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    Arylsulfonylmethyl or arylsulfonamide substituted aromatic compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor
    24.
    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

    申请人： Karla Drescher ,  Andreas Haupt ,  Liliane Unger ,  Sean C. Turner ,  Wilfried Braje ,  Roland Grandel ,  Christophe Henry

    发明人： Karla Drescher ,  Andreas Haupt ,  Liliane Unger ,  Sean C. Turner ,  Wilfried Braje ,  Roland Grandel ,  Christophe Henry

    IPC分类号： C07C311/44 ,  C07D207/10 ,  C07D211/10 ,  C07D215/38 ,  C07D263/32 ,  C07D413/04 ,  C07C311/21 ,  C07C311/29 ,  C07D239/84 ,  C07D277/82 ,  C07D311/04 ,  C07D491/04

    CPC分类号： C07C311/21 ,  C07C311/29 ,  C07C311/44 ,  C07C2601/02 ,  C07C2602/10 ,  C07D207/10 ,  C07D211/10 ,  C07D215/38 ,  C07D239/84 ,  C07D263/32 ,  C07D277/82 ,  C07D311/04 ,  C07D413/04 ,  C07D491/04

    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。

    Tetrahydrobenzazepines and their use in he modulation of the dopamine D3 receptor
    30.
    发明授权
    Tetrahydrobenzazepines and their use in he modulation of the dopamine D3 receptor 失效
    四氢苯并吖嗪及其在多巴胺D3受体调节中的应用

    公开(公告)号：US08207160B2

    公开(公告)日：2012-06-26

    申请号：US10583590

    申请日：2004-12-17

    申请人： Wilfried Braje ,  Andreas Haupt ,  Wilfried Lubisch ,  Roland Grandel ,  Karla Drescher ,  Herve Geneste ,  Liliane Unger ,  Daryl R. Sauer

    发明人： Wilfried Braje ,  Andreas Haupt ,  Wilfried Lubisch ,  Roland Grandel ,  Karla Drescher ,  Herve Geneste ,  Liliane Unger ,  Daryl R. Sauer

    IPC分类号： A61P25/00 ,  A61K31/55 ,  C07D223/16 ,  C07D409/12

    CPC分类号： C07D223/16 ,  C07D409/12

    摘要： The invention relates to tetrahydrobenzazepines of the general formula I in which the variables Ar, A, B, Y, R1 and R2 have the meanings indicated in claim 1, as well as the N-oxides of these compounds, the physiologically tolerated acid addition salts of these compounds and the physiologically tolerated acid addition salts of the N-oxides. The invention also relates to a pharmaceutical composition that comprises at least one tetrahydrobenzazepine compound of the formula I, the physically tolerated acid addition salt of I, the N-oxide of compound of the formula I and/or the physically tolerated acid addition salts of the N-oxides of I, and further to the use of a compound according to the present invention for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists. The compounds according to the invention are preferably useful for the treatment of disorders of the central nervous system such as schizophrenia and depression and for the treatment of renal function disorders.

    摘要翻译： 本发明涉及通式Ⅰ的四氢苯并吖庚因，其中变量Ar，A，B，Y，R 1和R 2具有权利要求1所示的含义，以及这些化合物的N-氧化物，生理上耐受的酸加成盐 的这些化合物和N-氧化物的生理上耐受的酸加成盐。 本发明还涉及药物组合物，其包含至少一种式I的四氢苯并氮杂化合物，I的物理耐受的酸加成盐，式I化合物的N-氧化物和/或其物理上耐受的酸加成盐 I的N-氧化物，并且进一步使用根据本发明的化合物用于治疗有益于多巴胺D3受体拮抗剂或多巴胺D3激动剂的病症。 根据本发明的化合物优选可用于治疗中枢神经系统疾病如精神分裂症和抑郁症以及治疗肾功能障碍。