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    1,2,4,-TRIAZIN-3,5-DIONE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR
    1.
    发明申请
    1,2,4,-TRIAZIN-3,5-DIONE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR 有权
    1,2,4，-TRIAZIN-3,5-DIONE适用于治疗多巴胺D3受体调节障碍的化合物

    公开(公告)号：US20100311755A1

    公开(公告)日：2010-12-09

    申请号：US12740714

    申请日：2008-10-31

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

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

    IPC分类号： A61K31/53 ,  C07D253/07 ,  A61P25/00 ,  A61P25/18 ,  A61P25/30 ,  A61P13/12

    CPC分类号： C07D403/12

    摘要： The invention relates to compounds of the formula I: wherein A is a saturated or unsaturated hydrocarbon chain having a chain length of 4 to 6 carbon atoms, the hydrocarbon chain being unsubstituted or substituted by 1, 2 or 3 methyl groups; R1 is selected from the group consisting of hydrogen, C1-C3 alkyl and fluorinated C1-C3 alkyl; R2 is hydrogen, halogen, cyano, C1-C3 alkyl, C1-C3 alkoxy, fluorinated C1-C3 alkyl or fluorinated C1-C3 alkoxy; R3 is selected from the group consisting of branched C4-C6 alkyl and C3-C6 cycloalkyl, and R4 is C1-C6 alkyl, C3-C6 cycloalkyl, fluorinated C1-C3-alkyl and fluorinated C3-C6 cycloalkyl. 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I化合物：其中A是链长为4-6个碳原子的饱和或不饱和烃链，烃链未被取代或被1,2或3个甲基取代; R1选自氢，C1-C3烷基和氟化C1-C3烷基; R2是氢，卤素，氰基，C1-C3烷基，C1-C3烷氧基，氟化C1-C3烷基或氟化C1-C3烷氧基; R3选自支链C4-C6烷基和C3-C6环烷基，R4为C1-C6烷基，C3-C6环烷基，氟化C1-C3-烷基和氟化C3-C6环烷基。 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。

    SUBSTITUTED OXINDOLE COMPOUNDS
    3.
    发明申请
    SUBSTITUTED OXINDOLE COMPOUNDS 有权
    取代的氧化物

    公开(公告)号：US20100286165A1

    公开(公告)日：2010-11-11

    申请号：US12529542

    申请日：2008-02-29

    申请人： Herve' Geneste ,  Thorsten Oost ,  Charles W Hutchins ,  Wolfgang Wernet ,  Liliane Unger ,  Wilfried Hornberger ,  Wilfried Lubisch ,  Astrid Netz

    发明人： Herve' Geneste ,  Thorsten Oost ,  Charles W Hutchins ,  Wolfgang Wernet ,  Liliane Unger ,  Wilfried Hornberger ,  Wilfried Lubisch ,  Astrid Netz

    IPC分类号： A61K31/444 ,  C07D401/14 ,  A61K31/496 ,  A61P9/12 ,  A61P11/00 ,  A61P9/10 ,  A61P9/00 ,  A61P1/04 ,  A61P1/00 ,  A61P25/22 ,  A61P25/28 ,  A61P25/18 ,  A61P25/24 ,  A61P25/30

    CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D401/12 ,  C07D471/08

    摘要： The present invention relates to compounds of the general formula (I) in which A, B, R1, R2 and Het have the meaning given in claim 1; Y is a bivalent group of the formula in which D is C1-C3-alkylene, where D may have a substituent R5; R3 is hydrogen, C1-C8-alkyl or together with R4 is C1-C3-alkylene which may have a radical R5a, or together with R5 is C1-C3-alkylene, and R4 is hydrogen, C1-C8-alkyl or together with R3 is C1-C3-alkylene which may have a radical R5a, or together with R5 is C1-C3-alkylene, where R5 together with R5a, where present, are a bond or C1-C3-alkylene; and where one of the following conditions is satisfied: R3 together with R4 is C1-C3-alkylene which may have a radical R5a; or R3 together with R5 is C1-C3-alkylene; or R4 together with R5 is C1-C3-alkylene where the radical A is different from phenyl when the radical B is phenyl or naphthyl; and medicaments which comprise such compounds and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.

    摘要翻译： 本发明涉及通式（I）的化合物，其中A，B，R1，R2和Het具有权利要求1中给出的含义; Y是下式的二价基团，其中D是C 1 -C 3 - 亚烷基，其中D可以具有取代基R 5; R 3是氢，C 1 -C 8烷基或与R 4一起是可以具有基团R 5a的C 1 -C 3亚烷基，或与R 5一起为C 1 -C 3 - 亚烷基，并且R 4是氢，C 1 -C 8 - 烷基或与 R 3是可以具有基团R 5a的C 1 -C 3亚烷基，或与R 5一起为C 1 -C 3 - 亚烷基，其中R 5与存在的R a a为键或C 1 -C 3 - 亚烷基; 并且其中满足以下条件之一：R 3与R 4一起可以具有基团R 5a的C 1 -C 3 - 亚烷基; 或R 3与R 5一起为C 1 -C 3 - 亚烷基; 或R 4与R 5一起为C 1 -C 3 - 亚烷基，其中基团B为苯基或萘基时，基团A不同于苯基; 以及包含这些化合物的药物及其用于预防和/或治疗加压素依赖性和/或催产素依赖性疾病的用途。