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    PIPERAZINE THIAZOLE DERIVATIVES USEFUL IN THE TREATMENT OF TAUOPATHIES SUCH AS ALZHEIMER'S DISEASE
    42.
    发明申请
    PIPERAZINE THIAZOLE DERIVATIVES USEFUL IN THE TREATMENT OF TAUOPATHIES SUCH AS ALZHEIMER'S DISEASE 有权
    用于治疗诸如阿尔茨海默病的TAUOPATHIES的哌嗪衍生物

    公开(公告)号：US20140206699A1

    公开(公告)日：2014-07-24

    申请号：US14238905

    申请日：2012-08-17

    申请人： Gerard Griffioen ,  Giuseppe Cecere ,  Matthias Nettekoven ,  Katrien Princen ,  Hasane Ratni ,  Mark Rogres-Evans ,  Walter Vifian

    发明人： Gerard Griffioen ,  Giuseppe Cecere ,  Matthias Nettekoven ,  Katrien Princen ,  Hasane Ratni ,  Mark Rogres-Evans ,  Walter Vifian

    IPC分类号： C07D285/08 ,  C07D417/14 ,  C07D417/04

    CPC分类号： A61K31/496 ,  C07D285/08 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

    摘要： The present invention relates to a compound of formula (IA), wherein G1 is lower alkyl; lower alkyl substituted by one or more halogens; cycloalkyl; tetrahydropyran-4-yl; phenethyl; phenethyl substituted by one or more halogens; phenoxymethyl; phenoxymethyl substituted by one or more halogens; benzyloxyethyl; benzyloxy-ethyl substituted by one or more halogens; or is —NR2R3; R2 is hydrogen or lower alkyl; R3 is lower alkyl; tetrahydropyran-4-yl; —CH2-cycloalkyl; or cycloalkyl optionally substituted by lower alkyl substituted by one or more halogens; or R2 and R3 form together with the N-atom to which they are attached a heterocycloalkyl group with 4 or 5 carbon atoms, which is optionally substituted by one or more substituents selected from halogen; or lower alkyl substituted by one or more halogens; X is —CH2— or —(CH2)2—; Ar is phenyl or pyridinyl; R4 is halogen; lower alkyl; lower alkyl substituted by one or more halogens; or lower alkoxy; n is 1 or 2; or to a pharmaceutically active salt thereof, to a stereoisomeric form, including an individual diastereoisomer or enantiomer of the compound of formula (IA) as well as to a racemic or non-racemic mixture thereof. The present invention also relates to the use of a compound of formula (IA) for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation.

    摘要翻译： 本发明涉及式（IA）化合物，其中G 1为低级烷基; 被一个或多个卤素取代的低级烷基; 环烷基 四氢吡喃-4-基; 苯乙基 被一个或多个卤素取代的苯乙基; 苯氧基甲基; 被一个或多个卤素取代的苯氧基甲基; 苄氧基乙基 由一个或多个卤素取代的苄氧基 - 乙基; 或为-NR2R3; R2是氢或低级烷基; R3为低级烷基; 四氢吡喃-4-基; -CH 2 - 环烷基 或任选被被一个或多个卤素取代的低级烷基取代的环烷基; 或者R 2和R 3与它们所连接的N-原子一起形成具有4或5个碳原子的杂环烷基，其任选被一个或多个选自卤素的取代基取代; 或被一个或多个卤素取代的低级烷基; X是-CH 2 - 或 - （CH 2）2 - ; Ar是苯基或吡啶基; R4是卤素; 低级烷基 被一个或多个卤素取代的低级烷基; 或低级烷氧基; n为1或2; 或其药物活性盐与立体异构体形式，包括式（IA）化合物的单独非对映异构体或对映异构体以及其外消旋或非外消旋混合物。 本发明还涉及式（IA）化合物用于治疗以细胞毒性TAU错误折叠和/或聚集为特征的某些神经变性疾病的用途。

    Methyl-pyrrolidine ether derivatives
    43.
    发明授权
    Methyl-pyrrolidine ether derivatives 有权
    甲基吡咯烷醚衍生物

    公开(公告)号：US08507535B2

    公开(公告)日：2013-08-13

    申请号：US13171507

    申请日：2011-06-29

    申请人： Matthias Nettekoven ,  Hasane Ratni ,  Walter Vifian

    发明人： Matthias Nettekoven ,  Hasane Ratni ,  Walter Vifian

    IPC分类号： A61K31/4439 ,  C07D401/14

    CPC分类号： C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14

    摘要： The invention relates to a compound of formula wherein A is defined herein or to pharmaceutically active salts, stereoisomeric forms, including individual diastereoisomers and enantiomers of the compound of formula I as well as racemic and non-racemic mixtures thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

    摘要翻译： 本发明涉及下式的化合物或其药学上可接受的盐或其盐，其中A定义为本文或其药学活性盐，立体异构体形式，包括式I化合物的单独非对映异构体和对映异构体以及其外消旋和非外消旋混合物。 本发明化合物是用于治疗抑郁症，疼痛，精神病，帕金森病，精神分裂症，焦虑和注意缺陷多动障碍（ADHD）的高潜力NK-3受体拮抗剂。

    Piperazine thiazole derivatives useful in the treatment of tauopathies such as alzheimer's disease
    45.
    发明授权
    Piperazine thiazole derivatives useful in the treatment of tauopathies such as alzheimer's disease 有权
    哌嗪噻唑衍生物可用于治疗tau病，如阿尔茨海默病

    公开(公告)号：US09187440B2

    公开(公告)日：2015-11-17

    申请号：US14238905

    申请日：2012-08-17

    申请人： Gerard Griffioen ,  Giuseppe Cecere ,  Matthias Nettekoven ,  Katrien Princen ,  Hasane Ratni ,  Mark Rogers-Evans ,  Walter Vifian

    发明人： Gerard Griffioen ,  Giuseppe Cecere ,  Matthias Nettekoven ,  Katrien Princen ,  Hasane Ratni ,  Mark Rogers-Evans ,  Walter Vifian

    IPC分类号： A61K31/496 ,  C07D285/08 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

    CPC分类号： A61K31/496 ,  C07D285/08 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

    摘要： The present invention relates to a compound of formula (IA), wherein G1 is lower alkyl; lower alkyl substituted by one or more halogens; cycloalkyl; tetrahydropyran-4-yl; phenethyl; phenethyl substituted by one or more halogens; phenoxymethyl; phenoxymethyl substituted by one or more halogens; benzyloxyethyl; benzyloxy-ethyl substituted by one or more halogens; or is —NR2R3; R2 is hydrogen or lower alkyl; R3 is lower alkyl; tetrahydropyran-4-yl; —CH2-cycloalkyl; or cycloalkyl optionally substituted by lower alkyl substituted by one or more halogens; or R2 and R3 form together with the N-atom to which they are attached a heterocycloalkyl group with 4 or 5 carbon atoms, which is optionally substituted by one or more substituents selected from halogen; or lower alkyl substituted by one or more halogens; X is —CH2—or —(CH2)2—; Ar is phenyl or pyridinyl; R4 is halogen; lower alkyl; lower alkyl substituted by one or more halogens; or lower alkoxy; n is 1 or 2; or to a pharmaceutically active salt thereof, to a stereoisomeric form, including an individual diastereoisomer or enantiomer of the compound of formula (IA) as well as to a racemic or non-racemic mixture thereof. The present invention also relates to the use of a compound of formula (IA) for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation.

    摘要翻译： 本发明涉及式（IA）化合物，其中G 1为低级烷基; 被一个或多个卤素取代的低级烷基; 环烷基 四氢吡喃-4-基; 苯乙基 被一个或多个卤素取代的苯乙基; 苯氧基甲基; 被一个或多个卤素取代的苯氧基甲基; 苄氧基乙基 由一个或多个卤素取代的苄氧基 - 乙基; 或为-NR2R3; R2是氢或低级烷基; R3是低级烷基; 四氢吡喃-4-基; -CH 2 - 环烷基 或任选被被一个或多个卤素取代的低级烷基取代的环烷基; 或者R 2和R 3与它们所连接的N-原子一起形成具有4或5个碳原子的杂环烷基，其任选被一个或多个选自卤素的取代基取代; 或被一个或多个卤素取代的低级烷基; X是-CH 2 - 或 - （CH 2）2 - ; Ar是苯基或吡啶基; R4是卤素; 低级烷基 被一个或多个卤素取代的低级烷基; 或低级烷氧基; n为1或2; 或其药物活性盐与立体异构体形式，包括式（IA）化合物的单独非对映异构体或对映异构体以及其外消旋或非外消旋混合物。 本发明还涉及式（IA）化合物用于治疗以细胞毒性TAU错误折叠和/或聚集为特征的某些神经变性疾病的用途。