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53 条记录 (耗时 0.032 秒)

    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

    申请人： Helen Jane Bryant ,  Mark Stuart Chambers ,  Philip Jones ,  Angus Murray MacLeod ,  Robert James Maxey

    发明人： Helen Jane Bryant ,  Mark Stuart Chambers ,  Philip Jones ,  Angus Murray MacLeod ,  Robert James Maxey

    IPC分类号： A61K471/04 ,  A61K31/505 ,  C07D239/00 ,  C07D471/00 ,  C07D487/00

    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
    4.
    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

    申请人： Howard Barff Broughton ,  Helen Jane Bryant ,  Mark Stuart Chambers ,  Neil Roy Curtis

    发明人： Howard Barff Broughton ,  Helen Jane Bryant ,  Mark Stuart Chambers ,  Neil Roy Curtis

    IPC分类号： A61K31404

    CPC分类号： C07D401/04 ,  A61K31/40 ,  C07D209/08 ,  C07D401/14 ,  C07D403/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

    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。

    Substituted thienlycyclohexanone derivatives for enhancing cognition
    9.
    发明授权
    Substituted thienlycyclohexanone derivatives for enhancing cognition 失效

    公开(公告)号：US6156787A

    公开(公告)日：2000-12-05

    申请号：US296753

    申请日：1999-04-22

    申请人： Howard Barff Broughton ,  Mark Stuart Chambers

    发明人： Howard Barff Broughton ,  Mark Stuart Chambers

    IPC分类号： C07D333/72 ,  C07D417/12 ,  A61K31/38 ,  A61K31/40 ,  C07D333/56 ,  C07D405/00

    CPC分类号： C07D417/12 ,  C07D333/72

    摘要： The present invention provides compounds of formula (I) or pharmaceutically acceptable salts thereof: ##STR1## where A is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, arylC.sub.1-6 alkyl, aryl, S(O),R.sup.1, OR.sup.1 or NR.sup.1 R.sup.6 ;R.sup.1 is hydrogen; C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl or C.sub.3-6 cycloalkenyl each of which is optionally substituted by amino, C.sub.1-6 alkylamino, di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkoxy, C.sub.1-6 alkylaminocarbonyl, one, two or three hydroxy groups, one, two or three halogen atoms or a four, five or six-membered saturated heterocyclic ring containing a nitrogen atom and optionally either an oxygen atom or a further nitrogen atom which ring is optionally substituted by C.sub.1-4 alkyl on the further nitrogen atom; aryl, arylC.sub.1-6 alkyl, arylC.sub.2-6 alkenyl or arylC.sub.2-6 alkynyl optionally substituted on the aryl ring by halogen, nitro, cyano, C.sub.1-6 alkylcarbonylamino, hydroxy or C.sub.1-6 alkoxy; or a five-membered aromatic ring containing 1, 2, 3 or 4 heteroatoms chosen from O, N and S provided that not more than one heteroatom is other than N, or a six-membered aromatic ring containing 1, 2, 3 or 4 nitrogen atoms, each of which rings is optionally substituted by halogen, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, aryl, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl;R.sup.2 and R.sup.3 are independently hydrogen or C.sub.1-6 alkyl or together with the carbon atom to which they are attached form a C.sub.3-8 cycloalkyl group;R.sup.4 and R.sup.5 are individually hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl or C.sub.3-8 cycloalkyl or R.sup.12 and R.sup.13, together with the nitrogen atom to which they are attached, form a saturated 4 to 8 membered ring optionally containing an oxygen atom or a further nitrogen atom as a ring member, the further nitrogen atom being unsubstituted or substituted by C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl;R.sup.6 is hydrogen or C.sub.1-6 alkyl;p is zero, 1 or 2; andq is 0, 1 or 2;the preparation of these compounds, their use in enhancing cognition in disease states, particularly Alzheimer's disease, and methods of treatment using them.