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41 条记录 (耗时 0.032 秒)

    Triazole compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor
    32.
    发明授权
    Triazole compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 失效
    适用于治疗对多巴胺D3受体调节作出反应的三唑化合物

    公开(公告)号：US06919342B2

    公开(公告)日：2005-07-19

    申请号：US10860823

    申请日：2004-06-04

    申请人： Andreas Haupt ,  Roland Grandel ,  Wilfried Braje ,  Hervé Geneste ,  Karla Drescher ,  Dorothea Starck ,  Hans-Jürgen Teschendorf

    发明人： Andreas Haupt ,  Roland Grandel ,  Wilfried Braje ,  Hervé Geneste ,  Karla Drescher ,  Dorothea Starck ,  Hans-Jürgen Teschendorf

    IPC分类号： A61K31/506 ,  C07D403/12 ,  C07D403/14

    CPC分类号： C07D403/12

    摘要： The invention relates to triazole compounds of the general formula I wherein R1 is hydrogen or methyl, and R2 is C3-C4 alkyl or C1-C2 fluoroalkyl, as well as the physiologically tolerated acid addition salts of these compounds. The invention also relates to a pharmaceutical composition that comprises at least one triazole 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 triazole compound or physiologically tolerated acid addition salt of the formula I to a subject in need thereof.

    摘要翻译： 本发明涉及通式Ⅰ的三唑化合物，其中R 1是氢或甲基，R 2是C 3 -C 3 > 4个烷基或C 1 -C 2 - 氟代烷基，以及这些化合物的生理上耐受的酸加成盐。 本发明还涉及一种药物组合物，其包含至少一种式I的三唑化合物和/或其至少一种生理上耐受的酸加成盐，还涉及治疗有益于多巴胺D 3的病症的方法 受体拮抗剂或多巴胺D 3激动剂，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III的三唑化合物或生理耐受的酸加成盐。

    Pyridazine compounds as glycogen synthase kinase 3 inhibitors
    39.
    发明授权
    Pyridazine compounds as glycogen synthase kinase 3 inhibitors 有权

    公开(公告)号：US07994160B2

    公开(公告)日：2011-08-09

    申请号：US11988578

    申请日：2006-07-12

    申请人： Sean C. Turner ,  Margaretha Bakker ,  Roland Grandel ,  Michael Vierling

    发明人： Sean C. Turner ,  Margaretha Bakker ,  Roland Grandel ,  Michael Vierling

    IPC分类号： C07D487/04 ,  C07D471/14 ,  A61K31/55 ,  A61K31/551

    CPC分类号： C07D487/04 ,  C07D471/14

    摘要： Disclosed are pyridazine compounds of the formula I which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds: In formula I indicates a single bond or a double bond; X is O, S or N—R5; R1, R2 are independently selected from the group consisting of H, NH2, NH—C1-C6-alkyl, OH, ═O, (i.e. a carbonyl group), C1-C6-alkoxy, halogen, methyl, C2-C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-alkenyl, formyl, C1-C3-alkylcarbonyl, and an aromatic radical Ar, R1 and R2 together with the carbon atoms, to which they are attached, form a fused, saturated or unsaturated 5-, 6- or 7-membered C-bound carbocyclic or heterocyclic ring comprising 1 heteroatom, selected from nitrogen, oxygen and sulfur as ring member and 0, 1 or 2 further heteroatoms, independently selected from O, S and N, as ring members, wherein the fused ring is unsubstituted or may carry 1, 2 or 3 substituents selected, independently of each other, from the group of radicals R4 as defined below; R3 is hydrogen OH, halogen, CN, nitro, C1-C6-alkyl, fluorinated C1-C6-alkyl, C1-C6-hydroxyalkyl, C1-C6-alkoxy-C1-C6-alkyl, C2-C6-alkenyl, fluorinated C2-C6-alkenyl, C2-C6-alkynyl, C3-C7-cycloalkyl, fluorinated C3-C7-cycloalkyl, C1-C6-alkoxy, C1-C6-hydroxyalkoxy, C1-C6-alkoxy-C1-C6-alkoxy, fluorinated C1-C6-alkoxy, C1-C6-alkylthio, fluorinated C1-C6-alkylthio, C1-C6-alkylsulfinyl, fluorinated C1-C6-alkylsulfinyl, C1-C6-alkylsulfonyl, fluorinated C1-C6-alkylsulfonyl, C1-C6-alkylcarbonyl, fluorinated C1-C6-alkylcarbonyl, C1-C6-alkylcarbonylamino, fluorinated C1-C6-alkylcarbonylamino, carboxy, C1-C6-alkyloxycarbonyl, fluorinated C1-C6-alkoxycarbonyl, NRaRb, C(O)—NReRf, NH—C(O)—NReRf, NRaRb—C1-C6-alkylene, O—NRaRb, etc. and wherein R4 and R5 are as defined in the specification and the claims.

    Pyridazine Compounds as Glycogen Synthase Kinase 3 Inhibitors
    40.
    发明申请
    Pyridazine Compounds as Glycogen Synthase Kinase 3 Inhibitors 有权

    公开(公告)号：US20090325937A1

    公开(公告)日：2009-12-31

    申请号：US11988578

    申请日：2006-07-12

    申请人： Sean C. Turner ,  Margaretha Bakker ,  Roland Grandel ,  Michael Vierling

    发明人： Sean C. Turner ,  Margaretha Bakker ,  Roland Grandel ,  Michael Vierling

    IPC分类号： A61K31/5513 ,  C07D487/04 ,  A61P25/28

    CPC分类号： C07D487/04 ,  C07D471/14

    摘要： Disclosed are pyridazine compounds of the formula I which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds: In formula I indicates a single bond or a double bond; X is O, S or N—R5; R1, R2 are independently selected from the group consisting of H, NH2, NH—C1-C6-alkyl, OH, ═O, (i.e. a carbonyl group), C1-C6-alkoxy, halogen, methyl, C2-C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-alkenyl, formyl, C1-C3-alkylcarbonyl, and an aromatic radical Ar, R1 and R2 together with the carbon atoms, to which they are attached, form a fused, saturated or unsaturated 5-, 6- or 7-membered C-bound carbocyclic or heterocyclic ring comprising 1 heteroatom, selected from nitrogen, oxygen and sulfur as ring member and 0, 1 or 2 further heteroatoms, independently selected from O, S and N, as ring members, wherein the fused ring is unsubstituted or may carry 1, 2 or 3 substituents selected, independently of each other, from the group of radicals R4 as defined below; R3 is hydrogen OH, halogen, CN, nitro, C1-C6-alkyl, fluorinated C1-C6-alkyl, C1-C6-hydroxyalkyl, C1-C6-alkoxy-C1-C6-alkyl, C2-C6-alkenyl, fluorinated C2-C6-alkenyl, C2-C6-alkynyl, C3-C7-cycloalkyl, fluorinated C3-C7-cycloalkyl, C1-C6-alkoxy, C1-C6-hydroxyalkoxy, C1-C6-alkoxy-C1-C6-alkoxy, fluorinated C1-C6-alkoxy, C1-C6-alkylthio, fluorinated C1-C6-alkylthio, C1-C6-alkylsulfinyl, fluorinated C1-C6-alkylsulfinyl, C1-C6-alkylsulfonyl, fluorinated C1-C6-alkylsulfonyl, C1-C6-alkylcarbonyl, fluorinated C1-C6-alkylcarbonyl, C1-C6-alkylcarbonylamino, fluorinated C1-C6-alkylcarbonylamino, carboxy, C1-C6-alkyloxycarbonyl, fluorinated C1-C6-alkoxycarbonyl, NRaRb, C(O)—NReRf, NH—C(O)—NReRf, NRaRb—C1-C6-alkylene, O—NRaRb, etc. and wherein R4 and R5 are as defined in the specification and the claims.