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    • 5. 发明公开
    • 도파민 D3 수용체 조절에 반응하는 질환 치료에 적합한헤테로사이클릭 화합물
    • 适用于治疗多巴胺D3受体调节障碍的异种化合物
    • KR1020070084208A
    • 2007-08-24
    • KR1020077010955
    • 2005-10-14
    • 애보트 게엠베하 운트 콤파니 카게
    • 드레셔카를라하웁트안드레아스운거릴리아네터너신씨브라예빌프리트그란델롤란트앙리크리스토프백피쉬기셀라베여바흐아르민루비쉬빌프리트
    • C07D211/26C07D401/04C07D403/04A61K31/397
    • C07D413/14C07D205/04C07D207/09C07D211/28C07D401/04C07D401/12C07D403/04C07D405/12C07D409/12C07D413/10C07D413/12
    • The invention relates to compounds of the formula (I) wherein n is 0, 1 or 2; G is CH2 or CHR3; R1 is H, C,-C 6-alkyl, C,-C6-alkyl substituted by C3-C 6-cycloalkyl, Cl-C6-hydroxyalkyl, fluorinated C,-C6-alkyl, C3-C6-cycloalkyl, fluorinated C3-C6-cycloalkyl, C3-C 6-alkenyl, fluorinated C3-C6-alkenyl, formyl, acetyl or propionyl; R2, R3 and R4 are, independently of each other, H, methyl, fluoromethyl, difluoromethyl, or trifluoromethyl; A is phenylene, pyridylene, pyrimidylene, pyrazinylene, pyridazinylene or thiophenylene, which can be substituted by one ore more substituents selected from halogen, methyl, methoxy and CF3; E is NR5 or CH2, wherein R5 is H or C 1 -C3-alkyl; Ar is a cyclic radical selected from the group consisting of phenyl, a 5-or 6-membered heteroaromatic radical comprising as ring members 1, 2 or 3 heteroatoms selected from N, O and S and a phenyl ring fused to a saturated or unsaturated 5-or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2 or 3 heteroatoms selected from N, O and S and/or 1, 2 or 3 heteroatom-containing groups each independently selected from NR8, where R8 is H, C1-C4-alkyl, fluorinated C1-C4-alkyl, C1-C 4-alkylcarbonyl or fluorinated C1-C4-alkylcarbonyl, and where the cyclic radical Ar may carry 1, 2 or 3 substituents Ra, wherein the variable Ra has the meanings given in the claims and in the description; and physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.
    • 本发明涉及式(I)化合物,其中n为0,1或2; G是CH 2或CHR 3; R 1是被C 3 -C 6 - 环烷基取代的C 1 -C 6 - 烷基,C 1 -C 6 - 烷基,C 1 -C 6羟基烷基,氟化C 1 -C 6烷基,C 3 -C 6环烷基,氟化C 3 -C 6 - C 3 - C 6 - 烯基,氟化C 3 -C 6 - 烯基,甲酰基,乙酰基或丙酰基; R2,R3和R4彼此独立地为H,甲基,氟甲基,二氟甲基或三氟甲基; A是可以被一个或多个选自卤素,甲基,甲氧基和CF 3的取代基取代的亚苯基,亚吡啶基,亚嘧啶基,吡嗪基,哒嗪基或亚噻吩基; E是NR 5或CH 2,其中R 5是H或C 1 -C 3 - 烷基; Ar是选自苯基,5-或6-元杂芳族基团的环状基团,其包含作为环成员1,2或3个选自N,O和S的杂原子和与饱和或不饱和5 - 或6-元碳环或杂环,其中杂环包含作为环成员1,2或3个选自N,O和S的杂原子和/或1,2或3个各自独立地选自NR8的含杂原子的基团,其中 R8是H,C1-C4-烷基,氟化C1-C4-烷基,C1-C4-烷基羰基或氟化C1-C4-烷基羰基,其中环状基团Ar可以带有1,2或3个取代基Ra,其中可变 Ra具有权利要求书和说明书中给出的含义; 和其生理学耐受的酸加成盐。 本发明还涉及式I化合物或其药学上可接受的盐在制备用于治疗易受多巴胺D3受体配体治疗的医学疾病的药物组合物中的用途。