5-(2-phenoxyethyloxy)indole

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 5-(2-phenoxyethyloxy)indole
• 英文别名: 5-(2-phenoxyethoxy)-1H-indole
• 化学式: C₁₆H₁₅NO₂
• 分子量: 253.301
• InChiKey: CRJAGJQFPQEDGO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  19
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  34.2
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  2-苯氧乙基溴 、 5-羟基吲哚 生成 5-(2-phenoxyethyloxy)indole
  参考文献：
  名称：

  Positive modulators of nicotinic receptor agonists

  摘要：

  本发明的化合物I式中，其中R1、R2、R3和R4的定义如规范中所述，其对映异构体，其药学上可接受的盐，制备它们的方法，包含它们的制药组合物以及它们在治疗中的应用，特别是用于治疗与尼古丁传递减少有关的疾病。本发明的化合物增强了尼古丁受体激动剂的功效。

  公开号：

  US06750242B1

文献信息

• POSITIVE MODULATORS OF NICOTINIC RECEPTOR AGONISTS
  申请人：AstraZeneca AB

  公开号：EP1230216A1

  公开（公告）日：2002-08-14
• US6750242B1
  申请人：——

  公开号：US6750242B1

  公开（公告）日：2004-06-15
• [EN] POSITIVE MODULATORS OF NICOTINIC RECEPTOR AGONISTS<br/>[FR] MODULATEURS POSITIFS DES AGONISTES DU RECEPTEUR NICOTINIQUE
  申请人：ASTRAZENECA AB

  公开号：WO2001032619A1

  公开（公告）日：2001-05-10

  A compound of Formula (I) wherein R?1 and R3¿ independently represent hydrogen, or C¿1?-C4 alkyl; R?2¿ represents hydrogen, C¿1?-C4 alkyl, or CH2CN; R?4¿ represents hydrogen, C¿1?-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, CH2C(W)=CH2, (CH2) nAr, CH2CH=CHAr, CH2COPh, CH2CONHAr, C(U)NH(CH2) mAr, or (CH2) dY(CH2) eAr; U represents O, or S; W represents halogen; X and Y independently represent O, S, or NR?5; R5¿ represents hydrogen, C¿1?-C4 alkyl, C2-C4 alkenyl; or together R?3 and R5¿ form a ring; n and m independently are 0-4; d is 1-3; e is 0-1; Ar represents phenyl, naphthyl or 5- or 6-membered heterocyclic ring containing zero to four nitrogens, zero to one sulfurs and zero to one oxygens; Ar is optionally substituted with one or more substituents selected from: hydrogen, halogen, C¿1?-C4 alkyl, C2-C4 alkenyl, C2-C?4¿ alkynyl CN, NO¿2?, CF3, OR?6, NR7R8, COOR9; R6, R7 and R8¿ are independently hydrogen, C¿1?-C4 alkyl, aryl, heteroaryl, C(O)R?10¿, C(O)NHR11, SO2R?12, or; R7 and R8¿ together may be (CH¿2?)jQ(CH2) k where; Q is O, S, NR?13¿ or a bond; j is 2-4; k is 0-2; R?9, R10, R11, R12 and R13¿ are independently hydrogen, C¿1?-C4 alkyl, aryl or heteroaryl; or an enantiomer thereof, and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially for treatment of conditions associated with reductions in nicotinic transmission. The compounds of the invention enhance the efficacy of agonists at nicotinic receptors.