Substituted 1,2,3-triazolo[1,5-a]quinazolines for enhancing cognition
    2.
    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

    Tetrahydroindolone derivatives as gabaaalpha5 ligands for enhancing cognition
    5.
    发明授权
    Tetrahydroindolone derivatives as gabaaalpha5 ligands for enhancing cognition 失效
    四氢吲哚酮衍生物作为增加认知的gabaaalpha5配体

    公开(公告)号:US06395766B1

    公开(公告)日:2002-05-28

    申请号:US09674740

    申请日:2000-11-06

    IPC分类号: A61K31404

    摘要: Compounds according to Formula (I) or a pharmaceutically acceptable salt thereof are GABA-A Alpha 5 ligands useful for enhancing cognition: where A is C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl, arylC1-6alkyl, or aryl wherein the aryl group is optionally substituted by halogen, C1-6alkyl, CF3, CN, NO2 or NH2, NR1R10, S(O)pR1, heteroarylC1-6alkyl or heteroaryl where heteroaryl is a 5- or 6-membered heteroaromatic ring as defined for B; and B is phenyl or a 5-membered ring having one or two unsaturations containing 1, 2, 3, or 4 heteroatoms chosen from O, N and S provided that not more than one heteroatom is other than N, a 6-membered heteroaromatic ring containing 1, 2, 3 or 4 nitrogen atoms, each of which rings is optionally substituted by one or more substituents.

    摘要翻译: 根据式(I)的化合物或其药学上可接受的盐是可用于增强认知的GABA-Aα5配体:其中A是C 1-6烷基,C 2-6烯基,C 2-6炔基,C 3-6环烷基,芳基C 1-6烷基或芳基 其中芳基任选被卤素,C 1-6烷基,CF 3,CN,NO 2或NH 2,NR 1 R 10,S(O)p R 1,杂芳基C 1-6烷基或杂芳基取代,其中杂芳基是5-或6-元杂芳环, B; 并且B是苯基或具有1或2个不饱和基团的5元环,其含有1,2,3或4个选自O,N和S的杂原子,条件是不超过一个杂原子不是N,6元杂芳环 含有1,2,3或4个氮原子,其中每个环任选被一个或多个取代基取代。