6-[4'-(4-Phenethyl-piperazin-1-ylmethyl)-biphenyl-4-yl]-pyridin-2-ylamine | 310433-39-7

• 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'-(4-Phenethyl-piperazin-1-ylmethyl)-biphenyl-4-yl]-pyridin-2-ylamine
• 英文别名: 6-[4-[4-[[4-(2-phenylethyl)piperazin-1-yl]methyl]phenyl]phenyl]pyridin-2-amine
• CAS: 310433-39-7
• 化学式: C₃₀H₃₂N₄
• 分子量: 448.611
• InChiKey: RLSCAFUCZAEEFS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.4
• 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：

  2-(2,5-dimethylpyrrolyl)-6-[4'-(4-phenethyl-piperazin-1-ylmethyl)-biphenyl-4-yl]-pyridine 在 盐酸 、 N2 、 盐酸羟胺 作用下， 以 乙醇 、 水 为溶剂， 以110 mg (55%)的产率得到6-[4'-(4-Phenethyl-piperazin-1-ylmethyl)-biphenyl-4-yl]-pyridin-2-ylamine
  参考文献：
  名称：

  6-phenylpyridyl-2-amine derivatives useful as NOS inhibitors

  摘要：

  本发明涉及公式中G、R1和R2如规范中所定义的6-苯基吡啶-2-胺衍生物，其表现为一氧化氮合酶（NOS）抑制剂的活性，以及包含它们的制药组合物，以及它们在中枢神经系统和其他疾病的治疗和预防中的使用。

  公开号：

  US06235750B1

文献信息

• 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。
• 6-Phenylpyridyl-2-amine derivatives useful as NOS inhibitors
  申请人：Pfizer Inc

  公开号：US20040142924A1

  公开（公告）日：2004-07-22

  The present invention relates to 6-phenyl-pyridin-2-ylamine derivatives of the formula 1 wherein G, R 1 and R 2 are defined as in the specification, 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 and other disorders.

  本发明涉及公式1中G、R1和R2如规范中定义的6-苯基-吡啶-2-基胺衍生物，它们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和它们在治疗和预防中枢神经系统和其他疾病中的应用。
• 6-PHENYLPYRIDYL-2-AMINE DERIVATIVES USEFUL AS NOS INHIBITORS
  申请人：PFIZER INC.

  公开号：EP0946512B1

  公开（公告）日：2003-10-08
• NEW PHARMACEUTICAL COMBINATIONS FOR NOS INHIBITORS
  申请人：Pfizer Products Inc.

  公开号：EP1178784A1

  公开（公告）日：2002-02-13