-binding effective amount of a FLNA-binding benzazocine-ring compound or a pharmaceutically acceptable salt thereof such as a) an opioid receptor antagonist compound or b) a mixed opioid receptor agonist and antagonist (agonist/antagonist) compound, c) an opioid receptor agonist compound or d) an enantiomer of an opioid receptor interacting compound, that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1. The administered compound preferably contains at least four of the six pharmacophores of FIGS. 5-10.

    摘要翻译: 公开了抑制tau蛋白和/或TLR4介导的免疫应答的高度磷酸化的方法。 该方法考虑对其认识到需要的细胞给药,例如中枢神经系统的细胞,FLNA结合有效量的FLNA结合苯并吖嗪环化合物或其药学上可接受的盐,例如a)阿片受体拮抗剂化合物或b )混合的阿片受体激动剂和拮抗剂(激动剂/拮抗剂)化合物,c)阿片受体激动剂化合物或d)与阿片样物质受体相互作用化合物的对映异构体,其结合SEQ ID NO: 施用的化合物优选含有图6和图6的六个药效团中的至少四个。 5-10。

    Filamin A binding anti-inflammatory and analgesic
    8.
    发明授权
    Filamin A binding anti-inflammatory and analgesic 有权
    Filamin A结合消炎止痛药

    公开(公告)号:US08614324B2

    公开(公告)日:2013-12-24

    申请号:US12719624

    申请日:2010-03-08

    IPC分类号: C07D491/10

    摘要: A compound or its pharmaceutically acceptable salt, optionally including both individual enantiomeric forms, a racemate, diastereomers and mixtures thereof, composition and method are disclosed that can provide analgesia and reduce inflammation. A contemplated compound has a structure that corresponds to Formula A, wherein the R group substituents, d, e, f, k, n, m, D, E, F, K, G, P, Q, W, and Z are defined within.

    摘要翻译: 公开了可以提供止痛和减轻炎症的化合物或其药学上可接受的盐,任选地包括单独的对映体形式,外消旋物,非对映异构体及其混合物。 考虑的化合物具有对应于式A的结构,其中R基团取代基d,e,f,k,n,m,D,E,F,K,G,P,Q,W和Z被定义 中。