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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
    PIPERAZINTHIAZOLDERIVATE阿尔茨海默病作为Tau蛋白病的治疗

    公开(公告)号：EP2744798B1

    公开(公告)日：2016-03-30

    申请号：EP12756402.9

    申请日：2012-08-17

    申请人： reMYND NV

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

    IPC分类号： C07D417/14 ,  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 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
    5.
    发明公开
    PIPERAZINE THIAZOLE DERIVATIVES USEFUL IN THE TREATMENT OF TAUOPATHIES SUCH AS ALZHEIMER'S DISEASE 有权
    PIPERAZINTHIAZOLDERIVATE阿尔茨海默病作为Tau蛋白病的治疗

    公开(公告)号：EP2744798A1

    公开(公告)日：2014-06-25

    申请号：EP12756402.9

    申请日：2012-08-17

    申请人： reMYND NV

    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 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.

    2,7-DIAZASPIRO[3.5]NONANE COMPOUNDS
    6.
    发明公开
    2,7-DIAZASPIRO[3.5]NONANE COMPOUNDS 有权
    2,7-二氮杂螺[3.5]壬烷VERBINDUNGEN

    公开(公告)号：EP3119782A1

    公开(公告)日：2017-01-25

    申请号：EP15710486.0

    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 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.

    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。