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    • 65. 发明授权
    • 6-amino(aza)indane compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor
    • 适用于治疗对多巴胺D3受体调节作出反应的病症的6-氨基(氮杂)二氢化茚化合物
    • US07759397B2
    • 2010-07-20
    • US11665420
    • 2005-10-14
    • Karla DrescherAndreas HauptLiliane UngerSean C. TurnerWilfried BrajeRoland Grandel
    • Karla DrescherAndreas HauptLiliane UngerSean C. TurnerWilfried BrajeRoland Grandel
    • A61K31/135C07C211/00
    • C07D239/38C07C311/21C07C2601/02C07C2601/04C07C2602/08C07D221/06C07D333/34C07D401/12C07D409/12
    • The present invention relates to 6-amino(aza)indane compound of the formula (I) Wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry I or 2 radicals Rb; X is N or CH; E is CR6R7 or NR3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H or R1a and R2 or R1a and R2a together are (CH2)n with n being 1, 2, 3 or 4; R2 and R2a each independently are H, CH3, CH2F, CHF2 or CF3; R3 is H or C,-C4-alkyl; and the physiologically tolerated acid addition salts of these compounds. The invention also relates to pharmaceutical compositions comprising at least one compound of the formula (I) or a pharmaceutically acceptable salt thereof and to a method for treating a medical disorder susceptible to treatment with a dopamine D3 receptor ligand, said method comprising administering an effective amount of at least one compound of the formula (I) or a pharmaceutically acceptable salt thereof.
    • 本发明涉及式(I)的6-氨基(氮杂)二氢化茚化合物,其中Ar是苯基或芳族5-或6-元C-结合的杂芳族基,其中Ar可以带有1个基团Ra,其中Ar也可以 携带I或2个基团Rb; X为N或CH; E为CR6R7或NR3; R 1是C 1 -C 4烷基,C 3 -C 4环烷基,C 3 -C 4环烷基甲基,C 3 -C 4链烯基,氟化C 1 -C 4烷基,氟化C 3 -C 4环烷基,氟化C 3 -C 4环烷基甲基, C4-烯基,甲酰基或C1-C3-烷基羰基; R1a是H或R1a,R2或R1a和R2a同时为(CH2)n,n为1,2,3或4; R2和R2a各自独立地为H,CH3,CH2F,CHF2或CF3; R3是H或C,-C4-烷基; 和这些化合物的生理上耐受的酸加成盐。 本发明还涉及包含至少一种式(I)化合物或其药学上可接受的盐的药物组合物和治疗易受多巴胺D3受体配体治疗的医学疾病的方法,所述方法包括施用有效量 的至少一种式(I)化合物或其药学上可接受的盐。