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    C6-and C9-substituted chromeno[4,3-c]isoxazoline derivatives and their use as anti-depressants
    2.
    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。

    C-substituted tricyclic isoxazoline derivatives and their use as anti-depressants
    5.
    发明授权
    C-substituted tricyclic isoxazoline derivatives and their use as anti-depressants 有权
    C-取代三环异恶唑啉衍生物及其作为抗抑郁剂的用途

    公开(公告)号：US07465741B2

    公开(公告)日：2008-12-16

    申请号：US10524197

    申请日：2003-08-12

    申请人： José Ignacio Andrés-Gil ,  José Manuel Bartolomé-Nebreda ,  Rosa Maria Alvarez-Escobar ,  Margaretha Henrica Maria Bakker ,  Antonius Adrianus Hendrikus Petrus Megens

    发明人： José Ignacio Andrés-Gil ,  José Manuel Bartolomé-Nebreda ,  Rosa Maria Alvarez-Escobar ,  Margaretha Henrica Maria Bakker ,  Antonius Adrianus Hendrikus Petrus Megens

    IPC分类号： A61K31/44 ,  C07D401/00 ,  C07D491/00 ,  C07D498/00 ,  C07D515/00 ,  C07D513/00

    CPC分类号： C07D498/04

    摘要： The invention concerns substituted tricyclic isoxazoline derivatives according to Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart of the tricyclic moiety with at least one radical that is attached to the phenyl radical by a carbon-carbon bond as well as processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for treating depression, anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders including anorexia nervosa and bulimia, wherin all variables are defined in claim 1. (I) The compounds have surprisingly been shown to have selective serotonine (5-HT) reuptake inhibitor activity in combination with additional α2-adrenocptor antagonist activity and show a strong antidepressant and/or anxiolytic activity and/or antipsychotic and/or a body weight control activity without being sedative. Also, in view of their selective serotonine (5-HT) reuptake inhibitor as well as α2-adrenoceptor antagonist activity, compounds according to the invention are also suitable for treatment and/or prophylaxis in diseases where either one of the activities alone or the combination of said activities may be of therapeutic use.

    摘要翻译： 本发明涉及取代的式（I）三环异恶唑啉衍生物，其药学上可接受的酸或碱加成盐，其立体化学异构形式及其N-氧化物形式，更特别地三环二氢苯并吡喃恶唑啉，二氢喹啉基异恶唑啉，二氢萘并恶唑啉和二氢苯并噻喃并恶唑啉衍生物取代 在具有至少一个通过碳 - 碳键连接到苯基的基团的三环部分的苯基上，以及它们的制备方法，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，运动障碍，精神病，帕金森病和包括神经性厌食症和贪食症的体重障碍，所有变量都在权利要求1中定义。（I）化合物令人惊奇地显示具有选择性5-羟色胺（5-HT）再摄取抑制剂活性 组合 具有额外的α2-肾上腺素能拮抗剂活性，并且显示强的抗抑郁药和/或抗焦虑活性和/或抗精神病和/或体重控制活性而不需要镇静。 此外，考虑到它们的选择性5-羟色胺再摄取抑制剂以及α2-肾上腺素能受体拮抗剂活性，根据本发明的化合物也适用于治疗和/或预防疾病，其中单独的一种活性或组合 的所述活动可能具有治疗用途。

    Substituted amino isoxazoline derivatives and their use as anti-depressants
    7.
    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.