Arylsulfonylmethyl or arylsulfonamide substituted aromatic compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor
    88.
    发明授权
    Arylsulfonylmethyl or arylsulfonamide substituted aromatic compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 有权
    芳基磺酰基甲基或芳基磺酰胺取代的芳族化合物,适用于治疗对多巴胺D3受体调节作用的疾病

    公开(公告)号:US08969552B2

    公开(公告)日:2015-03-03

    申请号:US11665428

    申请日:2005-10-14

    摘要: The present invention relates to aromatic compounds 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 1 or 2 radicals Rb; X is N or CH; Y is O, S, —CH═N—, —CH═CH— or —N═CH—; A is CH2, O or S; 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, C2-C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, or R1a and R2 together are (CH2)n with n being 2 or 3, or R1a and R2a together are (CH2)n with n being 2 or 3; R2 and R2a are independently of each other H, CH3, CH2F, CHF2 or CF3; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, C1-C2-alkyl and fluorinated C1-C2-alkyl; and the 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.

    摘要翻译: 本发明涉及式I的芳族化合物,其中Ar是苯基或芳族5-或6-元C-结合的杂芳族基团,其中Ar可以带有1个基团R a,并且其中Ar也可以带有1个或2个基团Rb; X为N或CH; Y是O,S,-CH = N - , - CH = CH-或-N = CH-; A是CH 2,O或S; 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为H,C2-C4-烷基,C3-C4-环烷基,C3-C4-烯基,氟化C1-C4-烷基,氟化C3-C4-环烷基或R1a和R2一起为(CH2)n,n为2 或3,或R 1a和R 2a一起为(CH 2)n,其中n为2或3; R2和R2a彼此独立地为H,CH3,CH2F,CHF2或CF3; R3是H或C1-C4-烷基; R6,R7彼此独立地选自H,C1-C2-烷基和氟化C1-C2-烷基; 及其生理上耐受的酸加成盐。 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。