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    BENZENESULFONAMIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR
    85.
    发明申请
    BENZENESULFONAMIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR 审中-公开
    适用于治疗多巴胺D3受体调节障碍的苯并呋喃半导体化合物

    公开(公告)号：US20100210664A1

    公开(公告)日：2010-08-19

    申请号：US12666627

    申请日：2008-10-30

    申请人： Sean Colm Turner ,  Andreas Haupt ,  Wilfred Braje ,  Udo Lange ,  Karla Drescher ,  Liliane Unger ,  Ana Lucia Jongen-Relo ,  Bespalov Anton

    发明人： Sean Colm Turner ,  Andreas Haupt ,  Wilfred Braje ,  Udo Lange ,  Karla Drescher ,  Liliane Unger ,  Ana Lucia Jongen-Relo ,  Bespalov Anton

    IPC分类号： A61K31/496 ,  C07D401/04 ,  A61P25/00 ,  A61P25/30 ,  A61P25/18

    CPC分类号： C07D401/04 ,  C07D213/76

    摘要： The invention relates to compounds of the formula R1 is selected from the group consisting of hydrogen, linear C1-C3 alkyl and fluorinated linear C1-C3 alkyl; R2 is hydrogen or methyl; R3 is selected from the group consisting of hydrogen, halogen, C1-C2-alkyl, fluorinated C1-C2-alkyl, C1-C2-alkoxy and fluorinated C1-C2-alkoxy, R4 is C1-C2-alkyl or fluorinated C1-C2-alkyl; n is 0, 1 or 2, and the physiologically tolerated salts of these compounds and the N-oxides thereof. The invention also relates to a pharmaceutical composition that comprises at least one compound of the formula I and/or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists, said method comprising administering an effective amount of at least one compound or physiologically tolerated acid addition salt of the formula I to a subject in need thereof.

    摘要翻译： 本发明涉及式R1的化合物选自氢，直链C 1 -C 3烷基和氟化线性C 1 -C 3烷基; R2是氢或甲基; R3选自氢，卤素，C1-C2-烷基，氟化C1-C2-烷基，C1-C2-烷氧基和氟化C1-C2-烷氧基，R4是C1-C2-烷基或氟化C1-C2 -烷基; n为0,1或2，以及这些化合物的生理上耐受的盐及其N-氧化物。 本发明还涉及包含至少一种式I化合物和/或其至少一种生理上耐受的酸加成盐的药物组合物，还涉及治疗有益于多巴胺D3受体拮抗剂或多巴胺D3的病症的方法 所述方法包括向有需要的受试者施用有效量的至少一种式I化合物或生理学上耐受的酸加成盐。

    Pyrimidin-2-one compounds and their use as dopamine D3 receptor ligands
    86.
    发明授权
    Pyrimidin-2-one compounds and their use as dopamine D3 receptor ligands 有权
    嘧啶-2-酮化合物及其作为多巴胺D3受体配体的用途

    公开(公告)号：US08008488B2

    公开(公告)日：2011-08-30

    申请号：US10548931

    申请日：2004-03-12

    申请人： Hervé Geneste ,  Andreas Kling ,  Wilfried Braje ,  Andreas Haupt ,  Liliane Unger

    发明人： Hervé Geneste ,  Andreas Kling ,  Wilfried Braje ,  Andreas Haupt ,  Liliane Unger

    IPC分类号： C07D403/06 ,  C07D403/14 ,  C07D401/06 ,  C07D401/14 ,  A61K31/505 ,  A61K31/506 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/22 ,  A61P25/30

    CPC分类号： C07D239/36 ,  C07D239/52 ,  C07D239/54 ,  C07D239/553 ,  C07D239/56 ,  C07D401/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14

    摘要： The invention relates to pyrimidin 2-one compounds of general formula (I), in addition to the derivatives and tautomers of (I) and the physiologically acceptable salts of said compounds. In said formula, A represents linear or branched C3-C6 alkene, which can have a double bond or triple bond and/or a group Z, which is not adjacent to the nitrogen atom of the pyrimidinone ring and is selected from O, S, C(O), NR3, C(O)NR3, NR3C(O), OC(O) and C(O)O; B represents a group of the formula (II), in which X stands for CH2 or N and Y stands for CH2 or CH2CH2, or X—Y can also jointly represent C═CH, C═CH—CH2 or CH—CH═CH; R1 and R2 are defined as cited in the description and the claims; and Ar represents an optionally substituted aromatic group. The invention also relates to a pharmaceutical agent, containing at least one compound (I) and the tautomers, derivatives and/or acid addition salts of said compound, optionally together with physiologically acceptable carriers and/or auxiliary agents. The invention also relates to the use of compounds of formula (I), and their tautomers, derivatives and pharmacologically acceptable acid addition salts for producing a pharmaceutical agent for treating diseases which respond to the influence of dopamine D3 receptor ligands.

    摘要翻译： 除了（I）的衍生物和互变异构体以及所述化合物的生理学上可接受的盐之外，本发明涉及通式（I）的嘧啶-2-酮化合物。 在所述式中，A表示可以具有双键或三键的直链或支链C 3 -C 6烯基和/或不与嘧啶酮环的氮原子相邻并且选自O，S， C（O），NR 3，C（O）NR 3，NR 3 C（O），OC（O）和C（O）O; B表示式（II）的基团，其中X表示CH2或N，Y表示CH2或CH2CH2，或X-Y也可共同表示C = CH，C = CH-CH 2或CH-CH = CH ; R1和R2定义为在说明书和权利要求书中引用的; 并且Ar表示任选取代的芳族基团。 本发明还涉及含有至少一种化合物（I）和所述化合物的互变异构体，衍生物和/或酸加成盐，任选地与生理上可接受的载体和/或辅助剂一起的药剂。 本发明还涉及式（I）化合物及其互变异构体，衍生物和药理学上可接受的酸加成盐的用途，用于制备用于治疗对多巴胺D3受体配体的影响作出反应的疾病的药剂。