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16 条记录 (耗时 0.049 秒)

    Substituted diaza-spiro-pyridinone derivatives for use in MCH-1 mediated diseases
    5.
    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。

    C6-and C9-substituted chromeno[4,3-c]isoxazoline derivatives and their use as anti-depressants
    6.
    发明授权
    C6-and C9-substituted chromeno[4,3-c]isoxazoline derivatives and their use as anti-depressants 有权
    C6-和C9-取代的色烯并[4,3-c]异恶唑啉衍生物及其作为抗抑郁剂的用途

    公开(公告)号：US07462717B2

    公开(公告)日：2008-12-09

    申请号：US10524989

    申请日：2003-08-19

    申请人： José Ignacio Andrés-Gil ,  Manuel Jesús Alcázar-Vaca ,  Maria Encarnacion Matesanz-Ballesteros ,  Margaretha Henrica Maria Bakker ,  Antonius Adrianus Hendrikus Petrus Megens

    发明人： José Ignacio Andrés-Gil ,  Manuel Jesús Alcázar-Vaca ,  Maria Encarnacion Matesanz-Ballesteros ,  Margaretha Henrica Maria Bakker ,  Antonius Adrianus Hendrikus Petrus Megens

    IPC分类号： A61K31/55 ,  A61K31/5377 ,  A61K31/496 ,  C07D498/04 ,  C07D413/00

    CPC分类号： C07D498/04

    摘要： The invention concerns substituted tricyclic isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on at least one of the C6- and C9-positions of the phenylpart of the tricyclic moiety with a selected radical, according to Formula (I) wherein X=CH2, N—R7, S or O, R1, R2, R14 and R15 are certain specific substituents, with the proviso that at least one of R14 and R15 is not hydrogen, Pir is preferably an optionally substituted piperidinyl or piperazinyl 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, anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders. The compounds according to the invention have surprisingly been shown to have a serotonine (5-HT) reuptake inhibitor activity in combination with additional α2-adrenoceptor antagonist activity and show a strong anti-depressant activity without being sedative. The invention also relates to novel combination of isoxazoline derivatives according to the invention with one or more other compounds selected from the group of antidepressants, anxiolytics, anti-psychotics and anti-Parkinson's disease drugs to improve efficacy and/or onset of action.

    摘要翻译： 本发明涉及取代的三环异恶唑啉衍生物，更具体地是三环二氢苯并吡喃恶唑啉，二氢喹诺酮异恶唑啉，二氢萘硫基异恶唑啉和二氢苯并噻唑并恶唑啉衍生物，其被三选择基团的苯基部分的C 6 - 和C 9位中的至少一个与选定的基团取代， ）其中X = CH 2，N-R 7，S或O，R 1，R 2，R 14和R 15是某些具体取代基，条件是R14和R15中的至少一个不是氢，Pir优选为任选取代的哌啶基或哌嗪基 基团和R 3表示任选取代的芳族双环或杂环系统，其包括最多6个原子长的部分或完全氢化的烃链，其中环系统连接到Pir基团，并且其可以含有一个或多个选自以下的杂原子： O，N和S; 其制备方法，包含它们的药物组合物及其作为药物的用途，特别是用于治疗抑郁症，焦虑症，运动障碍，精神病，帕金森病和体重障碍。 根据本发明的化合物令人惊奇地显示具有与另外的α2-肾上腺素受体拮抗剂活性组合的5-羟色胺（5-HT）再摄取抑制剂活性，并且在没有镇静作用的情况下表现出强烈的抗抑郁活性。 本发明还涉及根据本发明的异恶唑啉衍生物与一种或多种选自抗抑郁药，抗焦虑药，抗精神病药和抗帕金森病药物的其它化合物的新组合，以改善疗效和/或起效。