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    N-aroyl cyclic amines
    4.
    发明授权
    N-aroyl cyclic amines 失效
    N-芳酰基环胺

    公开(公告)号：US07432270B2

    公开(公告)日：2008-10-07

    申请号：US10477008

    申请日：2002-05-02

    申请人： Clive Leslie Branch ,  Steven Coulton ,  Amanda Johns ,  Christopher Norbert Johnson ,  Roderick Alan Porter ,  Geoffrey Stemp ,  Kevin Thewlis

    发明人： Clive Leslie Branch ,  Steven Coulton ,  Amanda Johns ,  Christopher Norbert Johnson ,  Roderick Alan Porter ,  Geoffrey Stemp ,  Kevin Thewlis

    IPC分类号： A61K31/498 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

    CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

    摘要： This invention relates to N-aroyl cyclic amine derivatives and their use as orexin antagonists wherein: Y represents a bond, oxygen, or a group (CH2)n, wherein n represents 1, 2 or 3; m represents 1, 2, or 3; p represents ) or 1; X is NR, wherein R is H or (C1-4)alkyl; Ar1 is aryl, or a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S; any of which may be optionally substituted; A2 represents phenyl or a 5- or 6-membered heterocyclyl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heterocyclyl group is substituted by R1 and further optional substituents; or Ar2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O and S; R1 represents hydrogen, optionally substituted (C1-4)alkoxy, halo, cyano, optionally substituted (C1-6)alkyl, optionally substituted phenyl, or an optionally substituted 5- or 6-membered heterocyclyl group containing up to 4 heteroatoms selected from N, O and S; when Ar1 is aryl p is not 1, or a pharmaceutical acceptable salt thereof.

    摘要翻译： 本发明涉及N-芳酰基环胺衍生物及其作为食欲素拮抗剂的用途，其中：Y表示键，氧或基团（CH 2）n，其中n 代表1,2或3; m表示1,2或3; p表示）或1; X是NR，其中R是H或（C 1-4 - ）烷基; Ar 1是芳基或含有至多3个选自N，O和S的杂原子的单或双环杂芳基; 任何一个可以任选地被取代; 代表苯基或含有至多3个选自N，O和S的杂原子的5或6元杂环基，其中苯基或杂环基被R 1取代， SUP>和另外任选的取代基; 或Ar 2表示含有至多3个选自N，O和S的杂原子的任选取代的双环芳族或双环杂芳族基团; R 1表示氢，任选取代的（C 1-4 - ）烷氧基，卤素，氰基，任选取代的（C 1-6 - ）烷基， 或任选取代的苯基，或任选取代的含有至多4个选自N，O和S的杂原子的5或6元杂环基; 当Ar 1是芳基p不为1时，或其药学上可接受的盐。