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    NOVEL POTASSIUM CHANNEL BLOCKERS
    61.
    发明申请
    NOVEL POTASSIUM CHANNEL BLOCKERS 审中-公开
    新型钾通道阻塞剂

    公开(公告)号：WO2010023448A1

    公开(公告)日：2010-03-04

    申请号：PCT/GB2009/002078

    申请日：2009-08-27

    申请人： XENTION LIMITED ,  JOHN, Derek, Edward ,  MULLA, Mushtaq ,  HAMLYN, Richard, John ,  GARRETT, Sarah, Louise ,  HARTZOULAKIS, Basil ,  MADGE, David ,  FORD, John

    发明人： JOHN, Derek, Edward ,  MULLA, Mushtaq ,  HAMLYN, Richard, John ,  GARRETT, Sarah, Louise ,  HARTZOULAKIS, Basil ,  MADGE, David ,  FORD, John

    IPC分类号： C07C311/21 ,  C07D205/04 ,  C07D211/08 ,  C07D213/04 ,  C07D231/00 ,  C07D233/54 ,  C07D265/28 ,  C07D271/12 ,  C07D277/32 ,  C07D307/79 ,  C07D311/70 ,  C07D317/62 ,  C07D319/18 ,  A61K31/18 ,  A61P29/00

    CPC分类号： C07C311/21 ,  C07C311/46 ,  C07C317/32 ,  C07C317/40 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07D207/12 ,  C07D209/08 ,  C07D211/16 ,  C07D211/34 ,  C07D211/44 ,  C07D213/36 ,  C07D213/40 ,  C07D213/71 ,  C07D231/12 ,  C07D231/18 ,  C07D231/56 ,  C07D233/61 ,  C07D233/64 ,  C07D233/84 ,  C07D265/30 ,  C07D265/36 ,  C07D271/08 ,  C07D277/28 ,  C07D277/36 ,  C07D277/46 ,  C07D285/12 ,  C07D285/135 ,  C07D307/79 ,  C07D311/70 ,  C07D317/62 ,  C07D319/18 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

    摘要： The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof wherein; X 1 is selected from a group consisting of CH 2 , C(=O), C(=NH), NC(=O), R 1 is selected from the group consisting of optionally substituted arylalkyl, and optionally substituted heteroarylalkyl R 2 is selected from the group consisting of optionally substituted alkyl, optionally substituted aryl or heteroaryl or NR 24 R 25 , R 3 is selected from the group consisting of hydrogen, halogen, hydroxyl, alkoxy, aryloxy, optionally substituted alkyl, optionally substituted amino, optionally substituted amino sulfonyl or nitrile; R 4 is selected from the group consisting of optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted acyl, optionally substituted sulfonyl, optionally substituted sulfamoyl, optionally substituted aryl, optionally substituted arylalkyl, and optionally substituted heteroaryl R 5 may be hydrogen, an optionally substituted alkyl, preferably CH 3 or, NR 4 R 5 may form an optionally substituted saturated or partially saturated 4-7 membered ring with the general formula (II). Wherein; X 2 is C(=O), CH 2 , CH(R 6 ) or C(R 6 )(R 6 ), X 3 is CH 2 , CH(R 7 ), C(R 7 )(R 7 ), NH, N(R 8 ), O or S Each R 6 independently represents optionally substituted amino, optionally substituted amino carbonyl, hydroxyl, optionally substituted acyl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalky, optionally substituted aryl or optionally substituted heteroaryl; Each R 7 independently represents optionally substituted amino, optionally substituted amino carbonyl, hydroxyl, optionally substituted acyl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalky, optionally substituted aryl or optionally substituted heteroaryl R 8 is optionally substituted acyl, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalkyl, optionally substituted aryl or optionally substituted heteroaryl; R 24 and R 25 are the same or different and each represents hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalkyl, optionally substituted aryl or optionally substituted heteroaryl, n = 1 or 2 m = 1, 2 or 3 With the proviso that when X 1 is C=O and R 5 is H then R 4 is not (a) or (b) or (c). Where R 4 a, R 5 a and R 6 a are each independently H, C 1-6 alkyl, aryl, heteroaryl, cycloalkyl, or aryl-C 1-6 alkyl; R 10 a is H or C 1-6 alkyl; and R 11 a is C 1-6 alkyl or aryl-C 1-6 alkyl and when X 1 is C=O or CH 2 and R 5 is H then R 4 is not (d) Where q is 0 to 5, R 3 b is H, OH or alkoxy and R 4 b is NH 2 , phenyl or a C 3-10 heterocycle. The compounds are useful as potassium ion channel inhibitors.

    摘要翻译： 本发明提供式（I）化合物或其盐或其药学上可接受的衍生物，其中： X 1选自CH 2，C（= O），C（= NH），NC（= O），R 1选自任选取代的芳烷基和任选取代的杂芳基烷基R 2选自基团 由任选取代的烷基，任选取代的芳基或杂芳基或NR 24 R 25组成，R 3选自氢，卤素，羟基，烷氧基，芳氧基，任选取代的烷基，任选取代的氨基，任选取代的氨基磺酰基或腈; R 4选自任选取代的烷基，任选取代的环烷基，任选取代的杂环烷基，任选取代的酰基，任选取代的磺酰基，任选取代的氨磺酰基，任选取代的芳基，任选取代的芳基烷基和任选取代的杂芳基R 5可以是氢， 任选取代的烷基，优选CH 3或NR 4 R 5可以形成具有通式（II）的任选取代的饱和或部分饱和的4-7元环。 其中： X2是C（= O），CH2，CH（R6）或C（R6）（R6），X3是CH2，CH（R7），C（R7）（R7），NH，N（R8） 每个R 6独立地表示任选取代的氨基，任选取代的氨基羰基，羟基，任选取代的酰基，任选取代的烷氧基，任选取代的芳氧基，任选取代的烷基，任选取代的环烷基，任选取代的芳基烷基，任选取代的芳基或任选取代的杂芳基; 每个R 7独立地表示任选取代的氨基，任选取代的氨基羰基，羟基，任选取代的酰基，任选取代的烷氧基，任选取代的芳氧基，任选取代的烷基，任选取代的环烷基，任选取代的芳基烷基，任选取代的芳基或任选取代的杂芳基R 8是任选取代的 酰基，任选取代的烷基，任选取代的环烷基，任选取代的芳基烷基，任选取代的芳基或任选取代的杂芳基; R 24和R 25相同或不同，各自表示氢，任选取代的烷基，任选取代的环烷基，任选取代的芳基烷基，任选取代的芳基或任选取代的杂芳基，n = 1或2 m = 1,2或3，条件是当 X1为C = O，R5为H，R4不为（a）或（b）或（c）。 其中R 4a，R 5a和R 6a各自独立地为H，C 1-6烷基，芳基，杂芳基，环烷基或芳基-C 1-6烷基; R10a是H或C1-6烷基; R 11a为C 1-6烷基或芳基-C 1-6烷基，当X 1为C = O或CH 2且R 5为H时，R 4不为（d）其中q为0至5，R 3b为H，OH或烷氧基，R 4b为NH 2 ，苯基或C 3-10杂环。 该化合物可用作钾离子通道抑制剂。

    AMINOAMIDES AS OREXIN ANTAGONISTS
    65.
    发明申请
    AMINOAMIDES AS OREXIN ANTAGONISTS 审中-公开
    AMINOAMIDES作为OREXIN ANTAGONISTS

    公开(公告)号：WO2008107335A1

    公开(公告)日：2008-09-12

    申请号：PCT/EP2008/052245

    申请日：2008-02-25

    申请人： F. HOFFMANN-LA ROCHE AG ,  GOBBI, Luca ,  KNUST, Henner ,  MALHERBE, Parichehr ,  NETTEKOVEN, Matthias ,  PINARD, Emmanuel ,  ROCHE, Olivier ,  ROGERS-EVANS, Mark

    发明人： GOBBI, Luca ,  KNUST, Henner ,  MALHERBE, Parichehr ,  NETTEKOVEN, Matthias ,  PINARD, Emmanuel ,  ROCHE, Olivier ,  ROGERS-EVANS, Mark

    IPC分类号： C07C237/06 ,  C07D213/36 ,  A61K31/16

    CPC分类号： C07D213/36 ,  A61K9/2018 ,  A61K9/4858 ,  C07C237/20 ,  C07C2601/02 ,  C07C2601/04

    摘要： The present invention relates to compounds of formula (I) wherein Ar 1 , Ar 2 and Ar 3 are independently from each other unsubstituted or substituted aryl or heteroaryl; R 1 , R 2 and R 3 are independently from each other hydroxy, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, cyano, 3-hydroxy-oxetan-3-yl, SO 2 -lower alkyl or di-lower alkyl amino; R 4 /R 5 are independently from each other hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, -(CH 2 ) o -O-lower alkyl, -(CH 2 ) o -N-(lower alkyl) 2 , (CH 2 ) p -cycloalkyl, (CH 2 ) p -aryl, which aryl ring may be substituted by halogen, or R 4 and R 5 may form together with the N-atom to which they are attached a heterocyclic ring, optionally with further ring-heteroatoms selected from N, O or S; R 6 is hydrogen or lower alkyl; R 7 is hydrogen or lower alkyl; R 8 is hydrogen or cyano; n is 0, 1, 2 or 3; o is 1, 2 or 3; p is 0, 1 or 2; or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. It has been found that the compounds of formula (I) are orexin receptor antagonists and the related compounds may be useful in the treatment of disorders, in which orexin pathways are involved like sleep disorders.

    摘要翻译： 本发明涉及式（I）化合物，其中Ar 1，Ar 2和Ar 3彼此独立地为未取代或取代的芳基 或杂芳基; R 1，R 2和R 3彼此独立地为羟基，卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基， 由卤素取代的低级烷氧基，氰基，3-羟基 - 氧杂环丁烷-3-基，SO 2 - 低级烷基或二 - 低级烷基氨基; R 4和R 5彼此独立地为氢，低级烷基，被卤素取代的低级烷基，被羟基取代的低级烷基， - （CH 2） -O - 低级烷基， - （CH 2）2 - （低级烷基）2 - （CH 2）2 - 环烷基，（CH 2）n - 芳基，该芳基环（CH 2） 可以被卤素取代，或者R 4和R 5可以与它们所连接的N-原子一起形成杂环，任选地与另外的选择的杂环杂原子一起形成 来自N，O或S; R 6是氢或低级烷基; R 7是氢或低级烷基; R 8是氢或氰基; n为0,1,2或3; o是1,2或3; p为0,1或2; 或其药学上合适的酸加成盐，旋光纯对映异构体，外消旋体或非对映体混合物。 已经发现式（I）化合物是食欲素受体拮抗剂，并且相关化合物可用于治疗其中食欲素途径参与睡眠障碍的病症。