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    Imidazol-1-ylmethyl pyridazine derivatives
    32.
    发明授权
    Imidazol-1-ylmethyl pyridazine derivatives 失效
    咪唑-1-基甲基哒嗪衍生物

    公开(公告)号：US07122546B2

    公开(公告)日：2006-10-17

    申请号：US10680351

    申请日：2003-10-07

    Applicant: Linghong Xie ,  Bingsong Han ,  Yuelian Xu ,  George D. Maynard

    Inventor： Linghong Xie ,  Bingsong Han ,  Yuelian Xu ,  George D. Maynard

    IPC: C07D403/06 ,  C07D403/14 ,  A61K31/501 ,  A61P25/22 ,  A61P25/24

    CPC classification number: C07D409/14 ,  C07D401/14 ,  C07D403/06 ,  C07D417/14

    Abstract: The invention provides imidazol-1-ylmethyl pyridazine derivatives of the formula: that bind to GABAA receptors. In the above formula, R1, R2 R3, R4, R5, R6 and Ar are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals, and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).

    Abstract translation: 本发明提供下式的咪唑-1-基甲基哒嗪衍生物：其结合GABA A A受体。 在上式中，R 1，R 2，R 3，R 4，R 5， / SUB，R 6和Ar如本文所定义。 这样的化合物可用于在体内或体外调节配体与GABA A A受体的结合，并且特别可用于治疗人类中的各种中枢神经系统（CNS）紊乱，驯养伴侣动物 ，和牲畜。 本文提供的化合物可以单独施用或与一种或多种其它CNS剂组合施用，以增强其它CNS剂的作用。 还提供了用于治疗这种病症的药物组合物和方法，以及使用这种配体检测GABA A受体的方法（例如，受体定位研究）。

    Aminoalkyl substituted 5,6,7,8-tetrahydro-9H-pyridino [2, 3-B] indole and 5,6,7,8-tetrahydro-9H-pyrimidino [4, 5-B] indole derivatives: CRF1 specific ligands
    33.
    发明授权
    Aminoalkyl substituted 5,6,7,8-tetrahydro-9H-pyridino [2, 3-B] indole and 5,6,7,8-tetrahydro-9H-pyrimidino [4, 5-B] indole derivatives: CRF1 specific ligands 失效
    氨基烷基取代的5,6,7,8-四氢-9H-吡啶并[2,3-B]吲哚和5,6,7,8-四氢-9H-嘧啶并[4,5-B]吲哚衍生物：CRF1特异性配体

    公开(公告)号：US06291473B1

    公开(公告)日：2001-09-18

    申请号：US09283723

    申请日：1999-04-01

    Applicant: Raymond F. Horvath ,  James W. Darrow ,  George D. Maynard

    Inventor： Raymond F. Horvath ,  James W. Darrow ,  George D. Maynard

    IPC: A61K31405

    CPC classification number: C07D471/04 ,  C07D487/04

    Abstract: Disclosed are compounds of the formula: wherein Ar, R1, W, X and m are substituents as defined herein. These compounds are modulators of CRF receptors and are therefore useful for treating affective disorder, anxiety, depression, headache, irritable bowel syndrome, post-traumatic stress disorder, supranuclear palsy, immune suppression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa or other feeding disorder, drug addiction, drug or alcohol withdrawal symptoms, inflammatory diseases, cardiovascular or heart-related diseases, fertility problems, human immunodeficiency virus infections, hemorrhagic stress, obesity, infertility, head and spinal cord traumas, epilepsy, stroke, ulcers, amyotrophic lateral sclerosis, hypoglycemia or a disorder the treatment of which can be effected or facilitated by antagonizing CRF, including but not limited to disorders induced or facilitated by CRF, in mammals, comprising: administering to the mammal a therapeutically effective amount of a compound of Formula I.

    Abstract translation: 公开了下式的化合物：其中Ar，R 1，W，X和m是如本文所定义的取代基。这些化合物是CRF受体的调节剂，因此可用于治疗情感障碍，焦虑症，抑郁症，头痛，肠易激综合征， 创伤性应激障碍，核上性麻痹，免疫抑制，阿尔茨海默病，胃肠道疾病，神经性厌食症或其他进食障碍，药物成瘾，药物或酒精戒断症状，​​炎症性疾病，心血管或心脏相关疾病，生育问题，人类免疫缺陷病毒感染， 出血性压力，肥胖症，不育症，头部和脊髓创伤，癫痫，中风，溃疡，肌萎缩性侧索硬化，低血糖或疾病，其治疗可以通过拮抗CRF来实现或促进，包括但不限于由 CRF，在哺乳动物中，包括：向哺乳动物施用治疗有效量的ac 一级方程式

    Substituted pyrrolidin-3-yl-alkyl-piperidines
    38.
    发明授权
    Substituted pyrrolidin-3-yl-alkyl-piperidines 失效
    取代的吡咯烷-3-基 - 烷基 - 哌啶

    公开(公告)号：US5635510A

    公开(公告)日：1997-06-03

    申请号：US332027

    申请日：1994-10-31

    Applicant: Timothy P. Burkholder ,  Elizabeth M. Kudlacz ,  George D. Maynard

    Inventor： Timothy P. Burkholder ,  Elizabeth M. Kudlacz ,  George D. Maynard

    IPC: C07D401/06 ,  C07D401/14 ,  C07D409/14 ,  C07D471/10 ,  A61K31/44 ,  A61K31/445

    CPC classification number: C07D401/06 ,  C07D401/14 ,  C07D409/14 ,  C07D471/10

    Abstract: The present invention relates to substituted pyrrolidinyl-3-yl-alkyl-piperidines, their stereoisomers, and pharmaceutically acceptable salts thereof and processes for preparation of the same. The compounds of the present invention are useful in their pharmacological activities such as tachykinin antagonism, especially substance P and neurokinin A antagonism, and the like. Compounds having the property of tachykinin antagonism are indicated for conditions associated with neurogenic inflammation and other diseases described herein.

    Abstract translation: 本发明涉及取代的吡咯烷基-3-基 - 烷基 - 哌啶，其立体异构体及其药学上可接受的盐及其制备方法。 本发明的化合物可用于其药理活性，如速激肽拮抗作用，特别是P物质和神经激肽A拮抗作用等。 表示具有速激肽拮抗作用的化合物用于与神经源性炎症和本文所述的其它疾病相关的病症。

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