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    2-Naphthamide derivatives and their therapeutic applications
    48.
    发明授权
    2-Naphthamide derivatives and their therapeutic applications 失效
    2-萘甲酰胺衍生物及其治疗应用

    公开(公告)号：US5872119A

    公开(公告)日：1999-02-16

    申请号：US762782

    申请日：1996-12-10

    申请人： Camille-Georges Wermuth ,  Andre Mann ,  Fabrice Garrido ,  Jeanne-Marie Lecomte ,  Jean-Charles Schwartz ,  Pierre Sokoloff

    发明人： Camille-Georges Wermuth ,  Andre Mann ,  Fabrice Garrido ,  Jeanne-Marie Lecomte ,  Jean-Charles Schwartz ,  Pierre Sokoloff

    IPC分类号： C07D295/12 ,  A61K31/445 ,  A61K31/451 ,  A61K31/495 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  A61P25/30 ,  A61P39/02 ,  A61P43/00 ,  C07D211/14 ,  C07D211/70 ,  C07D295/13 ,  A61K31/50 ,  C07D401/00 ,  C07D413/00

    CPC分类号： C07D295/13 ,  C07D211/14 ,  C07D211/70

    摘要： The invention related to 2-naphthamide derivatives, in the form of bases or of salts, corresponding to the following general formula (I): ##STR1## in which: the Z--Y entity represents an N--CH.sub.2, C.dbd.CH or CH--CH.sub.2 group;R.sup.1 represents a hydrogen, fluorine, bromine or iodine atom or a hydroxyl, methoxy, nitrile or nitro group;R.sup.2 represents a hydrogen or bromine atom or a hydroxyl, methoxy, nitrile or nitro group;the R.sub.1 and R.sup.2 substituents both being situated on the same ring of the naphthamide unit or each being situated on one of the rings;R.sup.3 and R.sup.4 can be identical or different and each independently represent a hydrogen or chlorine atom or a methoxy or methyl group or an electron-withdrawing group.The invention also relates to their therapeutic applications as partial agonists of the dopamine D.sub.3 receptor.The invention applies more particularly to the treatment of neuropsychiatric conditions involving the dopamine D.sub.3 receptor, in particular psychotic and depressive states, to the treatment of drug-dependence states or to the treatment of disorders of a sexual nature.

    摘要翻译： 本发明涉及对应于以下通式（I）的碱或盐形式的2-萘甲酰胺衍生物：其中：ZY实体代表N-CH 2，C = CH或 CH-CH2基; R1表示氢，氟，溴或碘原子或羟基，甲氧基，腈或硝基; R2表示氢或溴原子或羟基，甲氧基，腈或硝基; R1和R2取代基都位于萘甲酰胺单元的相同环上，或者各自位于其中一个环上; R3和R4可以相同或不同，并且各自独立地表示氢或氯原子或甲氧基或甲基或吸电子基团。 本发明还涉及其作为多巴胺D3受体的部分激动剂的治疗应用。 本发明更具体地涉及治疗涉及多巴胺D3受体，特别是精神病和抑郁状态的治疗药物依赖状态或治疗性性疾病的神经精神病学条件。