6-{4-[2-(4-Benzhydryl-piperazin-1-yl)-ethyl]-phenyl}-pyridin-2-ylamine

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 6-{4-[2-(4-Benzhydryl-piperazin-1-yl)-ethyl]-phenyl}-pyridin-2-ylamine
• 英文别名: 6-[4-[2-(4-Benzhydrylpiperazin-1-yl)ethyl]phenyl]pyridin-2-amine
• 化学式: C₃₀H₃₂N₄
• 分子量: 448.611
• InChiKey: XHLWQHUDZMTMJK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.5
• 重原子数：
  34
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  45.4
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  二苯甲基哌嗪 以54%的产率得到6-{4-[2-(4-Benzhydryl-piperazin-1-yl)-ethyl]-phenyl}-pyridin-2-ylamine
  参考文献：
  名称：

  6-phenyl-pyridin-2-ylamine derivatives

  摘要：

  本发明涉及具有一定活性的一类6-苯基-吡啶-2-胺衍生物，其作为一氧化氮合酶（NOS）抑制剂，以及含有它们的药物组合物，以及它们在治疗和预防中枢神经系统疾病中的用途。

  公开号：

  US06235747B1

文献信息

• PHARMACEUTICAL USES FOR NOS INHIBITORS
  申请人：——

  公开号：US20020151572A1

  公开（公告）日：2002-10-17

  The present invention relates to new pharmaceutical uses for compounds that exhibit activity as nitric oxide synthase (NOS) inhibitors. Specifically, it relates to the use of NOS inhibitors, particularly selective neuronal NOS (N-NOS) inhibitors: (a) alone or in combination with another active agent for the treatment of psoriasis; (b) in combination with an antiinflammatory agent for the treatment of inflammatory disorders; (c) in combination with a narcotic analgesic (e.g., opiates such as morphine or demerol) for the treatment of pain; (d) alone or in combination with other active agents for the enhancement of cognition; and (e) alone or in combination with other active agents for the treatment of sleep disorders such as apnea, narcolepsy and insomnia.

  本发明涉及表现为一氧化氮合酶（NOS）抑制剂活性的化合物的新药用途。具体而言，涉及使用NOS抑制剂，特别是选择性神经元NOS（N-NOS）抑制剂：（a）单独或与另一活性剂结合用于治疗牛皮癣；（b）与抗炎药物结合用于治疗炎症性疾病；（c）与麻醉镇痛剂（例如吗啡或度冷丁等阿片类药物）结合用于治疗疼痛；（d）单独或与其他活性剂结合用于增强认知功能；以及（e）单独或与其他活性剂结合用于治疗呼吸暂停、白天疲劳和失眠等睡眠障碍。
• New pharmaceutical combinations for NOS inhibitors
  申请人：Pfizer Inc

  公开号：US20040229911A1

  公开（公告）日：2004-11-18

  The present invention relates to new pharmaceutical uses for compounds that exhibit activity as nitric oxide synthase (NOS) inhibitors. Specifically, it relates to the use of NOS inhibitors, particularly selective neuronal NOS (nNOS) inhibitors, alone or in combination with another active agent, in particular, either an SSRI or an NK-1 receptor antagonist, for the treatment of disorders or conditions the treatment which can be effected or facilitated by altering circadian rhythms. Examples of such disorders and conditions are blindness, obesity, seasonal affective disorder, bipolar disorder; jet lag, circadian sleep rhythms disorder, sleep deprivation, parasomnias, REM sleep disorders, hypersomnia, sleep-wake cycle disorders, narcolepsy and sleep disorders associated with shift work or irregular work schedules; nocturnal enuresis, and restless-legs syndrome.

  本发明涉及表现为一氧化氮合酶（NOS）抑制剂活性的化合物的新药物用途。具体地，涉及使用NOS抑制剂，特别是选择性神经元NOS（nNOS）抑制剂，单独或与另一种活性剂联合使用，特别是SSRI或NK-1受体拮抗剂，用于治疗可以通过改变昼夜节律来达到或促进治疗的疾病或病况。这些疾病和病况的例子包括失明、肥胖症、季节性情感障碍、双相情感障碍、时差反应、昼夜节律睡眠障碍、睡眠剥夺、睡眠障碍、REM睡眠障碍、嗜睡症、睡眠-觉醒周期障碍、嗜睡症和与轮班工作或不规则工作时间表相关的睡眠障碍、夜尿症和不宁腿综合症。
• [EN] NEW PHARMACEUTICAL COMBINATIONS FOR NOS INHIBITORS<br/>[FR] NOUVELLES COMBINAISONS PHARMACEUTIQUES POUR LES INHIBITEURS DE NOS
  申请人：PFIZER PROD INC

  公开号：WO2000071107A2

  公开（公告）日：2000-11-30

  The present invention relates to new pharmaceutical uses for compounds that exhibit activity as nitric oxide synthase (NOS) inhibitors. Specifically, it relates to the use of NOS inhibitors, particularly selective neuronal NOS (nNOS) inhibitors, alone or in combination with another active agent, in particular, either an SSRI or an NK-1 receptor antagonist, for the treatment of disorders or conditions the treatment which can be effected or facilitated by altering circadian rhythms. Examples of such disorders and conditions are blindness, obesity, seasonal affective disorder, bipolar disorder, jet lag, circadian sleep rhythms disorder, sleep deprivation, parasomnias, REM sleep disorders, hypersomnia, sleep-wake cycle disorders, narcolepsy and sleep disorders associated with shift work or irregular work schedules; nocturnal enuresis, and restless-legs syndrome.

  本发明涉及表现为一氧化氮合酶（NOS）抑制剂的化合物的新药物用途。具体而言，涉及使用NOS抑制剂，特别是选择性神经元NOS（nNOS）抑制剂，单独或与另一活性剂，特别是SSRI或NK-1受体拮抗剂结合使用，治疗可以通过改变昼夜节律来实现或促进的疾病或状况。这些疾病和状况的例子包括失明，肥胖症，季节性情感障碍，双相情感障碍，时差反应，昼夜节律睡眠障碍，睡眠剥夺，睡眠障碍，REM睡眠障碍，嗜睡症，睡眠-清醒周期障碍，嗜睡症和与轮班或不规则工作时间表相关的睡眠障碍；夜尿症和不安腿综合症。
• [EN] 6-PHENYLPYRIDYL-2-AMINE DERIVATIVES<br/>[FR] DERIVES DE 6-PHENYLPYRIDYL-2-AMINES
  申请人：PFIZER INC.

  公开号：WO1997036871A1

  公开（公告）日：1997-10-09

  (EN) The present invention relates to certain 6-phenyl-pyridin-2-ylamine derivatives that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them and to their use in the treatment and prevention of central nervous system disorders.(FR) La présente invention, qui concerne certains dérivés de 6-phénylpyridyl-2-amines faisant preuve d'une activité d'inhibiteurs du monoxyde d'azote synthétase, concerne aussi des compositions pharmaceutiques contenant de tels dérivés. L'invention concerne également l'utilisation de ces compositions pharmaceutiques pour le traitement et la prévention de troubles du système nerveux central.

  该发明涉及某些6-苯基吡啶-2-基胺衍生物，其表现出一定的一氧化氮合酶（NOS）抑制剂活性，以及包含它们的制药组合物及其在治疗和预防中枢神经系统疾病中的使用。
• 6-phenylpyridyl-2-amine derivatives
  申请人：——

  公开号：US20010034348A1

  公开（公告）日：2001-10-25

  The present invention relates to certain 6-phenyi-pyridin-2-ylamine derivatives that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them and to their use in the treatment and prevention of central nervous system disorders.

  本发明涉及某些6-苯基吡啶-2-胺衍生物，其展示了作为一氧化氮合酶（NOS）抑制剂的活性，以及含有它们的制药组合物和它们在治疗和预防中枢神经系统疾病中的应用。