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    • 3. 发明授权
    • Pyridoindolone derivatives substituted in the 3-position by a heterocyclic group, their preparation and their application in therapeutics
    • 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
    • US07456193B2
    • 2008-11-25
    • US11109121
    • 2005-04-19
    • Bernard BourriePierre CasellasJean-Marie DerocqSamir JeghamYvette Muneaux
    • Bernard BourriePierre CasellasJean-Marie DerocqSamir JeghamYvette Muneaux
    • A61K31/437C07D487/04C07D471/04
    • C07D471/04
    • 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.
    • 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