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91 条记录 (耗时 0.053 秒)

    Isophthalates as beta-secretase inhibitors
    12.
    发明授权
    Isophthalates as beta-secretase inhibitors 有权
    异酞酸酯作为β-分泌酶抑制剂

    公开(公告)号：US07981913B2

    公开(公告)日：2011-07-19

    申请号：US12779986

    申请日：2010-05-14

    申请人： Lorin A. Thompson, III ,  Kenneth M. Boy ,  Jianliang Shi ,  John E. Macor

    发明人： Lorin A. Thompson, III ,  Kenneth M. Boy ,  Jianliang Shi ,  John E. Macor

    IPC分类号： A61K31/42 ,  C07D263/30

    CPC分类号： C07D265/30 ,  C07D207/09 ,  C07D207/12 ,  C07D207/27 ,  C07D265/32 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14

    摘要： There is provided a series of substituted isophthalates of formula (I) or a stereoisomer thereof; or a pharmaceutically acceptable salt thereof, wherein W, R3, R5 and R6 as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.

    摘要翻译： 提供了一系列取代的式（I）的间苯二甲酸酯或其立体异构体; 或其药学上可接受的盐，其中如本文所定义的W，R 3，R 5和R 6，其药物组合物和使用方法。 这些新化合物通过分泌酶抑制淀粉样蛋白前体蛋白（APP）的加工，更具体地，抑制Aβ的生成。 本公开涉及可用于治疗与淀粉样蛋白产生相关的神经系统疾病的化合物，例如阿尔茨海默病和受抗淀粉样蛋白活性影响的其它病症。

    Gamma-lactams as beta-secretase inhibitors
    14.
    发明授权
    Gamma-lactams as beta-secretase inhibitors 有权
    γ-内酰胺酶作为β-分泌酶抑制剂

    公开(公告)号：US07388007B2

    公开(公告)日：2008-06-17

    申请号：US11206441

    申请日：2005-08-18

    申请人： Lorin A. Thompson, III ,  Kenneth M. Boy ,  Jianliang Shi ,  John E. Macor

    发明人： Lorin A. Thompson, III ,  Kenneth M. Boy ,  Jianliang Shi ,  John E. Macor

    IPC分类号： A61K31/4025 ,  A61K31/5377 ,  C07D207/04 ,  C07D413/12

    CPC分类号： C07D277/42 ,  C07D417/12 ,  C07K5/06139

    摘要： There is provided a series of novel substituted gamma-lactams of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R4, R5 and R6 as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.

    摘要翻译： 提供一系列式（I）的新型取代的γ-内酰胺或立体异构体; 或其药学上可接受的盐，其中R 1，R 2，R 4，R 5和R 5， 它们的药物组合物和使用方法。 这些新型化合物通过β-分泌酶抑制淀粉样前体蛋白（APP）的加工，更具体地，抑制Aβ-肽的产生。 本公开涉及可用于治疗与β-淀粉样蛋白产生相关的神经系统疾病的化合物，例如阿尔茨海默病和受抗淀粉样蛋白活性影响的其它病症。

    Indole acetic acid acyl guanidines as β-secretase inhibitors
    17.
    发明授权
    Indole acetic acid acyl guanidines as β-secretase inhibitors 有权
    吲哚乙酸酰基胍作为β-分泌酶抑制剂

    公开(公告)号：US07601751B2

    公开(公告)日：2009-10-13

    申请号：US11508481

    申请日：2006-08-23

    申请人： Lorin A. Thompson, III ,  Jianliang Shi ,  F. Christopher Zusi ,  Michael F. Dee ,  John E. Macor

    发明人： Lorin A. Thompson, III ,  Jianliang Shi ,  F. Christopher Zusi ,  Michael F. Dee ,  John E. Macor

    IPC分类号： A61K31/404 ,  A61K31/5377 ,  C07D209/04 ,  C07D413/12 ,  C07D241/04

    CPC分类号： C07D209/18

    摘要： There is provided a series of substituted acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, and R8 as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.

    摘要翻译： 提供一系列式（I）的取代酰基胍或立体异构体; 或其药学上可接受的盐，其中如本文所定义的R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8，其药物组合物和使用方法。 这些化合物通过β-分泌酶抑制淀粉样蛋白前体蛋白（APP）的加工，更具体地抑制Aβ-肽的产生。 本公开涉及可用于治疗与β-淀粉样蛋白产生相关的神经系统疾病的化合物，例如阿尔茨海默病和受抗淀粉样蛋白活性影响的其它病症。