Substituted 1,2,3-triazolo[1,5-a]quinazolines for enhancing cognition
    4.
    发明授权
    Substituted 1,2,3-triazolo[1,5-a]quinazolines for enhancing cognition 失效
    取代的1,2,3-三唑并[1,5-a]喹唑啉用于增强认知

    公开(公告)号:US07144887B2

    公开(公告)日:2006-12-05

    申请号:US10149852

    申请日:2000-12-11

    CPC分类号: C07D487/04

    摘要: The present invention provides a compound of formula (I) in which R1 is generally hydrogen or CF3, R2 is generally hydrogen, W is a cyclic amine, a heterocycle or a group L-Y—X where L-Y is a linking portion and X is generally an aromatic or non-aromatic heterocycle, alkyl or alkylcarbonyl and Z is generally a heterocycle such as 5-methylisoxazol-3-yl, and pharmaceutically acceptable salts thereof for enhancing cognition in conditions such as Alzheimer's Disease, pharmaceutical compositions comprising them, their use for manufacturing medicaments and methods of treatment using them

    摘要翻译: 本发明提供式(I)化合物,其中R 1通常是氢或CF 3,R 2通常是氢,W 是环状胺,杂环或LYX基团,其中LY是连接部分,X通常是芳族或非芳族杂环,烷基或烷基羰基,Z通常是杂环,例如5-甲基异恶唑-3-基和药学上 用于增强诸如阿尔茨海默氏病等疾病的认知的可接受的盐,包含它们的药物组合物,其用于制备药物的用途和使用它们的治疗方法

    Phenylindole derivatives as 5-HT2A receptor antagonists
    8.
    发明授权
    Phenylindole derivatives as 5-HT2A receptor antagonists 失效
    苯基吲哚衍生物作为5-HT2A受体拮抗剂

    公开(公告)号:US06316468B1

    公开(公告)日:2001-11-13

    申请号:US09486846

    申请日:2000-03-01

    IPC分类号: A61K31445

    CPC分类号: C07D401/04

    摘要: 3-(Piperidin-4-yl)-1H-indole derivatives bearing an optionally substituted phenyl moiety at the 2-position of the indole ring system and an alkyl or aryl-alkyl substituent on the nitrogen atom of the piperndine ring are selective antagonists of the human 5-HT2A receptor. They are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including psychotic disorders such as schizophrenia.

    摘要翻译: 在吲哚环系统的2-位上带有任选取代的苯基部分的3-(哌啶-4-基)-1H-吲哚衍生物和哌啶环的氮原子上的烷基或芳基 - 烷基取代基是选择性拮抗剂 因此它们可用作药剂,特别是用于治疗和/或预防中枢神经系统的不利条件,包括精神病性精神病如精神分裂症。

    Nitrogen substituted 1,2,4-triazolo[3,4-a]phthalazine derivatives for enhancing cognition
    10.
    发明授权
    Nitrogen substituted 1,2,4-triazolo[3,4-a]phthalazine derivatives for enhancing cognition 失效
    氮取代的1,2,4-三唑并[3,4-a]酞嗪衍生物用于增强认知

    公开(公告)号:US06900209B2

    公开(公告)日:2005-05-31

    申请号:US10432391

    申请日:2001-11-22

    CPC分类号: C07D487/04

    摘要: The present invention provides a compound of formula (I) wherein A is an optionally substituted C1-4alkylidene group or a bond, R20 and R21 are hydrogen, alkyl groups or heterocyclic groups, R1 and R2 are small substituents or hydrogen, L is O, S or substituted N, X is a 5- or 6-membered heteroaromatic ring, Y is C1-4alkylidene and Z is a 5- or 6-membered heteroaromatic ring; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in therapy; its use in making medicaments for treating neurodegenerative disease and methods of using it to enhance cognition.

    摘要翻译: 本发明提供式(I)的化合物,其中A是任选取代的C 1-4烷基或键,R 20和R 21, / SO 2是氢,烷基或杂环基,R 1和R 2是小取代基或氢,L是O,S或取代的N,X是5 - 或6-元杂芳环,Y是C 1-4 - 亚烷基,Z是5-或6-元杂芳环; 或其药学上可接受的盐; 包含它的药物组合物; 其用于治疗; 其用于制备用于治疗神经退行性疾病的药物和使用其增强认知的方法。