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    Spiro (piperidine-4,2′-pyrrolidine)-1-(3,5-trifluoromethyl phenyl) methylcarboxamides as NK1 tachikynin receptor antagonists
    5.
    发明授权
    Spiro (piperidine-4,2′-pyrrolidine)-1-(3,5-trifluoromethyl phenyl) methylcarboxamides as NK1 tachikynin receptor antagonists 有权
    螺（哌啶-4,2'-吡咯烷）-1-（3,5-三氟甲基苯基）甲基甲酰胺作为N​​K1振动子受体拮抗剂

    公开(公告)号：US08367692B2

    公开(公告)日：2013-02-05

    申请号：US12989699

    申请日：2009-04-29

    申请人： Giuseppe Alvaro ,  Emiliano Castiglioni ,  Agostino Marasco

    发明人： Giuseppe Alvaro ,  Emiliano Castiglioni ,  Agostino Marasco

    IPC分类号： A61K31/438 ,  C07D401/04 ,  C07D471/10

    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 C1-4 alkyl; R1 is hydrogen, C1-4 alkyl, C(O)OH, C(O)NH2 or (C1-4 alkylene)R10; R2 and R3 are independently hydrogen, C1-4 alkyl or R2 together with R3 and together with the carbon atom to which they are attached form a C3-8 cycloalkyl group; R4 is C1-4 alkyl, C1-4 alkoxy or halogen; R5 and R7 are independently hydrogen, hydroxy, halogen, C(O)NH2, C(O)OH or (C1-4 alkylene)R10; R6 and R8 are independently hydrogen or halogen; R9 is hydrogen, (C1-4 alkylene)R10, C(O)NH2, C(O)OH or R9 together with R form a 6 membered heterocyclic ring optionally containing a further heteroatom selected from oxygen, sulphur or nitrogen; R10 is hydrogen, halogen, hydroxy, C(O)NH2, C(O)NH(C1-4 alkyl), C(O)N(C1-4 alkyl)2 or C(O)OH; n is 0, 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; R2和R3独立地为氢，C1-4烷基或R2与R3一起并与它们所连接的碳原子一起形成C 3-8环烷基; R4是C1-4烷基，C1-4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; R9是氢，（C1-4亚烷基）R10，C（O）NH2，C（O）OH或R9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0,1或2.其制备方法，含有它们的组合物及其在治疗NK1拮抗作用有益的疾病和病症中的用途。

    Spiro (Piperidine-4,2'-Pyrrolidine)-1-(3,5-Trifluoromethyl Phenyl) Methylcarboxamides As NK1 Tachikynin Receptor Antagonists
    7.
    发明申请
    Spiro (Piperidine-4,2'-Pyrrolidine)-1-(3,5-Trifluoromethyl Phenyl) Methylcarboxamides As NK1 Tachikynin Receptor Antagonists 有权
    螺（哌啶-4,2'-吡咯烷）-1-（3,5-三氟甲基苯基）甲基甲酰胺作为N​​K1激动素受体拮抗剂

    公开(公告)号：US20110053922A1

    公开(公告)日：2011-03-03

    申请号：US12989699

    申请日：2009-04-29

    申请人： Giuseppe Alvaro ,  Emiliano Castiglioni ,  Agostino Marasco

    发明人： Giuseppe Alvaro ,  Emiliano Castiglioni ,  Agostino Marasco

    IPC分类号： A61K31/5386 ,  C07D471/10 ,  A61K31/438 ,  C07D491/20 ,  A61P25/24 ,  A61P25/22

    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 C1-4 alkyl; R1 is hydrogen, C1-4 alkyl, C(O)OH, C(O)NH2 or (C1-4 alkylene)R10; R2 and R3 are independently hydrogen, C1-4 alkyl or R2 together with R3 and together with the carbon atom to which they are attached form a C3-8 cycloalkyl group; R4 is C1-4 alkyl, C1-4 alkoxy or halogen; R5 and R7 are independently hydrogen, hydroxy, halogen, C(O)NH2, C(O)OH or (C1-4 alkylene) R10; R6 and R8 are independently hydrogen or halogen; R9 is hydrogen, (C1-4 alkylene)R10, C(O)NH2, C(O)OH or R9 together with R form a 6 membered heterocyclic ring optionally containing a further heteroatom selected from oxygen, sulphur or nitrogen; R10 is hydrogen, halogen, hydroxy, C(O)NH2, C(O)NH(C1-4 alkyl), C(O)N(C1-4 alkyl)2 or C(O)OH; n is 0, 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; R2和R3独立地为氢，C1-4烷基或R2与R3一起并与它们所连接的碳原子一起形成C 3-8环烷基; R4是C1-4烷基，C1-4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; R9是氢，（C1-4亚烷基）R10，C（O）NH2，C（O）OH或R9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0,1或2.其制备方法，含有它们的组合物及其在治疗NK1拮抗作用有益的疾病和病症中的用途。