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    Use of small molecule radioligands to discover inhibitors of amyloid-beta peptide production and for diagnostic imaging
    1.
    发明申请
    Use of small molecule radioligands to discover inhibitors of amyloid-beta peptide production and for diagnostic imaging 审中-公开
    使用小分子放射性配体发现淀粉样蛋白β肽生产抑制剂和诊断成像

    公开(公告)号：US20050129612A1

    公开(公告)日：2005-06-16

    申请号：US11018331

    申请日：2004-12-21

    申请人： Robert Zaczek ,  Richard Olson ,  Dietmar Seiffert ,  Lorin Thompson

    发明人： Robert Zaczek ,  Richard Olson ,  Dietmar Seiffert ,  Lorin Thompson

    IPC分类号： A61K51/08 ,  A61K51/00

    CPC分类号： A61K51/0468

    摘要： This invention relates to a method of using radiolabelled and/or radiopharmaceutical small molecule inhibitors of beta-amyloid peptide production for the diagnosis of neurological and other disorders involving APP processing and beta-amyloid production. Furthermore, radiolabelled small molecule inhibitors identified by the methods of the present invention would be useful in the diagnosis of neurological disorders, such as Alzheimer's disease, which involve elevated levels of Aβ peptides.

    摘要翻译： 本发明涉及使用放射性标记的和/或放射性药物的β-淀粉样蛋白肽生产的小分子抑制剂用于诊断涉及APP处理和β-淀粉样蛋白生成的神经和其他病症的方法。 此外，通过本发明的方法鉴定的放射性标记的小分子抑制剂可用于诊断涉及升高水平的Aβ肽的神经障碍，例如阿尔茨海默氏病。

    Succinoylamino lactams as inhibitors of A-beta protein production
    4.
    发明申请
    Succinoylamino lactams as inhibitors of A-beta protein production 有权
    琥珀酰氨基内酰胺作为A-β蛋白生产的抑制剂

    公开(公告)号：US20050245501A1

    公开(公告)日：2005-11-03

    申请号：US11175644

    申请日：2005-07-06

    申请人： Richard Olson ,  Thomas Maduskuie ,  Lorin Thompson

    发明人： Richard Olson ,  Thomas Maduskuie ,  Lorin Thompson

    IPC分类号： A61K31/55 ,  A61K31/553 ,  A61K31/554 ,  C07D223/12 ,  C07D243/24 ,  C07D401/06 ,  C07D401/10 ,  C07D405/12

    CPC分类号： C07D401/06 ,  C07D223/12 ,  C07D243/24 ,  C07D401/10 ,  C07D405/12

    摘要： This invention relates to novel lactams having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.

    摘要翻译： 本发明涉及具有药物和生物影响性质的新型内酰胺，其药物组合物和使用方法。 这些新化合物抑制淀粉样蛋白前体蛋白的加工，更具体地，抑制Aβ肽的产生，从而起到防止淀粉样蛋白质神经沉积的形成的作用。 更具体地，本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病，例如阿尔茨海默病和唐氏综合征。

    Indole acetic acid acyl guanidines as beta-secretase inhibitors
    8.
    发明申请
    Indole acetic acid acyl guanidines as beta-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：US20070049589A1

    公开(公告)日：2007-03-01

    申请号：US11508481

    申请日：2006-08-23

    申请人： Lorin Thompson ,  Jianliang Shi ,  F. Zusi ,  Michael Dee ,  John Macor

    发明人： Lorin Thompson ,  Jianliang Shi ,  F. Zusi ,  Michael Dee ,  John Macor

    IPC分类号： A61K31/5377 ,  A61K31/496 ,  A61K31/4439 ,  A61K31/405 ,  C07D413/02 ,  C07D403/02 ,  C07D209/18

    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R 1，R 2，R 3，R 4，R 4， 如本文所定义的它们的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。

    Acyl guanidines as beta-secretase inhibitors
    9.
    发明申请
    Acyl guanidines as beta-secretase inhibitors 有权
    酰基胍作为β-分泌酶抑制剂

    公开(公告)号：US20070015754A1

    公开(公告)日：2007-01-18

    申请号：US11471125

    申请日：2006-06-20

    申请人： Samuel Gerritz ,  Andrew Good ,  Lorin Thompson ,  Weixu Zhai ,  Shuhao Shi ,  Shirong Zhu

    发明人： Samuel Gerritz ,  Andrew Good ,  Lorin Thompson ,  Weixu Zhai ,  Shuhao Shi ,  Shirong Zhu

    IPC分类号： A61K31/5377 ,  A61K31/55 ,  A61K31/425 ,  A61K31/42 ,  A61K31/416 ,  A61K31/4709

    CPC分类号： C07D275/03 ,  C07D231/14 ,  C07D261/18 ,  C07D413/12

    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 and R5 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R 1，R 2，R 3，R 4和R 4， 本文所定义的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。

    Novel gamma-lactams as beta-secretase inhibitors
    10.
    发明申请
    Novel gamma-lactams as beta-secretase inhibitors 有权
    新型γ-内酰胺酶作为β-分泌酶抑制剂

    公开(公告)号：US20060046984A1

    公开(公告)日：2006-03-02

    申请号：US11206441

    申请日：2005-08-18

    申请人： Lorin Thompson ,  Kenneth Boy ,  Jianliang Shi ,  John Macor

    发明人： Lorin Thompson ,  Kenneth Boy ,  Jianliang Shi ,  John Macor

    IPC分类号： A61K31/541 ,  A61K31/5377 ,  A61K31/4545 ,  A61K31/454 ,  C07D417/02 ,  C07D403/02 ,  C07D413/02

    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。