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    HYDANTOINS THAT MODULATE BACE-MEDIATED APP PROCESSING
    1.
    发明申请
    HYDANTOINS THAT MODULATE BACE-MEDIATED APP PROCESSING 审中-公开
    调制面媒介应用程序处理的H​​YDANTOINS

    公开(公告)号：WO2014127042A1

    公开(公告)日：2014-08-21

    申请号：PCT/US2014/016100

    申请日：2014-02-12

    Applicant: BUCK INSTITUTE FOR RESEARCH ON AGING

    Inventor： JOHN, Varghese ,  BREDESEN, Dale E.

    IPC: C07D233/88 ,  C07D233/70 ,  C07D401/10 ,  A61K31/4166 ,  A61P25/00

    CPC classification number: C07D233/76 ,  A61K31/4166 ,  A61K31/4168 ,  A61K31/4439 ,  A61K31/46 ,  A61K31/506 ,  A61K45/06 ,  C07D233/70 ,  C07D233/88 ,  C07D401/04 ,  C07D401/10 ,  C07D403/10 ,  A61K2300/00

    Abstract: In certain embodiments hydantoin compounds are provided herein that are effective to inhibit BACE activity against APP. Without being bound to a particular theory, it is believed the activity of the hydantoins identified herein appears to be associated with binding to BACE and/or to APP particularly when these moieties form a BACE/APP complex. Accordingly, it is believed the compounds described herein represent a new class of compounds designated herein as APP-Binding-BACE Inhibitors (ABBIs) and provide a new mechanism to modulate APP processing. The hydantoins described herein appear to show improved brain permeability and functional BACE inhibition.

    Abstract translation: 在某些实施方案中，本文提供了有效抑制针对APP的BACE活性的乙内酰脲化合物。 不受特定理论的约束，据信本文鉴定的乙内酰脲的活性似乎与结合BACE和/或APP有关，特别是当这些部分形成BACE / APP复合物时。 因此，据信本文所述的化合物代表本文中称为APP-结合-BACE抑制剂（ABBI）的新一类化合物，并提供调节APP处理的新机制。 本文所述的乙内酰脲似乎显示改善的脑渗透性和功能性BACE抑制。

    TROPINOL ESTERS AND RELATED COMPOUNDS TO PROMOTE NORMAL PROCESSING OF APP
    3.
    发明申请
    TROPINOL ESTERS AND RELATED COMPOUNDS TO PROMOTE NORMAL PROCESSING OF APP 审中-公开
    TROPINOL酯和相关化合物促进APP的正常加工

    公开(公告)号：WO2013019901A2

    公开(公告)日：2013-02-07

    申请号：PCT/US2012/049223

    申请日：2012-08-01

    Applicant: BUCK INSTITUTE FOR RESEARCH ON AGING ,  JOHN, Varghese ,  BREDESEN, Dale E.

    Inventor： JOHN, Varghese ,  BREDESEN, Dale E.

    IPC: A61K31/49

    CPC classification number: C07D453/02 ,  A61K31/439 ,  A61K31/444 ,  A61K45/06 ,  C07D451/12

    Abstract: In various embodiments, compositions and methods are provided for treatment and/or prevention of amyloidogenic diseases. In certain embodiments, the methods entail administering an effective amount of a tropinol ester to a subject in need thereof for prophylactic or therapeutic effect. The methods are particularly useful for prophylactic and therapeutic treatment of Alzheimer's disease. In certain embodiments, methods of reducing the risk, lessening the severity, or delaying the progression or onset of a disease characterized by beta-amyloid deposits in the brain of a mammal are also provided. In certain embodiments, methods of directly or indirectly inhibiting the C-terminal cleavage of APP resulting in the formation of APP-C31 peptide and APPneo (APP664) in a mammal are provided.

    Abstract translation: 在各种实施方案中，提供了用于治疗和/或预防致淀粉样变性疾病的组合物和方法。 在某些实施方案中，该方法需要将有效量的托品醇酯给予有需要的受试者以用于预防或治疗效果。 该方法对于预防和治疗阿尔茨海默氏病特别有用。 在某些实施方案中，还提供了降低哺乳动物脑中特征为β-淀粉样蛋白沉积物的疾病的风险，减轻严重程度或延迟疾病的进展或发作的方法。 在某些实施方案中，提供了直接或间接抑制APP的C末端切割从而导致哺乳动物中APP-C31肽和APPneo（APP664）形成的方法。

    COMPOUNDS TO PROMOTE NORMAL PROCESSING OF APP
    5.
    发明申请
    COMPOUNDS TO PROMOTE NORMAL PROCESSING OF APP 审中-公开
    化合物促进APP的正常加工

    公开(公告)号：WO2017197177A1

    公开(公告)日：2017-11-16

    申请号：PCT/US2017/032251

    申请日：2017-05-11

    Applicant: BUCK INSTITUTE FOR RESEARCH ON AGING

    Inventor： JOHN, Varghese ,  BREDESEN, Dale, E. ,  SPILMAN, Patricia, R. ,  JAGODZINSKA, Barbara

    IPC: C07D451/10 ,  C07D209/04 ,  A61K31/46 ,  A61K31/404

    Abstract: In various embodiments, compositions and methods are provided for treatment and/or prevention of amyloidogenic diseases. In certain embodiments, the methods entail administering an effective amount of compound C41 to a subject in need thereof for prophylactic or therapeutic effect. The methods are particularly useful for prophylactic and therapeutic treatment of Alzheimer's disease. In certain embodiments, methods of reducing the risk, lessening the severity, or delaying the progression or onset of a disease characterized by beta-amyloid deposits in the brain of a mammal are also provided. In certain embodiments, methods of directly or indirectly enhances sAPPα, lowers Aβ, p-Tau, inhibits the C-terminal cleavage of APP resulting in the formation of APP-C31 peptide and APPneo (APP664) and improves memory in a mammal are provided.

    Abstract translation: 在各种实施方案中，提供了用于治疗和/或预防致淀粉样变性疾病的组合物和方法。 在某些实施方案中，该方法需要将有效量的化合物C41给予有需要的受试者以用于预防或治疗效果。 该方法对于预防和治疗阿尔茨海默氏病特别有用。 在某些实施方案中，还提供了降低哺乳动物脑中特征为β-淀粉样蛋白沉积物的疾病的风险，减轻严重程度或延迟疾病的进展或发作的方法。 在某些实施方案中，提供了直接或间接增强sAPPα，降低Aβ，p-Tau，抑制APP的C末端切割导致APP-C31肽和APPneo（APP664）形成并改善哺乳动物记忆力的方法。

    FORMULATIONS AND METHODS FOR THE TREATMENT OR PROPHYLAXIS OF PRE-MCI AND/OR PRE-ALZHEIMER'S CONDITIONS
    7.
    发明申请
    FORMULATIONS AND METHODS FOR THE TREATMENT OR PROPHYLAXIS OF PRE-MCI AND/OR PRE-ALZHEIMER'S CONDITIONS 审中-公开
    预处理或预处理或预处理条件的处理或预处理的制剂和方法

    公开(公告)号：WO2013123426A1

    公开(公告)日：2013-08-22

    申请号：PCT/US2013/026487

    申请日：2013-02-15

    Applicant: BUCK INSTITUTE FOR RESEARCH ON AGING ,  JOHN, Varghese ,  BREDESEN, Dale E. ,  TZANNIS, Stelios

    Inventor： JOHN, Varghese ,  BREDESEN, Dale E. ,  TZANNIS, Stelios

    IPC: A61K31/439 ,  A61K9/22 ,  A61K9/20 ,  A61K47/40 ,  A61K47/36

    CPC classification number: A61K31/439 ,  A61K9/006 ,  A61K9/20 ,  A61K31/05 ,  A61K31/145 ,  A61K31/46 ,  A61K31/5513 ,  A61K31/724 ,  A61K47/48969 ,  A61K47/6951 ,  A61K2300/00

    Abstract: In certain embodiments the methods of preventing or delaying the onset of a pre-Alzheimer's condition and/or cognitive dysfunction, and/or ameliorating one or more symptoms of a pre-Alzheimer's cognitive dysfunction, and/or preventing or delaying the progression of a pre-Alzheimer's condition or cognitive dysfunction to Alzheimer's disease, and/or of promoting the processing of amyloid precursor protein (APP) by the non-amyloidogenic pathway are provided. In certain embodiments the methods involve administering, or causing to be administered, to a subject in need thereof certain formulations comprising or more active agent(s) selected from the group consisting of tropisetron disulfiram, honokiol, nimetazepam, and/or derivatives or analogs thereof.

    Abstract translation: 在某些实施方案中，预防或延迟阿尔茨海默病前状态和/或认知功能障碍的发作和/或改善前阿尔茨海默病认知功能障碍的一种或多种症状的方法，和/或预防或延迟前阿尔茨海默氏病的进展 提供阿尔茨海默氏病或​​阿尔茨海默病的认知功能障碍和/或通过非淀粉样蛋白生成途径促进淀粉样蛋白前体蛋白（APP）的加工。 在某些实施方案中，所述方法包括向有需要的受试者施用或引起给予受试者某些制剂，其包含或多于一种选自托烷司琼双硫仑，和厚朴酚，尼米西泮和/或其衍生物或类似物的活性剂 。

    TRKA AS A TARGET FOR INHIBITING APP CLEAVAGE AND/OR PROGRESSION OF ALZHEIMER'S DISEASE
    8.
    发明申请
    TRKA AS A TARGET FOR INHIBITING APP CLEAVAGE AND/OR PROGRESSION OF ALZHEIMER'S DISEASE 审中-公开
    TRKA作为抑制阿尔茨海默病应用切割和/或进展的目标

    公开(公告)号：WO2013026021A2

    公开(公告)日：2013-02-21

    申请号：PCT/US2012/051426

    申请日：2012-08-17

    Applicant: BUCK INSTITUTE FOR RESEARCH ON AGING ,  JOHN, Varghese ,  ZHANG, Qiang ,  BREDESEN, Dale, E.

    Inventor： JOHN, Varghese ,  ZHANG, Qiang ,  BREDESEN, Dale, E.

    IPC: A61K48/00 ,  A61K38/43

    CPC classification number: C07K14/71 ,  A61K31/433 ,  C07K14/4711 ,  C12N2999/005

    Abstract: In various embodiments method are provided for inhibiting (partially or fully) the C-terminal cleavage of APP resulting in the formation of APP-C31 peptide and APPneo (APP664) in a mammal. The methods typically involve administering or causing to be administered to the mammal a TrkA kinase inhibitor in an amount sufficient to reduce C-terminal cleavage of APP and production of a C31 peptide and/or APPneo. In certain embodiments the inhibitor comprises ADDN-1351 or a derivative thereof.

    Abstract translation: 在各种实施方案中，提供了用于抑制（部分或完全）APP的C末端切割从而导致在哺乳动物中形成APP-C31肽和APPneo（APP664）的方法。 所述方法通常涉及以足以减少APP的C末端切割和产生C31肽和/或APPneo的量向哺乳动物施用或导致施用TrkA激酶抑制剂。 在某些实施方案中，抑制剂包含ADDN-1351或其衍生物。

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