1-(1H-imidazol-2-ylmethyl)-5-phenoxy-1,2,3,4-tetrahydro-quinoline | 1023913-69-0

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 1-(1H-imidazol-2-ylmethyl)-5-phenoxy-1,2,3,4-tetrahydro-quinoline
• 英文别名: 1-(1H-imidazol-2-ylmethyl)-5-phenoxy-3,4-dihydro-2H-quinoline
• CAS: 1023913-69-0
• 化学式: C₁₉H₁₉N₃O
• 分子量: 305.379
• InChiKey: PTNAVYRZNAXCBK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  23
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  41.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  5-Phenoxy-1,2,3,4-tetrahydro-quinoline 、 2-咪唑甲醛 、 氰基硼氢化钠 在 氯化锌 作用下， 以 甲醇 为溶剂， 生成 1-(1H-imidazol-2-ylmethyl)-5-phenoxy-1,2,3,4-tetrahydro-quinoline
  参考文献：
  名称：

  Substituted-2-imidazoles

  摘要：

  本发明涉及式I的化合物，其中R1选自氢和较低的烷基组；每个R2独立地选自氢和较低的烷基组；每个R3独立地选自氢、较低的烷基、较低的烷氧基、苯氧基、苄氧基、卤素和被卤素取代的较低烷基；X选自-CH2-、-CH-和-O-组；Y选自-CH2-、-CH-和键，但当X为-O-时，Y不能是键；Z选自-CH2-和-CH-组；m为0、1或2；n为0、1或2；以及这些化合物的药学可接受的酸加盐。本发明还涉及制备这些化合物的方法，包含这样的化合物或其药学可接受的酸加盐的组合物，以及通过向需要此类治疗的患者施用这种化合物或其药学可接受的酸加盐来治疗患病或障碍的方法。

  公开号：

  US07834044B2

文献信息

• SUBSTITUTED-2-IMIDAZOLES
  申请人：Galley Guido

  公开号：US20080113980A1

  公开（公告）日：2008-05-15

  The present invention relates to compounds of formula I wherein R 1 is selected from the group consisting of hydrogen and lower alkyl; each R 2 is independently selected from the group consisting of hydrogen and lower alkyl; each R 3 is independently selected from the group consisting of hydrogen, lower alkyl, lower alkoxy, phenyloxy, benzyloxy, halogen and lower alkyl substituted by halogen; X is selected from the group consisting of —CH 2 —, —CH— and —O—; Y is selected from the group consisting of —CH 2 —, —CH— and a bond with the proviso that, when X is —O—, Y may not be a bond; Z is selected from the group consisting of —CH 2 — and —CH—; m is 0, 1 or 2; and n is 0, 1 or 2; and to pharmaceutically-acceptable acid addition salts of such compounds. The invention relates also to processes for preparing such compounds, compositions comprising such a compound or a pharmaceutically-acceptable acid addition salt thereof, and a method of treating a disease or disorder in a patient comprising administering such a compound, or pharmaceutically-acceptable acid addition salt thereof, to a patient in need of such treatment.

  本发明涉及公式I的化合物，其中R1选择自氢和较低烷基的群体；每个R2独立选择自氢和较低烷基的群体；每个R3独立选择自氢、较低烷基、较低烷氧基、苯氧基、苯甲氧基、卤素和被卤素取代的较低烷基的群体；X选择自—CH2—、—CH—和—O—的群体；Y选择自— —、—CH—和键的群体，但当X为—O—时，Y不能是键；Z选择自— —和—CH—的群体；m为0、1或2；n为0、1或2；以及该类化合物的药学上可接受的酸盐。本发明还涉及制备这种化合物的方法、包含这种化合物或其药学上可接受的酸盐的组合物，以及一种治疗患者疾病或障碍的方法，包括将这种化合物或其药学上可接受的酸盐用于需要此类治疗的患者的治疗中。
• SUBSTITUTED 4-IMIDAZOLES
  申请人：Galley Guido

  公开号：US20080139533A1

  公开（公告）日：2008-06-12

  The present invention relates to a compound of formula I, wherein R 1 is selected from the group consisting of hydrogen and lower alkyl; each R 2 is independently selected from the group consisting of hydrogen and lower alkyl; each R 3 is independently selected from the group consisting of hydrogen, lower alkyl, lower alkoxy, phenyloxy, benzyloxy, halogen and lower alkyl substituted by halogen; R 4 is selected from the group consisting of hydrogen and lower alkyl; X is selected from the group consisting of —CH 2 —, —CH— and —O—; Y is selected from the group consisting of —CH 2 —, —CH 2 CH 2 —, —CH— and a bond; with the proviso that, when X is —O—, Y is —CH 2 —; Z is selected from the group consisting of —CH 2 — and —CH—; m is 1 or 2; and n is 1 or 2. The invention relates also to a pharmaceutically-acceptable acid-addition salt of such a compound, methods for making the compound, and a composition comprising such a compound. It has been found that the compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1.

  本发明涉及一种化合物式I，其中R1选自氢和低碳基的群组；每个R2独立地选自氢和低碳基的群组；每个R3独立地选自氢、低碳基、低烷氧基、苯氧基、苄氧基、卤素和被卤素取代的低碳基的群组；R4选自氢和低碳基的群组；X选自—CH2—、—CH—和—O—的群组；Y选自— —、— —、—CH—和键的群组；但当X为—O—时，Y为— —；Z选自— —和—CH—的群组；m为1或2；n为1或2。本发明还涉及该化合物的药学可接受的酸加成盐、制备该化合物的方法和包含该化合物的组合物。已经发现，式I化合物对痕量胺相关受体（TAARs）具有良好的亲和力，特别是对TAAR1。
• SUBSTITUTED 2-IMIDAZOLES AS MODULATORS OF THE TRACE AMINE ASSOCIATED RECEPTORS
  申请人：F.HOFFMANN-LA ROCHE AG

  公开号：EP2086959A1

  公开（公告）日：2009-08-12
• IONTOPHORETIC DELIVERY SYSTEM
  申请人：Rivlin Alex Savelij

  公开号：US20110264029A1

  公开（公告）日：2011-10-27

  Methods, systems and other embodiments associated with administering ionotophoretic medicines are presented. A method of administering ionotophoretic medicines includes applying a voltage across a body tissue and an iontophoretic solution including medicine. At least some of the iontophoretic solution including medicine is then injected into the body tissue without requiring the iontophoretic transportation of the iontophoretic solution including medicine through the skin. The iontophoretic solution is typically injected while the voltage is applied. The voltage causes an ionic current of iontophoretic medicine to flow which disperses the medicine within the body tissue toward body tissue connected to the voltage.
• US7834044B2
  申请人：——

  公开号：US7834044B2

  公开（公告）日：2010-11-16