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    • 5. 发明授权
    • Indole Derivatives useful for the treatment of CNS disorders
    • 吲哚衍生物可用于治疗CNS疾病
    • US06743809B2
    • 2004-06-01
    • US10347574
    • 2003-01-17
    • Jakob FeldingBenny Bang-AndersenGarrick Paul SmithKim Andersen
    • Jakob FeldingBenny Bang-AndersenGarrick Paul SmithKim Andersen
    • A61K31454
    • C07D401/04C07D401/14C07D405/14C07D409/14C07D417/14
    • The present invention relates to substituted indole derivatives of formula I wherein R1 is hydrogen or optionally substituted C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl or C3-8-cycloalkyl-C1-6-alkyl, or R1 is optionally substituted aryl, aryl-C1-6-alkyl, heteroaryl, heteroaryl-C1-6-alkyl or R1 is —NR′R″ wherein R′ and R″ are independently selected from hydrogen and optionally substituted C1-6-alkyl, aryl, aryl-C1-6-alkyl, heteroaryl and heteroaryl-C1-6-alkyl, or R1 is a saturated or partially saturated 5- to 6-membered ring containing one, two or three hetero atoms selected from O or S, and a group N—R9 wherein R9 is hydrogen or optionally substituted C1-6-alkyl; R2 is C1-6-alkyl W, n, X, R3-R8 are as defined in the description. The compounds of the invention are potent dopamine D4 ligands.
    • 本发明涉及式I的取代的吲哚衍生物,其中R 1是氢或任选取代的C 1-6 - 烷基,C 2-6烯基,C 2-6 - 炔基,C 3-8 - 环烷基或C 3-8 - C 1-6 - 烷基或R 1是任选取代的芳基,芳基-C 1-6 - 烷基,杂芳基,杂芳基-C 1-6 - 烷基或R 1是-NR'R“,其中R'和R “独立地选自氢和任选取代的C 1-6 - 烷基,芳基,芳基-C 1-6 - 烷基,杂芳基和杂芳基-C 1-6 - 烷基,或R 1是饱和或部分饱和的5-至 含有一个,两个或三个选自O或S的杂原子的6元环和NR 9基团,其中R 9是氢或任选取代的C 1-6 - 烷基; R 2是C 1-6 - 烷基W,n,X,R 3 -R 8如说明书中所定义。本发明的化合物是有效的多巴胺D4配体。