利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

18 条记录 (耗时 0.017 秒)

    ETHYNYL DERIVATIVES
    11.
    发明公开
    ETHYNYL DERIVATIVES 有权
    乙炔衍生物

    公开(公告)号：EP3049409A1

    公开(公告)日：2016-08-03

    申请号：EP14781474.3

    申请日：2014-09-22

    申请人： F.Hoffmann-La Roche AG

    发明人： BIEMANS, Barbara ,  GUBA, Wolfgang ,  JAESCHKE, Georg ,  RICCI, Antonio ,  RUEHER, Daniel ,  VIEIRA, Eric

    IPC分类号： C07D405/14 ,  C07D401/04 ,  C07D401/10 ,  C07D405/04 ,  C07D239/91 ,  C07D471/04 ,  C07D473/04 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04 ,  A61K31/517 ,  A61P3/10 ,  A61P25/10 ,  A61P25/22 ,  A61P25/24

    CPC分类号： C07D239/96 ,  C07D239/91 ,  C07D401/04 ,  C07D401/10 ,  C07D405/04 ,  C07D405/14 ,  C07D471/04 ,  C07D473/04 ,  C07D475/02 ,  C07D475/04 ,  C07D487/04 ,  C07D487/06 ,  C07D495/04 ,  C07D513/04

    摘要： The present invention relates to compounds of formula I wherein Y is N or C-R
    1' ; G is a 5 or 6-membered aromatic or heteroaromatic ring containing 0, 1, 2 or 3 heteroatoms, selected from the group consisting of phenyl, pyridinyl with different N-positions, imidazolyl, pyrazinyl, pyrimidinyl, thiophenyl, thiazolyl, pyrazolyl or thiadiazolyl, which are optionally substituted by 1, 2 or 3 substituents, selected from the group consisting of halogen, lower alkyl, lower alkoxy, lower alkoxy substituted by halogen or NRR'; R and R' are independently from each other hydrogen or lower alkyl, or may form together with the N atom to which they are attached a five or six membered saturated heterocyclic group which may contain an additional oxygen, NH, or N-lower alkyl group; R
    1 is hydrogen, halogen or lower alkyl substituted by halogen; R
    1' is hydrogen, halogen or lower alkyl substituted by halogen; R
    2 is hydrogen, lower alkyl, lower alkoxyalkyl, cycloalkyl or heterocycloalkyl; or R
    2 may form together with the closest carbon atom in group G a group (IA) for A being -CH
    2 -, -CH
    2 CH
    2 , or -C(CH
    3 )
    2 -, R
    3 is phenyl or pyridinyl, wherein the N atom in the pyridinyl group may be in different positions; or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has been surprisingly been found that the compounds of general formula I are positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4), useful for the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.

    摘要翻译： 本发明涉及其中Y是N或C-R'的式I化合物; G是含有0,1,2或3个选自苯基，具有不同N-位的吡啶基，咪唑基，吡嗪基，嘧啶基，噻吩基，噻唑基，吡唑基或噻二唑基的5或6元芳族或杂芳族环 其任选被1,2或3个选自卤素，低级烷基，低级烷氧基，被卤素或NRR'取代的低级烷氧基的取代基取代; R和R'彼此独立地为氢或低级烷基，或者可以与它们所连接的N原子一起形成可含有另外的氧，NH或N-低级烷基的五元或六元饱和杂环基 ; R 1是氢，卤素或被卤素取代的低级烷基; R 1'是氢，卤素或被卤素取代的低级烷基; R 2是氢，低级烷基，低级烷氧基烷基，环烷基或杂环烷基; 或者R 2可与G组中最接近的碳原子一起形成A为-CH 2 - ， - CH 2 CH 2或-C（CH 3）2 - ，R 3为苯基或吡啶基的基团（IA），其中 吡啶基中的N原子可以位于不同的位置; 或其药学上可接受的盐或酸加成盐，外消旋混合物，或其相应的对映异构体和/或旋光异构体和/或立体异构体。 令人惊讶地发现，通式I的化合物是代谢型谷氨酸受体4（mGluR4）的正变构调节剂（PAM），可用于治疗帕金森病，焦虑症，呕吐，强迫症，自闭症，神经保护，癌症 ，抑郁症和2型糖尿病。

    ETHYNYL DERIVATIVES AS MGLUR5 ALLOSTERIC MODULATORS
    13.
    发明公开
    ETHYNYL DERIVATIVES AS MGLUR5 ALLOSTERIC MODULATORS 有权
    作为MGLUR5变构调节剂的乙炔衍生物

    公开(公告)号：EP2763977A1

    公开(公告)日：2014-08-13

    申请号：EP12767005.7

    申请日：2012-10-04

    申请人： F.Hoffmann-La Roche AG

    发明人： JAESCHKE, Georg ,  LINDEMANN, Lothar ,  RICCI, Antonio ,  RUEHER, Daniel ,  STADLER, Heinz ,  VIEIRA, Eric

    IPC分类号： C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  A61K31/4439 ,  A61K31/506 ,  A61P25/18 ,  A61P25/08 ,  A61P25/28

    CPC分类号： C07D401/04 ,  C07D403/04 ,  C07D413/04

    摘要： The present invention relates to ethynyl derivatives of formula (I) wherein U is N or CH, R
    8 is hydrogen, halogen, lower alkyl or lower alkoxy;Y is –N(R
    4 )-, -O- or –C(R
    5 R
    5 ')-; wherein R4 is hydrogen or lower alkyl and R
    5 /R
    5' are independently hydrogen, hydroxy, lower alkyl or lower alkoxy; V is –N(R
    6 )- or –C(R
    7 R
    7' ), wherein R6 is hydrogen or lower alkyl and R
    7 /R
    7' are independently from each other hydrogen, lower alkyl, CH
    2 -lower alkoxy or may form together with the carbon atom to which they are attached a C
    3 -C
    6 -cycloalkyl; R
    1 is phenyl or heteroaryl, which are optionally substituted by halogen, lower alkyl or lower alkoxy; m is 0 or 1; in case m is 1, R
    3 /R
    3' are independently from each other hydrogen, lower alkyl, CH
    2 -lower alkoxy or may form together with the carbon atom to which they are attached a C
    3 -C
    6 -cycloalkyl; n is 0 or 1; in case n is 1, R
    2 /R
    2' are independently from each other hydrogen, lower alkyl, CH
    2 -lower alkoxy or may form together with the carbon atom to which they are attached a C
    3 -C
    6 -cycloalkyl; or if m is 1 and n is 0, R
    3 and R
    7 may form together with the carbon atoms to which they are attached a C
    4-6 -cycloalkyl; or if m is 1 and n is 1, R
    2 and R
    3 or R
    3 and R
    7 may form together with the carbon atoms to which they are attached a C
    4-6 -cycloalkyl; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has been found that the compounds of general formula (I) are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).

    摘要翻译： 本发明涉及式（I）的乙炔基衍生物，其中U是N或CH，R 8是氢，卤素，低级烷基或低级烷氧基; Y是-N（R 4） - ，-O-或-C（R 5R 5'） - ; 其中R4是氢或低级烷基，并且R5 / R5'独立地是氢，羟基，低级烷基或低级烷氧基; V是-N（R 6） - 或-C（R 7 R 7'），其中R 6是氢或低级烷基和R 7 / R 7'彼此独立地是氢，低级烷基，CH 2 - 低级烷氧基或可以是 与它们所连接的碳原子一起形成C 3 -C 6 - 环烷基; R 1为苯基或杂芳基，其任选被卤素，低级烷基或低级烷氧基取代; m是0或1; 在m为1的情况下，R 3 / R 3'彼此独立地为氢，低级烷基，CH 2 - 低级烷氧基或可与它们所连接的碳原子一起形成C 3 -C 6 - 环烷基; n是0或1; 在n为1的情况下，R 2 / R 2'彼此独立地为氢，低级烷基，CH 2 - 低级烷氧基或可与它们所连接的碳原子一起形成C 3 -C 6 - 环烷基; 或者如果m是1并且n是0，则R 3和R 7可以与它们所连接的碳原子一起形成C 4-6 - 环烷基; 或者如果m为1并且n为1，则R 2和R 3或R 3和R 7可以与它们所连接的碳原子一起形成C 4-6 - 环烷基; 或药学上可接受的酸加成盐，外消旋混合物或其相应的对映体和/或光学异构体和/或立体异构体。 已经发现通式（I）的化合物是代谢型谷氨酸受体亚型5（mGluR5）的变构调节剂。