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16 条记录 (耗时 0.07 秒)

    Substituted diaza-spiro-pyridinone derivatives for use in MCH-1 mediated diseases
    14.
    发明授权
    Substituted diaza-spiro-pyridinone derivatives for use in MCH-1 mediated diseases 有权
    用于MCH-1介导的疾病的取代的二氮杂螺 - 吡啶酮衍生物

    公开(公告)号：US08158643B2

    公开(公告)日：2012-04-17

    申请号：US12444878

    申请日：2007-12-04

    申请人： José Ignacio Andrés-Gil ,  Manuel Jesús Alcázar-Vaca ,  Frank Matthias Dautzenberg ,  Joannes Theodorus Maria Linders

    发明人： José Ignacio Andrés-Gil ,  Manuel Jesús Alcázar-Vaca ,  Frank Matthias Dautzenberg ,  Joannes Theodorus Maria Linders

    IPC分类号： A61K31/438 ,  C07D215/02

    CPC分类号： C07D471/10 ,  C07D498/10

    摘要： The present invention concerns aryl and heteroaryl substituted diaza-spiro-pyridinone derivatives having antagonistic melanin-concentrating hormone (MCH) activity, in particular MCH-1 activity according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of psychiatric disorders, including but not limited to anxiety, eating disorders, mood disorders, such as bipolar disorders and depression, psychoses, such as schizophrenia, and sleeping disorders; obesity; diabetes; sexual disorders and neurological disorders.

    摘要翻译： 本发明涉及具有拮抗性黑色素浓缩激素（MCH）活性的芳基和杂芳基取代的二氮 - 螺 - 吡啶酮衍生物，特别是根据通式（I）的MCH-1活性，其药学上可接受的酸或碱加成盐， N-氧化物形式或其季铵盐，其中变量在权利要求1中定义。它还涉及它们的制备方法，包含它们的组合物及其作为药物的用途。 根据本发明的化合物可用于预防和/或治疗精神病学障碍，包括但不限于焦虑，进食障碍，情绪障碍，例如双相性精神障碍和抑郁症，精神病如精神分裂症和睡眠障碍; 肥胖; 糖尿病; 性障碍和神经障碍。

    Substituted amino isoxazoline derivatives and their use as anti-depressants
    16.
    发明授权
    Substituted amino isoxazoline derivatives and their use as anti-depressants 有权

    公开(公告)号：US07265103B2

    公开(公告)日：2007-09-04

    申请号：US10510220

    申请日：2003-03-27

    申请人： José Ignacio Andrés-Gil ,  Manuel Jesús Alcázar-Vaca ,  Margaretha Henrica Maria Bakker ,  Ana Isabel De Lucas Olivares

    发明人： José Ignacio Andrés-Gil ,  Manuel Jesús Alcázar-Vaca ,  Margaretha Henrica Maria Bakker ,  Ana Isabel De Lucas Olivares

    IPC分类号： A61K31/55 ,  A61K31/5377 ,  A61K31/496 ,  C07D498/04

    CPC分类号： C07D498/04 ,  C07D498/14

    摘要： The invention concerns substituted amino isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisozazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart of the tricyclic moiety with primary, secondary and/or tertiary amino groups, according to Formula (I) wherein X=CH2, N—R7, S or O, R1, R2 and R3 are certain specific substituents, with the proviso that at least one of R1 and R2 is an amino radical of formula N—R10R11 wherein R10 and R11 are each a variety of radicals, Pir is an optionally substituted piperidyl or piperazyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for the treatment of depression and/of anxiety and disorders of body weight. The compounds according to the invention have surprisingly been shown to have a serotonin (5-HT) reuptake inhibitor activity in combination with additional α2-adrenoceptor antagonist activity and show a strong anti-depressant activity without being sedative. Compounds according to the invention are also suitable for treating depression, anxiety and body weight disorders. The invention also relates to novel combination of substituted amino isoxazoline derivatives according to the invention with antidepressants, anxiolytics and/or antipsychotics to improve efficacy and/or onset of action.