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111 条记录 (耗时 0.099 秒)

    ASPARTYL PROTEASE INHIBITORS
    62.
    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
    65.
    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。

    Aspartyl protease inhibitors
    67.
    发明申请
    Aspartyl protease inhibitors 有权
    天冬氨酰蛋白酶抑制剂

    公开(公告)号：US20060287294A1

    公开(公告)日：2006-12-21

    申请号：US11451195

    申请日：2006-06-12

    申请人： Zhaoning Zhu ,  Brian McKittrick ,  Andrew Stamford ,  Tao Guo ,  Thuy Le

    发明人： Zhaoning Zhu ,  Brian McKittrick ,  Andrew Stamford ,  Tao Guo ,  Thuy Le

    IPC分类号： A61K31/554 ,  A61K31/553 ,  A61K31/551 ,  C07D285/36 ,  C07D243/10 ,  C07D223/14

    CPC分类号： C07D471/10 ,  C07D239/70 ,  C07D487/10 ,  C07D491/10 ,  C07D495/10

    摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein U, W, A, R, R1, R2, R6a 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. 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合物，其中U，W，A，R，R 1，R 2， R 6a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。 还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱m 1激动剂或m 2 H 2拮抗剂组合治疗认知或神经变性疾病的方法。

    Gamma secretase modulators
    70.
    发明授权
    Gamma secretase modulators 有权

    公开(公告)号：US09598437B2

    公开(公告)日：2017-03-21

    申请号：US15101224

    申请日：2014-12-02

    申请人： Mihir B. Mandal ,  Zhaoning Zhu

    发明人： Mihir B. Mandal ,  Zhaoning Zhu

    IPC分类号： C07D498/04

    CPC分类号： C07D498/04

    摘要： Disclosed herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.