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    Substituted Tetrahydroisoquinolines as Beta-secretase Inhibitors
    1.
    发明申请
    Substituted Tetrahydroisoquinolines as Beta-secretase Inhibitors 有权
    取代四氢异喹啉作为β-分泌酶抑制剂

    公开(公告)号：US20080153868A1

    公开(公告)日：2008-06-26

    申请号：US11951516

    申请日：2007-12-06

    申请人： Lorin A. Thompson ,  Kenneth M. Boy ,  Jianliang Shi ,  John E. Macor ,  Andrew C. Good ,  Lawrence R. Marcin

    发明人： Lorin A. Thompson ,  Kenneth M. Boy ,  Jianliang Shi ,  John E. Macor ,  Andrew C. Good ,  Lawrence R. Marcin

    IPC分类号： A61K31/437 ,  C07D217/00 ,  A61K31/47 ,  A61P25/00 ,  A61P25/28 ,  C07D221/02

    CPC分类号： C07K5/06139 ,  C07D471/04

    摘要： There is provided a series of tetrahydroisoquinoline diaminopropane compounds of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, R8 and R9 are 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）的四氢异喹啉二氨基丙烷化合物或立体异构体; 或其药学上可接受的盐，其中R 8 R 8和R 9如本文所定义，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。

    Substituted tetrahydroisoquinolines as β-secretase inhibitors
    2.
    发明授权
    Substituted tetrahydroisoquinolines as β-secretase inhibitors 有权
    取代的四氢异喹啉作为分泌酶抑制剂

    公开(公告)号：US07902218B2

    公开(公告)日：2011-03-08

    申请号：US11951516

    申请日：2007-12-06

    申请人： Lorin A. Thompson, III ,  Kenneth M. Boy ,  Jianliang Shi ,  John E. Macor ,  Andrew C. Good ,  Lawrence R. Marcin

    发明人： Lorin A. Thompson, III ,  Kenneth M. Boy ,  Jianliang Shi ,  John E. Macor ,  Andrew C. Good ,  Lawrence R. Marcin

    IPC分类号： C07D217/00 ,  A61K31/47

    CPC分类号： C07K5/06139 ,  C07D471/04

    摘要： There is provided a series of tetrahydroisoquinoline diaminopropane compounds of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, R8 and R9 are 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）的四氢异喹啉二氨基丙烷化合物或立体异构体; 或其药学上可接受的盐，其中R，R 8和R 9如本文所定义，其药物组合物和使用方法。 这些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。

    Isophthalates as beta-secretase inhibitors
    9.
    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：US07745470B2

    公开(公告)日：2010-06-29

    申请号：US11370728

    申请日：2006-03-08

    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。