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    2-PHENYL OR 2-HETARYL IMIDAZOL[1,2-a]PYRIDINE DERIVATIVES
    1.
    发明公开
    2-PHENYL OR 2-HETARYL IMIDAZOL[1,2-a]PYRIDINE DERIVATIVES 有权
    2-苯基-2-甲基咪唑并[1,2-A]吡啶衍生物

    公开(公告)号：EP2991983A1

    公开(公告)日：2016-03-09

    申请号：EP14719326.2

    申请日：2014-04-25

    申请人： F.Hoffmann-La Roche AG

    发明人： BORRONI, Edilio ,  GOBBI, Luca ,  HONER, Michael ,  KNUST, Henner ,  KOERNER, Matthias ,  MURI, Dieter

    IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P9/00

    CPC分类号： C07D471/04 ,  A61K49/0002

    摘要： The invention relates to compounds of formulas I and II, formula I or formula II wherein R
    1 is hydrogen, lower alkyl, lower alkoxy, halogen, S-lower alkyl, lower alkoxy substituted by halogen, di-lower alkyl amino, C(O)O-lower alkyl, lower alkyl substituted by hydroxy or hydroxy; R
    2 is hydrogen, lower alkyl, halogen, lower alkoxy, S-lower alkyl, lower alkoxy substituted by halogen, O(CH
    2 )
    2 -lower alkoxy substituted by halogen, di-lower alkyl amino, alkyl amino, NH-lower alkyl substituted by halogen, N(lower alkyl)-benzyl, lower alkyl substituted by hydroxy, heterocycloalkyl optionally substituted by halogen, CH
    2 -lower alkoxy, CH
    2 -lower alkoxy substituted by halogen or hydroxy; or R
    1 and R
    2 form together with the carbon atoms to which they are attached a ring containing -OCH
    2 CH
    2 O-, OCH
    2 O-, OCH
    2 CH
    2 CH
    2 O- or -NHC(O)CH
    2 O-; R
    3 is hydrogen or lower alkoxy; R
    4 is hydrogen or lower alkyl; R
    5 is lower alkyl, cycloalkyl, lower alkyl substituted by hydroxy or lower alkyl substituted by halogen; or R
    4 and R
    5 form together with the nitrogen atom to which they are attached a ring containing -CH
    2 CH
    2 CHRCH
    2 CH
    2 -, -CH
    2 CHRCH
    2 CH
    2 -, -CH
    2 CH
    2 OCH
    2 CH
    2 -, -CH
    2 CH
    2 NR'CH
    2 CH
    2 -, CH
    2 CHR- or -CH
    2 CH
    2 CH
    2 -; wherein R is hydrogen, halogen, lower alkyl, lower alkoxy or lower alkyl substituted by halogen; R' is lower alkyl substituted by halogen; R
    a is hydrogen or H; R
    b is hydrogen, hydroxy or
    3 H; R
    6 is hydrogen, halogen or lower alkyl; HetAr is selected from the group consisting of thiophenyl, furanyl, thiozolyl, benzofuranyl, pyrazolyl, benzoimidazolyl or pyridinyl; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The present compounds are suitable as imaging tool, which will improve diagnosis by identifying potential patients with excess of tau aggregates in the brain, which may be likely to develop Alzheimer's disease.

    摘要翻译： 本发明涉及式I和II化合物，其中R 1是氢，低级烷基，低级烷氧基，卤素，S-低级烷基，被卤素取代的低级烷氧基，二低级烷基氨基，C（O）O-低级烷基，低级 被羟基或羟基取代的烷基; R 2是氢，低级烷基，卤素，低级烷氧基，S-低级烷基，被卤素取代的低级烷氧基，被卤素取代的O（CH 2）2 - 低级烷氧基，二低级烷基氨基，烷基氨基，被NH 卤素，N（低级烷基） - 苄基，被羟基取代的低级烷基，任选被卤素取代的杂环烷基，CH 2 - 低级烷氧基，被卤素或羟基取代的CH 2 - 低级烷氧基; 或R 1和R 2与它们所连接的碳原子一起形成含有-OCH 2 CH 2 O-，OCH 2 O-，OCH 2 CH 2 CH 2 O-或-NHC（O）CH 2 O-的环; R3是氢或低级烷氧基; R4是氢或低级烷基; R5是低级烷基，环烷基，被羟基取代的低级烷基或被卤素取代的低级烷基; 或R 4和R 5与它们所连接的氮原子一起与含有-CH 2 CH 2 CHRCH 2 CH 2 - ， - CH 2 CHRCH 2 CH 2 - ， - CH 2 CH 2 OCH 2 CH 2 -CH 2 CH 2 NR'CH 2 CH 2 - ，CH 2 CHR-或-CH 2 CH 2 CH 2 - 其中R为氢，卤素，低级烷基，低级烷氧基或被卤素取代的低级烷基; R'是被卤素取代的低级烷基; Ra为氢或3H; Rb是氢，羟基或3H; R6是氢，卤素或低级烷基; HetAr选自噻吩基，呋喃基，噻唑基，苯并呋喃基，吡唑基，苯并咪唑基或吡啶基; n为1或2; 或其药学上可接受的酸加成盐与外消旋混合物或其相应的对映体和/或光学异构体反应。 本发明化合物适合作为成像工具，其可以通过鉴定潜在的大脑中tau聚集体的潜在患者来改善诊断，这可能可能发展为阿尔茨海默氏病。

    DIAZACARBAZOLE DERIVATIVES AS TAU-PET-LIGANDS
    2.
    发明公开
    DIAZACARBAZOLE DERIVATIVES AS TAU-PET-LIGANDS 有权
    DIAZACARBAZOLE DERIVATIVES TAU-PET-LIGANDS

    公开(公告)号：EP3055308A1

    公开(公告)日：2016-08-17

    申请号：EP14781169.9

    申请日：2014-10-06

    申请人： F.Hoffmann-La Roche AG

    发明人： GOBBI, Luca ,  KNUST, Henner ,  KOERNER, Matthias ,  MURI, Dieter

    IPC分类号： C07D471/04 ,  A61K31/44 ,  A61P25/28

    CPC分类号： A61K51/0455 ,  C07D471/04 ,  C07D471/14

    摘要： The present invention relates to compounds that may be used for binding and imaging tau aggregates and related beta-sheet aggregates including, besides others, beta-amyloid aggregates or alpha-synuclein aggregates.

    摘要翻译： 本发明涉及通式（I）的化合物，其中R是氢或氚; F是氟或18氟; 或可药用酸加成盐。 式I化合物包括2-（6-氟 - 吡啶-3-基）-9H-二吡啶并[2,3-b; 3'，4'-d]吡咯，3H-2-（6-氟 - -9H-二吡啶并[2,3-b; 3'，4'-d]吡咯和[18 F] -2-（6-氟 - 吡啶-3-基）-9H-二吡啶并[2,3- -b; 3' ，4'-d]吡咯。 这些化合物可用于结合和成像tau聚集体和相关的β折叠聚集体，包括除了其他β-淀粉状蛋白聚集体或α-突触核蛋白聚集体。