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118 条记录 (耗时 0.084 秒)

    Cyclic amine bace-1 inhibitors having a heterocyclic substituent
    73.
    发明授权
    Cyclic amine bace-1 inhibitors having a heterocyclic substituent 有权
    具有杂环取代基的环胺类bace-1抑制剂

    公开(公告)号：US07910590B2

    公开(公告)日：2011-03-22

    申请号：US12490884

    申请日：2009-06-24

    申请人： Ying Huang ,  Guoqing Li ,  Ulrich Iserloh ,  Andrew Stamford ,  Corey Strickland ,  Johannes H. Voigt ,  Jianping Pan

    发明人： Ying Huang ,  Guoqing Li ,  Ulrich Iserloh ,  Andrew Stamford ,  Corey Strickland ,  Johannes H. Voigt ,  Jianping Pan

    IPC分类号： A61K31/496 ,  A61K31/506

    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(R 14)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 beta-secretase inhibitors
    78.
    发明申请
    Macrocyclic beta-secretase inhibitors 有权
    大环β-分泌酶抑制剂

    公开(公告)号：US20060040948A1

    公开(公告)日：2006-02-23

    申请号：US11189346

    申请日：2005-07-26

    申请人： Andrew Stamford ,  Ying Huang ,  Guoqing Li ,  Corey Strickand ,  Johannes Voigt

    发明人： Andrew Stamford ,  Ying Huang ,  Guoqing Li ,  Corey Strickand ,  Johannes Voigt

    IPC分类号： A61K31/496 ,  C07D491/14

    CPC分类号： C07D498/04 ,  C07D413/06

    摘要： Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, n and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of β-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.

    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化物，其中R 1，R 2，R 3，n和X 如说明书中所定义。 还公开了包含式I化合物的药物组合物。还公开了治疗认知或神经变性疾病如阿尔茨海默病的方法。 还公开了治疗认知或神经变性疾病的方法，其包括向需要这种治疗的患者施用至少一种式I化合物和至少一种选自β-分泌酶抑制剂的化合物的组合，所述β-分泌酶抑制剂除 式I，HMG-CoA还原酶抑制剂，γ-分泌酶抑制剂，非甾体抗炎剂，N-甲基-D-天冬氨酸受体拮抗剂，胆碱酯酶抑制剂和抗淀粉样蛋白抗体。

    Pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
    80.
    发明申请
    Pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists 有权
    吡唑并[4,3-e] -1,2,4-三唑并 - [1,5-c] - 嘧啶腺苷A2a受体拮抗剂

    公开(公告)号：US20050239795A1

    公开(公告)日：2005-10-27

    申请号：US11108916

    申请日：2005-04-19

    申请人： Bernard Neustadt ,  Jinsong Hao ,  Hong Liu ,  Craig Boyle ,  Samuel Chackalamannil ,  Unmesh Shah ,  Andrew Stamford ,  Joel Harris

    发明人： Bernard Neustadt ,  Jinsong Hao ,  Hong Liu ,  Craig Boyle ,  Samuel Chackalamannil ,  Unmesh Shah ,  Andrew Stamford ,  Joel Harris

    IPC分类号： A61K31/519 ,  C07D487/14

    CPC分类号： C07D487/14

    摘要： Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, furanyl, thienyl, pyridyl, pyridyl N-oxide, oxazolyl or pyrrolyl, or cycloalkenyl R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; and Z is optionally substituted aryl or heteroaryl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.

    摘要翻译： 具有结构式I的化合物或其药学上可接受的盐，其中R是任选取代的苯基，呋喃基，噻吩基，吡啶基，吡啶基N-氧化物，恶唑基或吡咯基，或环烯基R 1， R 3，R 3，R 4和R 5是H，烷基或烷氧基烷基; 和Z是任选取代的芳基或杂芳基。 还公开了式I化合物在治疗中枢神经系统疾病，特别是帕金森病中单独使用或与用于治疗帕金森病的其它药物组合的用途，以及包含它们的药物组合物的用途。