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118 条记录 (耗时 0.071 秒)

    Aspartyl protease inhibitors
    41.
    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。

    Neuropeptide receptor modulators
    43.
    发明申请
    Neuropeptide receptor modulators 失效
    神经肽受体调节剂

    公开(公告)号：US20060089351A1

    公开(公告)日：2006-04-27

    申请号：US11117584

    申请日：2005-04-28

    申请人： Zhaoning Zhu ,  Zhong-Yue Sun ,  Yuanzan Ye ,  Deborra Mullins ,  Brian McKitrtick ,  Andrew Stamford ,  William Greenlee

    发明人： Zhaoning Zhu ,  Zhong-Yue Sun ,  Yuanzan Ye ,  Deborra Mullins ,  Brian McKitrtick ,  Andrew Stamford ,  William Greenlee

    IPC分类号： A61K31/541 ,  A61K31/4709 ,  A61K31/506 ,  A61K31/4439 ,  A61K31/427 ,  C07D417/02

    CPC分类号： C07D487/04 ,  C07D417/12 ,  C07D513/04

    摘要： The present invention discloses compounds, which are novel receptor antagonists for NPY Y1 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y1 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes. The compounds are represented by the structural Formula 1, a prodrug thereof, or any pharmaceutically acceptable salt, solvate, isomer or racemic mixture of the compound or said prodrug wherein R1 is heteroaryl, N-arylaminocarbonyl, N-heteroarylaminocarbonyl, benzimidazolyl or benzothiazolyl; R15 is present or not and if present is H, aryl, alkyl, arylalky or heteroarylalkyl; A is aryl, heteroaryl, cycloalkyl, cycloalkylidene, heterocycloalkylidene or heterocycloalkyl wherein said aryl, heteroaryl, cycloalkyl, cycloalkylidene, heterocycloalkylidene and heterocycloalkyl moieties may be substituted or unsubstituted; and B, L, X and R18 are defined herein.

    摘要翻译： 本发明公开了作为NPY Y1的新受体拮抗剂的化合物以及这些化合物的制备方法。 在另一个实施方案中，本发明公开了包含这种NPY Y1受体拮抗剂的药物组合物以及使用它们治疗肥胖，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。 化合物由结构式1表示，其前体药物或化合物或所述前体药物的任何药学上可接受的盐，溶剂合物，异构体或外消旋混合物，其中R 1是杂芳基，N-芳基氨基羰基，N - 杂芳基氨基羰基，苯并咪唑基或苯并噻唑基; R 15存在或不存在，如果存在，则为H，芳基，烷基，芳基烷基或杂芳基烷基; A是芳基，杂芳基，环烷基，环烷叉基，杂环亚烷基或杂环烷基，其中所述芳基，杂芳基，环烷基，亚环烷基，杂环亚烷基和杂环烷基部分可以是取代或未取代的; 和B，L，X和R 18在本文中定义。

    Macrocyclic heterocyclic aspartyl protease inhibitors
    45.
    发明授权
    Macrocyclic heterocyclic aspartyl protease inhibitors 有权
    大环杂环天门冬酰胺蛋白酶抑制剂

    公开(公告)号：US08557798B2

    公开(公告)日：2013-10-15

    申请号：US12620291

    申请日：2009-11-17

    申请人： Ulrich Iserloh ,  Zhaoning Zhu ,  Andrew Stamford ,  Johannes H. Voigt

    发明人： Ulrich Iserloh ,  Zhaoning Zhu ,  Andrew Stamford ,  Johannes H. Voigt

    IPC分类号： A61K31/33 ,  C07D245/00

    CPC分类号： C07D487/08

    摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt, solvate or ester thereof, wherein U, W, X, L, Y, M, Z, c, d, e, f, g, h, s, t, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and R18 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，溶剂化物或酯，其中U，W，X，L，Y，M，Z，c，d，e，f，g， s，t，R1，R2，R7，R8，R9，R10，R11，R12，R13，R14，R15，R16，R17和R18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
    46.
    发明授权
    Thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use 有权
    噻吩基取代的2-亚氨基-3-甲基吡咯并嘧啶酮化合物作为BACE-1抑制剂，组合物及其用途

    公开(公告)号：US08450331B2

    公开(公告)日：2013-05-28

    申请号：US12988464

    申请日：2009-04-21

    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： C07D487/04 ,  A61K31/519 ,  A61P25/28 ,  A61P3/10

    CPC分类号： C07D487/04

    摘要： In its many embodiments, the present invention 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，本发明提供了具有结构式（III）的化合物（或其互变异构体或其药学上可接受的盐）的某些噻吩基取代的2-亚氨基-3-甲基吡咯烷酮化合物：其中R2，R3，R4 ，R 5，R 6，R 7，R 8和R 9各自独立地并如本文所定义。 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包括阿尔茨海默病在内的淀粉样蛋白β（Abeta）蛋白相关的病理学的方法。

    Macrocyclic heterocyclic aspartyl protease inhibitors
    48.
    发明授权
    Macrocyclic heterocyclic aspartyl protease inhibitors 有权
    大环杂环天门冬酰胺蛋白酶抑制剂

    公开(公告)号：US07812013B2

    公开(公告)日：2010-10-12

    申请号：US11451064

    申请日：2006-06-12

    申请人： Ulrich Iserloh ,  Zhaoning Zhu ,  Andrew Stamford ,  Johannes H. Voigt

    发明人： Ulrich Iserloh ,  Zhaoning Zhu ,  Andrew Stamford ,  Johannes H. Voigt

    IPC分类号： A01N43/00 ,  A61K31/33 ,  C07D498/00

    CPC分类号： C07D487/08

    摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt, solvate or ester thereof, wherein U, W, X, L, Y, M, Z, c, d, e, f, g, h, s, t, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and R18 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，溶剂化物或酯，其中U，W，X，L，Y，M，Z，c，d，e，f，g， s，t，R1，R2，R7，R8，R9，R10，R11，R12，R13，R14，R15，R16，R17和R18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。

    DIARYL MORPHOLINES AS CB1 MODULATORS
    49.
    发明申请
    DIARYL MORPHOLINES AS CB1 MODULATORS 审中-公开
    二元醇作为CB1调节剂

    公开(公告)号：US20100197564A1

    公开(公告)日：2010-08-05

    申请号：US12593777

    申请日：2008-04-17

    申请人： Jack D. Scott ,  Andrew Stamford

    发明人： Jack D. Scott ,  Andrew Stamford

    IPC分类号： A61K31/5355 ,  C07D265/30 ,  A61K31/5375 ,  C07D413/12 ,  A61K38/28 ,  A61K31/397 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P25/00 ,  A61P29/00 ,  A61P1/00 ,  A61P9/00

    CPC分类号： C07D265/30 ,  C07D265/32 ,  C07D413/12

    摘要： The present invention provides compounds having the general structure of Formula (I) or a pharmaceutically acceptable salt, solvate, ester or prodrug thereof, which are useful as CB1 receptor antagonists. The compounds of the invention may be useful in treating diseases, disorders, or conditions responsive to CB1 receptor antagonists, including, but not limited to, metabolic syndrome, obesity, waist circumference, dyslipidemia, insulin sensitivity, neuroinflammatory disorders, cognitive disorders, psychosis, addictive behavior, gastrointestinal disorders, and cardiovascular conditions.

    摘要翻译： 本发明提供具有式（I）的通式结构的化合物或其药学上可接受的盐，溶剂合物，酯或前药，其可用作CB1受体拮抗剂。 本发明的化合物可用于治疗对CB1受体拮抗剂反应的疾病，病症或病症，包括但不限于代谢综合征，肥胖症，腰围，血脂异常，胰岛素敏感性，神经炎症性疾病，认知障碍，精神病， 成瘾行为，胃肠道疾病和心血管疾病。

    Substituted spiro iminopyrimidinones as aspartyl protease inhibitors, compositions, and methods of treatment
    50.
    发明授权
    Substituted spiro iminopyrimidinones as aspartyl protease inhibitors, compositions, and methods of treatment 有权
    取代的螺亚氨基嘧啶酮作为天冬氨酰蛋白酶抑制剂，组合物和治疗方法

    公开(公告)号：US07759353B2

    公开(公告)日：2010-07-20

    申请号：US11451195

    申请日：2006-06-12

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

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

    IPC分类号： C07D239/22 ,  A61K31/527 ,  A61P9/00 ,  A61P25/00 ,  A61P25/28

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

    摘要： Disclosed are certain substituted spiro iminopyrimidinones and other 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 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： 公开了某些取代的螺亚氨基嘧啶酮和其它式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U，W，A，R，R 1，R 2，R 6a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。还公开了使用这些化合物和组合物来抑制天冬氨酰蛋白酶的方法，以及治疗多种疾病和适应证，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。