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111 条记录 (耗时 0.062 秒)

    Aspartyl protease inhibitors
    51.
    发明授权
    Aspartyl protease inhibitors 失效
    天冬氨酰蛋白酶抑制剂

    公开(公告)号：US07560451B2

    公开(公告)日：2009-07-14

    申请号：US11589387

    申请日：2006-10-30

    申请人： Zhaoning Zhu ,  Andrew W. Stamford ,  Brian McKittrick

    发明人： Zhaoning Zhu ,  Andrew W. Stamford ,  Brian McKittrick

    IPC分类号： C07D411/04 ,  A61K31/553

    CPC分类号： C07D413/04 ,  C07F9/65848

    摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W, R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes.Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.

    摘要翻译： 公开了式I化合物或其立体异构体，互变异构体或其药学上可接受的盐或溶剂合物，其中W，R 1，R 2，R 3，R 4，R 5，R 6和R 7如说明书中所定义; 以及包含式I化合物的药物组合物。还公开了抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经变性疾病的方法以及抑制人类免疫缺陷病毒，plasmepins，组织蛋白酶D 和原生动物酶。 还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱拮抗剂组合来治疗认知或神经变性疾病的方法。

    HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS
    55.
    发明申请
    HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS 有权
    异源ASPARTYL蛋白酶抑制剂

    公开(公告)号：US20110280867A1

    公开(公告)日：2011-11-17

    申请号：US13191978

    申请日：2011-07-27

    申请人： Zhaoning Zhu ,  Andrew W. Stamford ,  Brian McKittrick

    发明人： Zhaoning Zhu ,  Andrew W. Stamford ,  Brian McKittrick

    IPC分类号： A61K39/395 ,  A61K31/55 ,  C07D409/04 ,  A61P25/28 ,  A61P25/00 ,  A61P9/00 ,  C07D498/04 ,  A61K31/5517 ,  C07D487/04

    CPC分类号： C07D409/04 ,  C07D487/04

    摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

    摘要翻译： 公开了式I化合物或其立体异构体，互变异构体或其药学上可接受的盐或溶剂化物，其中Ar，R 1，R 2，R 3，R 4和R 5如说明书中所定义; 以及包含式I化合物的药物组合物。还公开了抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经变性疾病的方法。 还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱m1激动剂或m2拮抗剂组合治疗认知或神经变性疾病的方法。

    Heterocyclic aspartyl protease inhibitors
    56.
    发明授权
    Heterocyclic aspartyl protease inhibitors 有权
    杂环天门冬氨酰蛋白酶抑制剂

    公开(公告)号：US08012960B2

    公开(公告)日：2011-09-06

    申请号：US12794858

    申请日：2010-06-07

    申请人： Zhaoning Zhu ,  Andrew W. Stamford ,  Brian McKittrick

    发明人： Zhaoning Zhu ,  Andrew W. Stamford ,  Brian McKittrick

    IPC分类号： C07D487/04 ,  C07D498/04 ,  A61K31/18

    CPC分类号： C07D409/04 ,  C07D487/04

    摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

    摘要翻译： 公开了式I化合物或其立体异构体，互变异构体或其药学上可接受的盐或溶剂化物，其中Ar，R 1，R 2，R 3，R 4和R 5如说明书中所定义; 以及包含式I化合物的药物组合物。还公开了抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经变性疾病的方法。 还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱m1激动剂或m2拮抗剂组合治疗认知或神经变性疾病的方法。

    THIOPHENYL-SUBSTITUTED 2-IMINO-3-METHYL PYRROLO PYRIMIDINONE COMPOUNDS AS BACE-1 INHIBITORS, COMPOSITIONS, AND THEIR USE
    57.
    发明申请
    THIOPHENYL-SUBSTITUTED 2-IMINO-3-METHYL PYRROLO PYRIMIDINONE COMPOUNDS AS BACE-1 INHIBITORS, COMPOSITIONS, AND THEIR USE 有权
    作为BACE-1抑制剂，组合物及其使用的噻吩基取代的2-亚氨基-3-甲基吡咯烷酮吡啶酮化合物

    公开(公告)号：US20110110927A1

    公开(公告)日：2011-05-12

    申请号：US12988464

    申请日：2009-04-21

    申请人： Andrew W. Stamford ,  Zhaoning Zhu ,  Mihirbaran Mandal ,  Xiaoxiang Liu

    发明人： Andrew W. Stamford ,  Zhaoning Zhu ,  Mihirbaran Mandal ,  Xiaoxiang Liu

    IPC分类号： A61K39/395 ,  C07D471/04 ,  A61K31/519 ,  A61P25/28 ,  A61P25/00

    CPC分类号： C07D487/04

    摘要： In its many embodiments, the present invention provides provides certain thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidone compounds, including compounds (or tautomers or a pharmaceutically acceptable salts thereof) having the structural Formula (III): wherein R2, R3, R4, R5, R6, R7, R8, and R9 are each selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds, and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimer's Disease, are also disclosed.

    摘要翻译： 在其许多实施方案中，本发明提供某些噻吩基取代的2-亚氨基-3-甲基吡咯并嘧啶酮化合物，包括具有结构式（III）的化合物（或其互变异构体或其药学上可接受的盐）：其中R2，R3， R 4，R 5，R 6，R 7，R 8和R 9各自独立地如本文所定义。 还公开了包含一种或多种这样的化合物的药物组合物，及其制备和用于治疗与淀粉样蛋白β（A＆bgr））蛋白质（包括阿尔茨海默氏病）相关的病理学的方法。

    ASPARTYL PROTEASE INHIBITORS
    58.
    发明申请
    ASPARTYL PROTEASE INHIBITORS 有权
    ASPARTYL PROTEASE抑制剂

    公开(公告)号：US20100069406A1

    公开(公告)日：2010-03-18

    申请号：US12517744

    申请日：2007-12-10

    申请人： Zhaoning Zhu ,  Andrew Stamford ,  Mihirbaran Mandal ,  Xiaoxiang Liu

    发明人： Zhaoning Zhu ,  Andrew Stamford ,  Mihirbaran Mandal ,  Xiaoxiang Liu

    IPC分类号： A61K31/5025 ,  C07D471/22 ,  A61P25/28

    CPC分类号： C07D471/14 ,  C07D239/95

    摘要： Disclosed are compounds of formula I (Chemical formula should be inserted here as it appears on abstract in paper form) Formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4, R14, V, W, X, Y, Z, p, and ring A are as described in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

    摘要翻译： 公开了式I的化合物（化学式应该在此插入，如其以纸的形式呈现）式I或其立体异构体，互变异构体或其药学上可接受的盐或溶剂化物，其中R1，R2，R3，R4，R14，V ，W，X，Y，Z，p和环A如说明书中所述。 还公开了抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经变性疾病的方法。 还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱m1激动剂或m2拮抗剂组合治疗认知或神经变性疾病的方法。

    Preparation and use of compounds as protease inhibitors
    60.
    发明申请
    Preparation and use of compounds as protease inhibitors 审中-公开
    化合物作为蛋白酶抑制剂的制备和使用

    公开(公告)号：US20080113957A1

    公开(公告)日：2008-05-15

    申请号：US11451194

    申请日：2006-06-12

    申请人： Brian McKittrick ,  Zhaoning Zhu ,  Andrew Stamford

    发明人： Brian McKittrick ,  Zhaoning Zhu ,  Andrew Stamford

    IPC分类号： A61K31/397 ,  C07D471/02

    CPC分类号： C07D487/04 ,  C07D205/06

    摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein, X is —C(R3R4)—; Y is —N(R5)—; Z is (—C(═N—R5′)—; and R1, R2, R3, and R4 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes.Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.

    摘要翻译： 公开了式I化合物或其立体异构体，互变异构体或其药学上可接受的盐或溶剂合物，其中X是-C（R 3）R 4） - 。 Y是-N（R 5） - ; Z是（-C（-NR 5） - ），R 1，R 2，R 3， 和R 4如本说明书中所定义;以及包含式I化合物的药物组合物。还公开了抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知功能的方法 和神经变性疾病，以及抑制人类免疫缺陷病毒，plasmepins，组织蛋白酶D和原生动物酶的方法。还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱拮抗剂组合治疗认知或神经变性疾病的方法。