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    USE OF TETRAHYDROPYRIDINES IN THE TREATMENT OF SODIUM CHANNEL RELATED DISEASE AND DISORDERS
    1.
    发明公开
    USE OF TETRAHYDROPYRIDINES IN THE TREATMENT OF SODIUM CHANNEL RELATED DISEASE AND DISORDERS 审中-公开

    公开(公告)号：EP3226865A4

    公开(公告)日：2018-06-06

    申请号：EP15864987

    申请日：2015-11-19

    申请人： CENNERV PHARMA S PTE LTD

    发明人： RATTY ANIL KUMAR ,  MICHAEL ENTZEROTH

    IPC分类号： C07D211/70 ,  A61K31/4402 ,  A61P1/00

    CPC分类号： C07D211/70 ,  A61K31/4402

    摘要： The present invention provides a method of treating one or more sodium channel related diseases or disorders in an individual, including related symptoms. The method comprises administering to the individual a tetrahydropyridine derivative in an amount effective to treat sodium channel related diseases or disorders in individuals. These compounds are generally categorised as Ritalin related compounds. The present invention also provides compounds for use in the treatment of and also for use in the manufacture of a medicament for the treatment of sodium channel related diseases or disorders in an individual. A method is further provided for the preparation and isolation of the derivatives of the compound of the present invention.

    S1P AND/OR ATX MODULATING AGENTS
    4.
    发明授权
    S1P AND/OR ATX MODULATING AGENTS 有权
    S1P和/或ATX调节剂

    公开(公告)号：EP2925721B1

    公开(公告)日：2017-06-07

    申请号：EP13799458.8

    申请日：2013-11-20

    申请人： Biogen MA Inc.

    发明人： PENG, Hairuo ,  LIN, Edward, Yin-Shiang ,  CHAO, Jianhua ,  XIN, Zhili ,  MA, Bin ,  GUCKIAN, Kevin ,  CHAN, Timothy ,  KUMARAVEL, Gnanasambandam ,  TAVERAS, Arthur, G.

    IPC分类号： C07D207/08 ,  C07D211/22 ,  C07D211/56 ,  C07D211/62 ,  C07D211/70 ,  C07D213/74 ,  C07D237/22 ,  C07D239/47 ,  C07D295/15 ,  C07D295/155 ,  C07D401/12 ,  A61K31/40 ,  A61K31/451 ,  A61K31/4545 ,  A61K31/495

    CPC分类号： C07D211/22 ,  A61K31/451 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06 ,  C07D207/08 ,  C07D211/56 ,  C07D211/62 ,  C07D211/70 ,  C07D213/74 ,  C07D237/22 ,  C07D239/47 ,  C07D295/15 ,  C07D295/155 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04

    摘要： Compounds of formula (I) wherein: X is —O—, —S(O)r—, —CH2—, or —NR—, wherein r is 0, 1, or 2; X1, X2, and X5 are each independently CR7 or N; one of X3 or X4 is C and is attached by a single bond to -L-, and the other is CR7 or N, provided that no more than three of X1, X2, X3, X or X5 are N; Ring A is monocyclic C5-6scycloalkyl or a 5- to 6-membered monocyclic heterocyclyl comprising from 1 to 5 heteroatoms independently selected from N, S, or O; wherein Ring A is further optionally substituted with from 1 to 3 R4; provided that Ring A is not morpholinyl, thiomorpholinyl or tetrahydro-2H-pyranyl; L is a bond, —O—, —NR—, —S(O)n—, —CH2—, or —C(O)—, wherein n is 0, 1, or 2; 1 2 L1 is an C1-8alkylene, C3-scycloalkylene, —CH2-L2-, or a 3- to 8-membered heterocyclylene comprising 1 to 5; R1 is C6-20alkyl or a monocyclic C3-8cycloalkyl; wherein said C3-8cycloalkyl is substituted with at least one R6 and may be optionally substituted with from 1 to 5 additional R6 substituents, wherein R6 for each occurrence is independently selected; and R2 is —C(O)OR3, —C(O)N(R3)—S(O)2R3, —S(O)2OR3, —C(O)NHC(O)R3, —Si(O)OH, —B(OH)2, —N(R3)S(O)2R3, —S(O)2N(R3)2, —O—P(O)(OR3)2, or —P(O)(OR3)2, —CN, —S(O)2NHC(O)R3, —C(O)NHS(O)2R3, —C(O)NHOH, —C(O)NHCN, —CH(CF3)OH, —C(CF3)2OH, or a selected heteroaryl or heterocyclyl; and pharmaceutically acceptable salts thereof, can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX).

    摘要翻译： 其中：X是-O - ， - S（O）r - ， - CH 2 - 或-NR-，其中r是0,1或2的式（I） X1，X2和X5各自独立地为CR7或N; 条件是X1，X2，X3，X或X5中不超过三个是N; X3或X4中的一个是C并且通过单键连接至-L-，另一个是CR7或N。 环A是单环C5-6环烷基或包含1至5个独立地选自N，S或O的杂原子的5-至6-元单环杂环基; 其中环A进一步任选被1至3个R 4取代; 环A不是吗啉基，硫代吗啉基或四氢-2H-吡喃基; L是键，-O - ， - NR - ， - S（O）n - ， - CH 2 - 或-C（O） - ，其中n是0,1或2; 1 2 L 1为C 1-8亚烷基，C 3 - 亚环烷基，-CH 2 -L 2 - 或包含1至5的3至8元杂环烯基; R1是C6-20烷基或单环C3-8环烷基; 其中所述C 3-8环烷基被至少一个R 6取代并且可以任选被1至5个另外的R 6取代基取代，其中R 6每次出现时独立地选择; （O）OR3，-C（O）N（R3）-S（O）2R3，-S（O）2OR3，-C（O）NHC（O）R3，-Si（O）OH ，-B（OH）2，-N（R3）S（O）2R3，-S（O）2N（R3）2，-O-P（O）（OR3）2或-P（O） ）2，-CN，-S（O）2NHC（O）R3，-C（O）NHS（O）2R3，-C（O）NHOH，-C（O）NHCN，-CH（CF3）OH， - C（CF 3）2 OH或选择的杂芳基或杂环基; 及其药学上可接受的盐可以调节一种或多种SIP受体的活性和/或autotaxin（ATX）的活性。