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    2,7-DIAZASPIRO[3.5]NONANE COMPOUNDS
    2.
    发明申请
    2,7-DIAZASPIRO[3.5]NONANE COMPOUNDS 有权
    2,7-DIAZASPIRO [3.5] NONANE化合物

    公开(公告)号：US20170015665A1

    公开(公告)日：2017-01-19

    申请号：US15121790

    申请日：2015-03-17

    Applicant: REMYND NV

    Inventor： Gerard Griffioen ,  Bart De Taeye ,  Katrien Princen ,  Koen De Witte ,  Emilie Blanche ,  Hasane Ratni ,  Mark Rogers-Evans

    IPC: C07D471/10

    CPC classification number: A61K31/5377 ,  A61K31/435 ,  A61K31/444 ,  C07D471/10

    Abstract: The present invention relates to a compound of formula (I) or a stereoisomer, enantiomer, racemic, or tautomer thereof, Formula (I), wherein R1, R3, R4, L1, L2, L3, L4, and n, have the same meaning as that defined in the claims and the description. The present invention also relates to compositions, in particular pharmaceuticals, comprising such compounds, and to uses of such compounds and compositions for the prevention and/or treatment of metabolic disorders and/or neurodegenerative diseases, and/or protein misfolding disorders.

    Abstract translation: 本发明涉及式（I）化合物或式（I）的立体异构体，对映异构体，外消旋或互变异构体，其中R1，R3，R4，L1，L2，L3，L4和n具有相同 意义如权利要求和说明书中所限定的那样。 本发明还涉及包含这些化合物的组合物，特别是药物，以及这些化合物和组合物用于预防和/或治疗代谢紊乱和/或神经变性疾病和/或蛋白质错误折叠障碍的用途。

    Piperazine thiazole derivatives useful in the treatment of tauopathies such as Alzheimer's disease
    4.
    发明授权
    Piperazine thiazole derivatives useful in the treatment of tauopathies such as Alzheimer's disease 有权

    公开(公告)号：US09808456B2

    公开(公告)日：2017-11-07

    申请号：US14884689

    申请日：2015-10-15

    Applicant: REMYND NV

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

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

    CPC classification number: A61K31/496 ,  C07D285/08 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

    Abstract: 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.

    PIPERAZINE THIAZOLE DERIVATIVES USEFUL IN THE TREATMENT OF TAUOPATHIES SUCH AS ALZHEIMER'S DISEASE
    6.
    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：US20160101102A1

    公开(公告)日：2016-04-14

    申请号：US14884689

    申请日：2015-10-15

    Applicant: REMYND NV

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

    IPC: A61K31/496

    CPC classification number: A61K31/496 ,  C07D285/08 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

    Abstract: 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.

    Abstract translation: 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。

    OXADIAZOLE COMPOUNDS
    8.
    发明申请
    OXADIAZOLE COMPOUNDS 审中-公开
    奥沙利多化合物

    公开(公告)号：US20170073319A1

    公开(公告)日：2017-03-16

    申请号：US15122959

    申请日：2015-03-17

    Applicant: REMYND NV

    Inventor： Gerard GRIFFIOEN ,  Bart DE TAEYE ,  Katrien PRINCEN ,  Koen DE WITTE ,  Emilie BLANCHE ,  Hasane RATNI ,  Matthias NETTEKOVEN ,  Mark ROGERS-EVANS

    IPC: C07D271/07 ,  C07D471/10 ,  C07D413/12

    Abstract: The present invention relates to a compound of formula (I) or (II) or a stereoisomer, enantiomer, racemic, or tautomer thereof, (I) (II) wherein R1, R2, R3, L1, L2, L3, L4, L5 and n, have the same meaning as that defined in the claims and the description. The present invention also relates to compositions, in particular pharmaceuticals, comprising such compounds, and to uses of such compounds and compositions for the prevention and/or treatment of metabolic disorders and/or neurodegenerative diseases, and/or protein misfolding disorders.

    Abstract translation: 本发明涉及式（I）或（II）化合物或其立体异构体，对映异构体，外消旋或互变异构体，（I）（II）其中R1，R2，R3，L1，L2，L3，L4，L5 和n具有与权利要求和说明书中所定义的相同的含义。 本发明还涉及包含这些化合物的组合物，特别是药物，以及这些化合物和组合物用于预防和/或治疗代谢紊乱和/或神经变性疾病和/或蛋白质错误折叠障碍的用途。

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