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111 条记录 (耗时 0.078 秒)

    Preparation and use of compounds as aspartyl protease inhibitors
    6.
    发明授权
    Preparation and use of compounds as aspartyl protease inhibitors 有权
    制备和使用化合物作为天冬氨酰蛋白酶抑制剂

    公开(公告)号：US08110682B2

    公开(公告)日：2012-02-07

    申请号：US11451262

    申请日：2006-06-12

    申请人： Brian McKittrick ,  Zhaoning Zhu ,  Andrew Stamford ,  Elizabeth M. Smith

    发明人： Brian McKittrick ,  Zhaoning Zhu ,  Andrew Stamford ,  Elizabeth M. Smith

    IPC分类号： C07D251/42 ,  C07D251/16 ,  C07D251/22 ,  A61K31/53 ,  A61P3/10

    CPC分类号： C07D251/72 ,  C07D239/70 ,  C07F9/6584

    摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein A is a bond, —C(O)—, or —C(R3′)(R4′)—; X is —N(R1)— or —C(R6)(R7)—; Y is —S(O)2—, —C(═O)—, —PO(OR9) or —C(R6′R7′)—; is a single or double bond and R, R1, R2, R3, R4, R3′, R4′, R5, R6, R6′, R7 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化物，其中A为键，-C（O） - 或-C（R3'）（R4'） - ; X是-N（R 1） - 或-C（R 6）（R 7） - ; Y是-S（O）2 - ， - C（= O） - ， - PO（OR 9）或-C（R 6'R 7'） - ; 是单键或双键，R，R1，R2，R3，R4，R3'，R4'，R5，R6，R6'，R7和R7'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。

    Bicyclic guanidine derivatives as asparyl protease inhibitors, compositions, and uses thereof
    8.
    发明授权
    Bicyclic guanidine derivatives as asparyl protease inhibitors, compositions, and uses thereof 有权
    作为芳香族蛋白酶抑制剂的双环胍衍生物，组合物及其用途

    公开(公告)号：US07759354B2

    公开(公告)日：2010-07-20

    申请号：US11451074

    申请日：2006-06-12

    申请人： Zhaoning Zhu ,  Brian McKittrick ,  Andrew Stamford ,  Ying Huang ,  Elizabeth M. Smith

    发明人： Zhaoning Zhu ,  Brian McKittrick ,  Andrew Stamford ,  Ying Huang ,  Elizabeth M. Smith

    IPC分类号： C07D273/06 ,  A61K31/551 ,  A61P31/18 ,  A61K31/553 ,  A61K31/519 ,  C07D243/04 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： The present application provides compounds of the Formula: and stereoisomers, tautomers, or pharmaceutically acceptable salts and solvates thereof, wherein U, W, R, R1, R2, R3 and R4 in each formula (when present) are as defined in the specification, and pharmaceutical compositions comprising such compounds. Also disclosed are methods of using such compounds and compositions to inhibit aspartyl protease, and to treat a variety of disease and indications including (but not limited) to cardiovascular disease and cognitive and neurodegenerative disease. The compounds of the present invention are disclosed for use alone or in combination with one or more additional active ingredients such as cholinesterase inhibitors and a muscarinic m1 agonist and/or m2 antagonists.

    摘要翻译： 本申请提供了式及其立体异构体，互变异构体或其药学上可接受的盐和溶剂合物的化合物，其中每个式（当存在时）中的U，W，R，R 1，R 2，R 3和R 4如说明书中所定义， 和包含这些化合物的药物组合物。 还公开了使用这些化合物和组合物来抑制天冬氨酰蛋白酶的方法，并且治疗多种疾病和适应症，包括（但不限于）心血管疾病和认知和神经变性疾病。 公开本发明的化合物单独使用或与一种或多种另外的活性成分如胆碱酯酶抑制剂和毒蕈碱m1激动剂和/或m2拮抗剂组合使用。

    Aspartyl protease inhibitors
    10.
    发明申请
    Aspartyl protease inhibitors 失效
    天冬氨酰蛋白酶抑制剂

    公开(公告)号：US20070099875A1

    公开(公告)日：2007-05-03

    申请号：US11589387

    申请日：2006-10-30

    申请人： Zhaoning Zhu ,  Andrew Stamford ,  Brian McKittrick

    发明人： Zhaoning Zhu ,  Andrew Stamford ,  Brian McKittrick

    IPC分类号： A61K31/66 ,  C07F9/28 ,  A61K31/554

    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 1，R 2，R 2，R 3， R 4，R 4，R 5，R 6和R 7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。