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    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
    44.
    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。

    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：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。

    CYCLIC AMINE BACE-1 INHIBITORS HAVING A HETEROCYCLIC SUBSTITUENT
    47.
    发明申请
    CYCLIC AMINE BACE-1 INHIBITORS HAVING A HETEROCYCLIC SUBSTITUENT 有权
    具有杂环取代基的循环胺BACE-1抑制剂

    公开(公告)号：US20090312341A1

    公开(公告)日：2009-12-17

    申请号：US12490884

    申请日：2009-06-24

    申请人： Jared N. Cumming ,  Ying Huang ,  Guoqing Li ,  Ulrich Iserloh ,  Andrew Stamford ,  Corey Strickland ,  Johannes H. Voigt ,  Yusheng Wu ,  Jianping Pan ,  Tao Guo ,  Douglas W. Hobbs ,  Thuy X. H. Le ,  Jeffrey F. Lowrie

    发明人： Jared N. Cumming ,  Ying Huang ,  Guoqing Li ,  Ulrich Iserloh ,  Andrew Stamford ,  Corey Strickland ,  Johannes H. Voigt ,  Yusheng Wu ,  Jianping Pan ,  Tao Guo ,  Douglas W. Hobbs ,  Thuy X. H. Le ,  Jeffrey F. Lowrie

    IPC分类号： A61K31/496 ,  C12N9/99 ,  A61P25/28

    CPC分类号： C04B35/632 ,  C07D207/277 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

    摘要： Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is X is —O—, —C(R14)2— or —N(R)—; Z is —C(R14)2— or —N(R)—; t is 0, 1, 2 or 3; each R and R2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R14 is H, alkyl, alkenyl, alkynyl, halo, —CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, —OR35, —N(R24) (R25) or —SR35; R41 is alkyl, cycloalkyl, —SO2(alkyl), —C(O)-alkyl, —C(O)-cycloalkyl or -alkyl-NH—C(O)CH3; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula I.Also disclosed are pharmaceutical compositions and methods of treatment comprising compounds of formula I in combination with other agents useful in treating cognitive or neurodegenerative diseases.

    摘要翻译： 公开了下式的新化合物或其药学上可接受的盐或溶剂合物，其中R 1是X是-O - ， - C（R 14）2 - 或-N（R） - ; Z是-C（R 14）2 - 或-N（R） - ; t为0,1,2或3; 每个R和R 2独立地为H，烷基，环烷基，环烷基烷基，芳基，杂芳基，杂环烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，烯基或炔基; 每个R 14是H，烷基，烯基，炔基，卤素，-CN，卤代烷基，环烷基，环烷基烷基，芳基，杂芳基，杂环烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，-OR 35，-N（R 24）（R 25）或-SR 35; R41是烷基，环烷基，-SO2（烷基），-C（O） - 烷基，-C（O） - 环烷基或 - 烷基-NH-C（O）CH3; 其余变量如本说明书中所定义。 还公开了包含式I化合物的药物组合物和用式I化合物治疗认知障碍或神经变性疾病的方法。还公开了药物组合物和治疗方法，其包含式I化合物与用于治疗认知或神经变性的其它药剂 疾病

    Macrocyclic Heterocyclic Aspartyl Protease Inhibitors
    48.
    发明申请
    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：US20100063121A1

    公开(公告)日：2010-03-11

    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： A61K31/4188 ,  C07D487/08

    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。