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    Pyridoindolone derivatives substituted in the 3-position by a heterocyclic group, their preparation and their application in therapeutics
    1.
    发明授权
    Pyridoindolone derivatives substituted in the 3-position by a heterocyclic group, their preparation and their application in therapeutics 失效
    吡啶并吲哚酮衍生物在3位被杂环基取代，其制备及其在治疗中的应用

    公开(公告)号：US07456193B2

    公开(公告)日：2008-11-25

    申请号：US11109121

    申请日：2005-04-19

    申请人： Bernard Bourrie ,  Pierre Casellas ,  Jean-Marie Derocq ,  Samir Jegham ,  Yvette Muneaux

    发明人： Bernard Bourrie ,  Pierre Casellas ,  Jean-Marie Derocq ,  Samir Jegham ,  Yvette Muneaux

    IPC分类号： A61K31/437 ,  C07D487/04 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： The present invention relates to pyridoindolone derivatives substituted in the 3-position by a heterocyclic group of general formula (I): in which: R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 represents a hydrogen atom or a (C1-C4)alkyl group; R3 represents a thienyl mono- or polysubstituted by a methyl group; or a monocyclic or bicyclic heterocyclic radical chosen from: a pyridyl, an N-oxidopyridinio, a pyrazolyl, an (N-phenyl)pyrazolyl, an (N-halophenyl)pyrazolyl, a furyl, an indolyl, an (N-benzyl)indolyl, an (N-halobenzyl)indolyl, a benzothienyl or a benzofuryl, the said radicals being unsubstituted or substituted one or more times by a halogen atom or a methyl or methoxy group; R4 and R5 are identical or different and each independently represent a hydrogen or halogen atom or a hydroxyl, hydroxymethyl, (C1-C4)alkyl, trifluoromethyl, C1-C4)alkoxy, (C1-C4)alkoxycarbonyl or cyano group. Preparation process and application in therapeutics.

    摘要翻译： 本发明涉及通式（I）的杂环基在3-位上取代的吡啶并吲哚酮衍生物：其中：R 1表示氢原子或（C 1〜 （C 1 -C 4）烷基; R 2表示氢原子或（C 1 -C 4 -C 4）烷基; R 3表示被甲基单取代或多取代的噻吩基; 或选自以下的单环或双环杂环基：吡啶基，N-氧化吡啶基，吡唑基，（N-苯基）吡唑基，（N-卤代苯基）吡唑基，呋喃基，吲哚基，（N-苄基）吲哚基 ，（N-卤代苄基）吲哚基，苯并噻吩基或苯并呋喃基，所述基团是未取代的或被卤素原子或甲基或甲氧基取代一次或多次; R 4和R 5相同或不同，并且各自独立地表示氢或卤素原子或羟基，羟甲基，（C 1 -C 3 - （C 1 -C 4）烷基，三氟甲基，C 1 -C 4烷氧基，（C 1 -C 4 - 4）烷氧基羰基或氰基。 制剂工艺及其在治疗中的应用