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    Piperazine thiazole derivatives useful in the treatment of tauopathies such as alzheimer's disease
    1.
    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。

    PIPERAZINE THIAZOLE DERIVATIVES USEFUL IN THE TREATMENT OF TAUOPATHIES SUCH AS ALZHEIMER'S DISEASE
    2.
    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。

    NOVEL COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
    5.
    发明申请
    NOVEL COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES 有权
    用于治疗神经损伤性疾病的新型化合物

    公开(公告)号：US20130289033A1

    公开(公告)日：2013-10-31

    申请号：US13993756

    申请日：2011-12-13

    申请人： Gerard Griffioen ,  Tom Van Dooren ,  Verónica Rojas De La Parra ,  Arnaud Marchand ,  Sara Alassia ,  Amuri Kilonda ,  Patrick Chaltin

    发明人： Gerard Griffioen ,  Tom Van Dooren ,  Verónica Rojas De La Parra ,  Arnaud Marchand ,  Sara Alassia ,  Amuri Kilonda ,  Patrick Chaltin

    IPC分类号： C07D209/18 ,  C07D409/12 ,  C07D401/12

    CPC分类号： C07D209/18 ,  C07D209/14 ,  C07D401/12 ,  C07D409/12 ,  C07D471/04

    摘要： This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1), wherein R1, R2, R4, R5, R6, E, n, Y1, Y2, Y3, Y4, Y5, B, R8, and m are as defined in the claims.

    摘要翻译： 本发明提供新的化合物和用作药物的新化合物，更特别是用于预防或治疗神经变性疾病，更具体地说是某些神经系统疾病，例如统称为tau蛋白病的病症，以及细胞毒性α-突触核蛋白淀粉样变性特征的病症 。 本发明还涉及所述新化合物在制备可用于治疗这种神经变性疾病的药物中的用途。 本发明还涉及包含所述新化合物的药物组合物和制备所述新化合物的方法。 化合物具有式（A1），其中R1，R2，R4，R5，R6，E，n，Y1，Y2，Y3，Y4，Y5，B，R8和m如权利要求中所定义。