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    SPIRO (PIPERIDINE-4, 2 ' -PYRROLIDINE) -1- (3, 5- TRIFLUOROMETHYL PHENYL) METHYLCARBOXAMIDES AS NK1 TACHIKYNIN RECEPTOR ANTAGONISTS
    2.
    发明申请
    SPIRO (PIPERIDINE-4, 2 ' -PYRROLIDINE) -1- (3, 5- TRIFLUOROMETHYL PHENYL) METHYLCARBOXAMIDES AS NK1 TACHIKYNIN RECEPTOR ANTAGONISTS 审中-公开
    作为NK1 TACHIKYNIN受体拮抗剂的SPIRO（哌啶-4，2'-吡咯烷）-1-（3,5-二氟甲基苯基）甲基氨基甲酰胺

    公开(公告)号：WO2009133135A1

    公开(公告)日：2009-11-05

    申请号：PCT/EP2009/055190

    申请日：2009-04-29

    申请人： GLAXO WELLCOME MANUFACTURING PTE LTD ,  ALVARO, Giuseppe ,  CASTIGLIONI, Emiliano ,  MARASCO, Agostino

    发明人： ALVARO, Giuseppe ,  CASTIGLIONI, Emiliano ,  MARASCO, Agostino

    IPC分类号： C07D471/10 ,  C07D498/20 ,  A61P25/22 ,  A61P25/24 ,  A61P29/00

    CPC分类号： C07D471/10 ,  C07D498/20

    摘要： Compounds of formula (I) or a pharmaceutically acceptable salt thereof wherein R is hydrogen or C 1-4 alkyl; R 1 is hydrogen, C 1-4 alkyl, C(O)OH, C(O)NH 2 or (C 1-4 alkylene)R 10 ; R 2 and R 3 are independently hydrogen, C 1-4 alkyl or R 2 together with R 3 and together with the carbon atom to which they are attached form a C 3-8 cycloalkyl group; R 4 is C 1-4 alkyl, C 1-4 alkoxy or halogen; R 5 and R 7 are independently hydrogen, hydroxy, halogen, C(O)NH 2 , C(O)OH or (C 1-4 alkylene) R 10 ; R 6 and R 8 are independently hydrogen or halogen; R 9 is hydrogen, (C 1-4 alkylene)R 10 , C(O)NH 2 , C(O)OH or R 9 together with R form a 6 membered heterocyclic ring optionally containing a further heteroatom selected from oxygen, sulphur or nitrogen; R 10 is hydrogen, halogen, hydroxy, C(O)NH 2 , C(O)NH(C 1-4 alkyl), C(O)N(C 1-4 alkyl) 2 or C(O)OH; n is O, 1 or 2. processes for their preparation, to compositions containing them and to their use in the treatment of diseases and conditions for which antagonism of NK1 is beneficial.

    摘要翻译： 式（I）化合物或其药学上可接受的盐，其中R是氢或C 1-4烷基; R 1是氢，C 1-4烷基，C（O）OH，C（O）NH 2或（C 1-4亚烷基）R 10; R 2和R 3独立地是氢，C 1-4烷基或R 2与R 3一起并与它们所连接的碳原子一起形成C 3-8环烷基; R4是C 1-4烷基，C 1-4烷氧基或卤素; R 5和R 7独立地是氢，羟基，卤素，C（O）NH 2，C（O）OH或（C 1-4亚烷基）R 10; R6和R8独立地是氢或卤素; R 9是氢，（C 1-4亚烷基）R 10，C（O）NH 2，C（O）OH或R 9与R一起形成任选地含有另外选自氧，硫或氮的杂原子的6元杂环; R 10是氢，卤素，羟基，C（O）NH 2，C（O）NH（C 1-4烷基），C（O）N（C 1-4烷基）2或C（O） n为O，1或2.制备方法，含有它们的组合物及其用于治疗NK1拮抗作用的疾病和病症的用途。