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    COMPOUNDS FOR THE TREATMENT OF AMYLOID-ASSOCIATED DISEASES
    1.
    发明申请
    COMPOUNDS FOR THE TREATMENT OF AMYLOID-ASSOCIATED DISEASES 审中-公开
    用于治疗淀粉样相关性疾病的化合物

    公开(公告)号：WO2016083490A1

    公开(公告)日：2016-06-02

    申请号：PCT/EP2015/077731

    申请日：2015-11-26

    申请人： REMYND NV

    发明人： ROBIN, Maxime ,  CASANO, Gilles ,  ABEL, Sébastien ,  GRIFFIOEN, Gerard ,  PRINCEN, Katrien ,  ROJAS DE LA PARRA, Veronica

    IPC分类号： C07D471/04 ,  C07D493/04 ,  C07D498/04 ,  C07D513/04 ,  C07D513/14 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61K31/429 ,  A61K31/519 ,  A61K31/5365 ,  A61K31/424 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/4188

    CPC分类号： C07D513/04 ,  C07D471/04 ,  C07D493/04 ,  C07D498/04 ,  C07D513/14

    摘要： This invention provides novel compounds of formulae (I) or (II) or a stereoisomer, enantiomer, racemic, or tautomer thereof, (I) (II) wherein the substituents are as defined in the specification. The present invention also relates to the novel compounds for use as a medicine, more in particular for the prevention or treatment of amyloid-related diseases, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, disorders characterized 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 amyloid-related diseases. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.

    摘要翻译： 本发明提供新的式（I）或（II）化合物或其立体异构体，对映体，外消旋或互变异构体，（I）（II），其中取代基如说明书中所定义。 本发明还涉及用作药物的新化合物，特别是用于预防或治疗淀粉样蛋白相关疾病，更具体地，某些神经系统疾病，例如统称为tau蛋白病的病症，以细胞毒性α-突触核蛋白为特征的疾病 淀粉蛋白。 本发明还涉及所述新化合物在制备可用于治疗这种淀粉样蛋白相关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用于制备所述新化合物的方法。

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

    公开(公告)号：WO2015140132A1

    公开(公告)日：2015-09-24

    申请号：PCT/EP2015/055494

    申请日：2015-03-17

    申请人： REMYND NV

    发明人： GRIFFIOEN, Gerard ,  DE TAEYE, Bart ,  PRINCEN, Katrien ,  DE WITTE, Koen ,  BLANCHE, Emilie ,  RATNI, Hasane ,  ROGERS-EVANS, Mark

    IPC分类号： C07D471/10 ,  A61P3/10 ,  A61K31/438

    CPC分类号： A61K31/5377 ,  A61K31/435 ,  A61K31/444 ,  C07D471/10

    摘要： The present invention relates to a compound of formula (I) or a stereoisomer, enantiomer, racemic, or tautomer thereof, Formula (I), wherein R 1 , R 3 , R 4 , L 1 , L 2 , L 3 , L 4 , 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.

    摘要翻译： 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具有相同的 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
    3.
    发明申请
    PIPERAZINE THIAZOLE DERIVATIVES USEFUL IN THE TREATMENT OF TAUOPATHIES SUCH AS ALZHEIMER'S DISEASE 审中-公开
    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：WO2013024168A1

    公开(公告)日：2013-02-21

    申请号：PCT/EP2012/066136

    申请日：2012-08-17

    申请人： REMYND NV ,  GRIFFIOEN, Gerard ,  CECERE, Giuseppe ,  NETTEKOVEN, Matthias ,  PRINCEN, Katrien ,  RATNI, Hasane ,  ROGERS-EVANS, Mark ,  VIFIAN, Walter

    发明人： GRIFFIOEN, Gerard ,  CECERE, Giuseppe ,  NETTEKOVEN, Matthias ,  PRINCEN, Katrien ,  RATNI, Hasane ,  ROGERS-EVANS, Mark ,  VIFIAN, Walter

    IPC分类号： C07D285/08 ,  C07D417/04 ,  C07D417/12 ,  A61K31/433 ,  A61P25/28

    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 G 1 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 -NR 2 R 3 ; R 2 is hydrogen or lower alkyl; R 3 is lower alkyl; tetrahydropyran-4-yl; -CH 2 -cycloalkyl; or cycloalkyl optionally substituted by lower alkyl substituted by one or more halogens; or R 2 and R 3 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 -CH 2 - or -(CH 2 ) 2 -; Ar is phenyl or pyridinyl; R 4 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; 被一个或多个卤素取代的苯乙基; 苯氧基; 被一个或多个卤素取代的苯氧基甲基; 苄氧; 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。

    A YEAST MODEL FOR AMYLOIDOGENIC PROTEIN TOXICITY
    9.
    发明申请
    A YEAST MODEL FOR AMYLOIDOGENIC PROTEIN TOXICITY 审中-公开
    用于蛋白质蛋白毒性的YEAST模型

    公开(公告)号：WO2005005640A1

    公开(公告)日：2005-01-20

    申请号：PCT/BE2004/000102

    申请日：2004-07-09

    申请人： reMYND NV ,  GRIFFIOEN, Gerard ,  DUHAMEL, Hein ,  VAN DAMME, Nele ,  WINDERICKX, Joris ,  WERA, Stefaan

    发明人： GRIFFIOEN, Gerard ,  DUHAMEL, Hein ,  VAN DAMME, Nele ,  WINDERICKX, Joris ,  WERA, Stefaan

    IPC分类号： C12N15/81

    CPC分类号： C12N15/81 ,  C07K14/395

    摘要： The present invention relates to an engineered yeast strain, comprising a transgene encoding one or more amyloidogenic proteins or mutant(s) thereof, characterised in that it lacks one or more functional genes responsive to oxidative stress. The invention further relates to the use of this yeast strain for pharmaceutical screening, for modelling of neurodegenerative diseases and for cellular modelling of biochemistry of the amyloidogenic proteins involved therein.

    摘要翻译： 本发明涉及工程改造的酵母菌株，其包含编码一种或多种淀粉样蛋白形成蛋白质或其突变体的转基因，其特征在于其缺少一种或多种对氧化应激有响应的功能基因。 本发明还涉及这种酵母菌株用于药物筛选，神经变性疾病的建模和涉及其中的淀粉样蛋白形成蛋白的生物化学的细胞建模的用途。