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    Substituted triazole derivatives
    1.
    发明申请
    Substituted triazole derivatives 失效
    取代的三唑衍生物

    公开(公告)号：US20070021475A1

    公开(公告)日：2007-01-25

    申请号：US11488837

    申请日：2006-07-18

    申请人： Luca Gobbi ,  Marius Hoener ,  Claus Riemer ,  Will Spooren

    发明人： Luca Gobbi ,  Marius Hoener ,  Claus Riemer ,  Will Spooren

    IPC分类号： A61K31/4192 ,  C07D249/16 ,  C07D407/02

    CPC分类号： C07D249/04 ,  C07D403/12

    摘要： The present invention relates to compounds of formula (I) wherein R1, R2 and R3 are as defined in the specification and to pharmaceutically suitable acid addition salts thereof. The invention includes all sterioisomeric forms, including individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. It has been found that the present compounds are selective allosteric positive modulators of the human NK-3 receptor for the treatment of anxiety, depression, bipolar disorders, Parkinson's disease, schizophrenia and pain.

    摘要翻译： 本发明涉及式（I）的化合物，其中R 1，R 2和R 3 3如说明书中所定义，并且与药学上 其合适的酸加成盐。 本发明包括所有的异构异构体形式，包括式（I）化合物的单独非对映异构体和对映异构体，以及其外消旋和非外消旋混合物。 已经发现，本发明化合物是用于治疗焦虑，抑郁，双相情感障碍，帕金森病，精神分裂症和疼痛的人NK-3受体的选择性变构的阳性调节剂。

    Substituted triazole compounds
    2.
    发明授权
    Substituted triazole compounds 失效
    取代三唑化合物

    公开(公告)号：US07268154B2

    公开(公告)日：2007-09-11

    申请号：US11488837

    申请日：2006-07-18

    申请人： Luca Claudio Gobbi ,  Marius Hoener ,  Claus Riemer ,  Will Spooren

    发明人： Luca Claudio Gobbi ,  Marius Hoener ,  Claus Riemer ,  Will Spooren

    IPC分类号： A61K31/4192 ,  A61K31/454 ,  C07D249/04 ,  C07D401/06

    CPC分类号： C07D249/04 ,  C07D403/12

    摘要： The present invention relates to compounds of formula (I) wherein R1, R2 and R3 are as defined in the specification and to pharmaceutically suitable acid addition salts thereof. The invention includes all sterioisomeric forms, including individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. It has been found that the present compounds are selective allosteric positive modulators of the human NK-3 receptor for the treatment of anxiety, depression, bipolar disorders, Parkinson's disease, schizophrenia and pain.

    摘要翻译： 本发明涉及式（I）的化合物，其中R 1，R 2和R 3 3如说明书中所定义，并且与药学上 其合适的酸加成盐。 本发明包括所有的异构异构体形式，包括式（I）化合物的单独非对映异构体和对映异构体，以及其外消旋和非外消旋混合物。 已经发现，本发明化合物是用于治疗焦虑，抑郁，双相情感障碍，帕金森病，精神分裂症和疼痛的人NK-3受体的选择性变构的阳性调节剂。

    Aminomethylpyrimidines as allosteric enhancers of the GABAB receptors
    3.
    发明申请
    Aminomethylpyrimidines as allosteric enhancers of the GABAB receptors 失效
    氨基甲基嘧啶作为GABAB受体的变构增强子

    公开(公告)号：US20050197337A1

    公开(公告)日：2005-09-08

    申请号：US11064046

    申请日：2005-02-23

    申请人： Pari Malherbe ,  Raffaello Masciadri ,  Eric Prinssen ,  Will Spooren ,  Andrew Thomas

    发明人： Pari Malherbe ,  Raffaello Masciadri ,  Eric Prinssen ,  Will Spooren ,  Andrew Thomas

    IPC分类号： C07D239/38 ,  C07D239/42 ,  C07D401/06 ,  C07D403/06 ,  C07D413/06 ,  C07D471/14 ,  C07D491/10 ,  A61K31/5377 ,  C07D413/02

    CPC分类号： C07D239/38 ,  C07D239/42 ,  C07D401/06 ,  C07D403/06 ,  C07D413/06 ,  C07D471/14 ,  C07D491/10

    摘要： The present invention relates to compounds of formula whereinX is —S— or —NH—; R3/R4 together with the N-atom to which they are attached form a non aromatic 5, 6 or 7 membered ring, which optionally contains in addition to the N-atom one additional heteroatom selected from the group consisting of O, S and N, and wherein the ring is optionally substituted by hydroxy, lower alkyl, lower alkoxy, —NR2, —CONR2, —CO-lower alkyl or benzyl; or R3/R4 form together with the N-atom to which they are attached a heterocyclic ring system, containing two or three rings and which optionally contains one or two additional heteroatoms selected from the group consisting of N and O and which has no more than 20 carbon atoms; and R, R1, R2, and R5 are as defined herein and to pharmaceutically suitable acid addition salts thereof. It has been found that the compounds of the invention are active on the GABAB receptor and therefore are useful for the treatment of anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, psychosis, panic disorder, posttraumatic stress disorders and gastro-intestinal disorders.

    摘要翻译： 本发明涉及下式的化合物其中X是-S-或-NH-; R 3和R 4连同它们所连接的N-原子一起形成非芳族的5,6或7元环，除了N - 一个另外的选自O，S和N的杂原子，并且其中该环任选地被羟基，低级烷基，低级烷氧基，-NR 2 - ， - CONR 2 -CO-低级烷基或苄基; 或R 3 3 R 4和它们所连接的N-原子一起形成杂环体系，其含有两个或三个环，并且任选地含有一个或两个另外的 选自N和O并且不超过20个碳原子的杂原子; R 1，R 2，R 2和R 5如本文所定义，以及其药学上合适的酸加成盐。 已经发现，本发明的化合物在GABA B受体上是有活性的，因此可用于治疗焦虑，抑郁，癫痫，精神分裂症，认知障碍，痉挛和骨骼肌僵硬，脊柱 脐带损伤，多发性硬化，肌萎缩性侧索硬化，脑性麻痹，神经性疼痛和与可卡因和尼古丁相关的渴望，精神病，恐慌症，创伤后应激障碍和胃肠道疾病。

    NK3 receptor in vivo assay
    4.
    发明申请
    NK3 receptor in vivo assay 审中-公开
    NK3受体体内测定

    公开(公告)号：US20070048225A1

    公开(公告)日：2007-03-01

    申请号：US11504241

    申请日：2006-08-14

    申请人： Will Spooren

    发明人： Will Spooren

    IPC分类号： A61K49/00 ,  A61K38/08

    CPC分类号： A61K49/0008 ,  G01N33/566

    摘要： The present invention relates to a method of assessing the in vivo potency of a NK3 receptor antagonist comprising: a) the non-human animal with the NK3 receptor antagonist of interest, b) treating an non-human animal with a NK3 R agonist treating, c) measuring the activity of the treated non-human animal, and d) correlating the effect of the antagonist of interest on the activity of the treated non-human animal with the in vivo potency of the antagonist.

    摘要翻译： 本发明涉及一种评估NK3受体拮抗剂的体内效力的方法，包括：a）非人动物与感兴趣的NK3受体拮抗剂，b）用NK3R激动剂治疗非人动物， c）测量所治疗的非人动物的活性，以及​​d）将感兴趣的拮抗剂对所治疗的非人动物的活性与拮抗剂的体内效力的影响相关联。

    METHODS FOR THE TREATMENT OF GERD WITH MGLUR5 ANTAGONISTS
    5.
    发明申请
    METHODS FOR THE TREATMENT OF GERD WITH MGLUR5 ANTAGONISTS 审中-公开
    用MGLUR5拮抗剂治疗GERD的方法

    公开(公告)号：US20090054490A1

    公开(公告)日：2009-02-26

    申请号：US12190614

    申请日：2008-08-13

    申请人： Georg Jaeschke ,  Sabine Kolczewski ,  Will Spooren ,  Eric Vieira

    发明人： Georg Jaeschke ,  Sabine Kolczewski ,  Will Spooren ,  Eric Vieira

    IPC分类号： A61K31/444 ,  A61K31/4439 ,  A61P1/04

    CPC分类号： A61K31/4439

    摘要： The present invention relates to methods for the treatment, prevention and/or delay of progression of gastro-esophageal reflux disease (GERD) by administering compounds that act as antagonists of metabotropic glutamate type-5 receptors (mGluR5 receptor antagonists), for example compounds of formula (I) wherein A, E, R1, R2, R2 and R4 are as defined in the specification.

    摘要翻译： 本发明涉及通过施用作为代谢型谷氨酸-5型受体拮抗剂（mGluR5受体拮抗剂）的化合物来治疗，预防和/或延缓胃食管反流病（GERD）进展的方法，例如化合物 式（I）其中A，E，R 1，R 2，R 2和R 4如说明书中所定义。

    Aminomethylpyrimidines as allosteric enhancers of the GABAB receptors
    6.
    发明授权
    Aminomethylpyrimidines as allosteric enhancers of the GABAB receptors 失效
    氨基甲基嘧啶作为GABAB受体的变构增强子

    公开(公告)号：US07351700B2

    公开(公告)日：2008-04-01

    申请号：US11064046

    申请日：2005-02-23

    申请人： Pari Malherbe ,  Raffaello Masciadri ,  Eric Prinssen ,  Will Spooren ,  Andrew William Thomas

    发明人： Pari Malherbe ,  Raffaello Masciadri ,  Eric Prinssen ,  Will Spooren ,  Andrew William Thomas

    IPC分类号： C07D239/38 ,  A61K31/506

    CPC分类号： C07D239/38 ,  C07D239/42 ,  C07D401/06 ,  C07D403/06 ,  C07D413/06 ,  C07D471/14 ,  C07D491/10

    摘要： The present invention relates to compounds of formula wherein X is —S— or —NH—; R3/R4 together with the N-atom to which they are attached form a non aromatic 5, 6 or 7 membered ring, which optionally contains in addition to the N-atom one additional heteroatom selected from the group consisting of O, S and N, and wherein the ring is optionally substituted by hydroxy, lower alkyl, lower alkoxy, —NR2, —CONR2, —CO-lower alkyl or benzyl; or R3/R4 form together with the N-atom to which they are attached a heterocyclic ring system, containing two or three rings and which optionally contains one or two additional heteroatoms selected from the group consisting of N and O and which has no more than 20 carbon atoms; and R, R1, R2, and R5 are as defined herein and to pharmaceutically suitable acid addition salts thereof. It has been found that the compounds of the invention are active on the GABAB receptor and therefore are useful for the treatment of anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, psychosis, panic disorder, posttraumatic stress disorders and gastro-intestinal disorders.

    摘要翻译： 本发明涉及下式的化合物其中X是-S-或-NH-; R 3和R 4连同它们所连接的N-原子一起形成非芳族的5,6或7元环，除了N - 一个另外的选自O，S和N的杂原子，并且其中该环任选地被羟基，低级烷基，低级烷氧基，-NR 2 - ， - CONR 2 -CO-低级烷基或苄基; 或R 3 3 R 4和它们所连接的N-原子一起形成杂环体系，其含有两个或三个环，并且任选地含有一个或两个另外的 选自N和O并且不超过20个碳原子的杂原子; R 1，R 2，R 2和R 5如本文所定义，以及其药学上合适的酸加成盐。 已经发现，本发明的化合物在GABA B受体上是有活性的，因此可用于治疗焦虑，抑郁，癫痫，精神分裂症，认知障碍，痉挛和骨骼肌僵硬，脊柱 脐带损伤，多发性硬化，肌萎缩性侧索硬化，脑性麻痹，神经性疼痛和与可卡因和尼古丁相关的渴望，精神病，恐慌症，创伤后应激障碍和胃肠道疾病。