methyl(2-(pyridin-3-yloxy)ethyl)amine | 228272-00-2

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: methyl(2-(pyridin-3-yloxy)ethyl)amine
• 英文别名: methyl(2-(3-pyridyloxy)ethyl)amine；N-methyl-2-(pyridin-3-yloxy)ethanamine；N-methyl-2-pyridin-3-yloxyethanamine
• CAS: 228272-00-2
• 化学式: C₈H₁₂N₂O
• 分子量: 152.196
• InChiKey: HKLZABNBARUZMN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  11
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  34.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  2-氯-1-(吡啶-3-氧基)乙烷 在 sodium hydroxide 、 甲胺 、 sodium chloride 作用下， 以 甲醇 为溶剂， 以0.253 g (12.0%)的产率得到methyl(2-(pyridin-3-yloxy)ethyl)amine
  参考文献：
  名称：

  Pharmaceutical compositions and methods for use

  摘要：

  对于容易受到或患有中枢神经系统疾病等疾病和疾病的患者，可以通过给予需要的患者芳基氧烷胺来进行治疗，包括吡啶氧烷胺和苯氧烷胺。示例化合物包括二甲基(2-(3-吡啶氧基)乙基)胺，二甲基(4-(3-吡啶氧基)丁基)胺，2-(3-吡啶氧基)乙基胺，4-(3-吡啶氧基)丁基胺，甲基(3-(5-甲氧基-3-吡啶氧基)丙基)胺，乙基(3-(3-吡啶氧基)丙基)胺，甲基(2-(3-吡啶氧基)乙基)胺，甲基(3-(6-甲基(3-吡啶氧基))丙基)胺，(3-(3-甲氧基苯氧基)丙基)甲基胺，(3-(5-氯(3-吡啶氧基))-1-甲基丙基)甲基胺，二甲基(3-(3-吡啶氧基)丙基)胺，3-(3-吡啶氧基)丙基胺，甲基(4-(3-吡啶氧基)丁基)胺，3-(5-氯-3-吡啶氧基)丙基胺，甲基(3-(5-异丙氧基-3-吡啶氧基)丙基)胺，(3-(5-氯(3-吡啶氧基))丙基)甲基胺，甲基(3-(5-(苯甲氧基)(3-吡啶氧基))丙基)胺，甲基(3-(2-甲基(3-吡啶氧基))丙基)胺，(甲基乙基)(3-(3-吡啶氧基)丙基)胺，苄基(3-(3-吡啶氧基)丙基)胺，环丙基(3-(3-吡啶氧基)-丙基)胺，甲基(1-甲基-3-(3-吡啶氧基)丙基)胺，甲基(3-(3-硝基苯氧基)丙基)胺，1-(3-氯丙氧基)-3-硝基苯，(3-(3-氨基苯氧基)丙基)甲基胺，二甲基(3-(3-(甲基氨基)-丙氧基)苯基)胺，甲基(3-三环[7.3.1.0<5,13>]十三烷-2-氧基丙基)胺，(3-苯并[3,4-d]1,3-二噁烷-5-氧基丙基)甲基胺，3-(4-哌啶氧基)吡啶和3-((3S)-3-吡咯烷氧基)吡啶。

  公开号：

  US06441006B2

文献信息

• [EN] QUINAZOLINE AND QUINOLINE COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS QUINAZOLINE ET QUINOLÉINE, ET UTILISATIONS DE CEUX-CI
  申请人：MILLENNIUM PHARM INC

  公开号：WO2016118565A1

  公开（公告）日：2016-07-28

  This invention provides compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein T, J, R, R4, Rq, o, RA, W and RB and subsets thereof are as described in the specification. The compounds are inhibitors of NAMPT and are thus useful for treating cancer, inflammatory conditions, and/or T-cell mediated autoimmune disease.

  这项发明提供了式（I）的化合物或其药用盐，其中T、J、R、R4、Rq、o、RA、W和RB及其子集如规范中所述。这些化合物是NAMPT的抑制剂，因此可用于治疗癌症、炎症性疾病和/或T细胞介导的自身免疫疾病。
• PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE
  申请人：——

  公开号：US20010014691A1

  公开（公告）日：2001-08-16

  Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof aryloxyalkylamines, including pyridyloxylalkylamines and phenoxyalkylamines. Exemplary compounds include dimethyl(2-(3-pyridyloxy)ethylamine, dimethyl(4-(3-pyridyloxy)butyl)amine, 2-(3-pyridyloxy)ethylamine, 4-(3-pyridyloxy)butylamine, methyl(3-(5-methoxy-3-pyridyloxy)propyl)amine, ethyl(3-(3-pyridyloxy)propyl)amine, methyl(2-(3-pyridyloxy)ethyl)amine, methyl(3-(6-methyl(3-pyridyloxy))propyl)amine, (3-(3-methoxyphenoxy)propyl)methylamine, (3-(5-chloro(3-pyridyloxy))-1-methylpropyl)methylamine, dimethyl(3-(3-pyridyloxy)propyl)amine, 3-(3-pyridyloxy)propylamine, methyl(4-(3-pyridyloxy)butyl)amine, 3-(5-chloro-3-pyridyloxy)propyl amine, methyl(3-(5-isopropoxy-3-pyridyloxy)propyl)amine, (3-(5-chloro(3-pyridyloxy))propyl) methylamine, methyl(3-(5-(phenylmethoxy)(3-pyridyloxy))propyl)amine, methyl(3-(2-methyl(3-pyridyloxy))propyl)amine, (methylethyl)(3-(3-pyridyloxy)propyl)amine, benzyl(3-(3-pyridyloxy)propyl)amine, cyclopropyl(3-(3-pyridyloxy)-propyl)amine, methyl(1-methyl-3-(3-pyridyloxy)propyl)amine, methyl(3-(3-nitrophenoxy)propyl)amine, 1-(3-chloropropoxy)-3-nitrobenzene, (3-(3-aminophenoxy)propyl)methylamine,dimethyl (3-(3-(methylamino)-propoxy)phenyl)amine, methyl(3-tricyclo[7.3.1.0<5,13>]tridec-2-yloxypropyl)amine, (3-benzo[3,4-d]1,3-dioxolan-5-yloxypropyl)methylamine, 3-(4-piperidinyloxy)pyridine and 3-((3S)-3-pyrrolidinyloxy)pyridine.

  患有或易受中枢神经系统疾病等病症和紊乱的患者，通过向需要的患者施用芳基氧烷胺类化合物进行治疗，包括吡啶氧烷胺和苯氧烷胺。示例化合物包括二甲基(2-(3-吡啶氧基)乙基)胺，二甲基(4-(3-吡啶氧基)丁基)胺，2-(3-吡啶氧基)乙基胺，4-(3-吡啶氧基)丁基胺，甲基(3-(5-甲氧基-3-吡啶氧基)丙基)胺，乙基(3-(3-吡啶氧基)丙基)胺，甲基(2-(3-吡啶氧基)乙基)胺，甲基(3-(6-甲基(3-吡啶氧基))丙基)胺，(3-(3-甲氧基苯氧基)丙基)甲基胺，(3-(5-氯(3-吡啶氧基))-1-甲基丙基)甲基胺，二甲基(3-(3-吡啶氧基)丙基)胺，3-(3-吡啶氧基)丙基胺，甲基(4-(3-吡啶氧基)丁基)胺，3-(5-氯-3-吡啶氧基)丙基胺，甲基(3-(5-异丙氧基-3-吡啶氧基)丙基)胺，(3-(5-氯(3-吡啶氧基))丙基)甲基胺，甲基(3-(5-(苯甲氧基)(3-吡啶氧基))丙基)胺，甲基(3-(2-甲基(3-吡啶氧基))丙基)胺，(甲基乙基)(3-(3-吡啶氧基)丙基)胺，苄基(3-(3-吡啶氧基)丙基)胺，环丙基(3-(3-吡啶氧基)-丙基)胺，甲基(1-甲基-3-(3-吡啶氧基)丙基)胺，甲基(3-(3-硝基苯氧基)丙基)胺，1-(3-氯丙氧基)-3-硝基苯，(3-(3-氨基苯氧基)丙基)甲基胺，二甲基(3-(3-(甲氨基)-丙氧基)苯基)胺，甲基(3-三环七叁.壹.零<5,13>三十二氧基丙基)胺，(3-苯并三.四-壹,三-二氧杂环戊氧基丙基)甲基胺，3-(4-哌啶氧基)吡啶和3-((3S)-3-吡咯啶氧基)吡啶。
• 薬学的組成物およびその使用
  申请人：ターガセプト,インコーポレイテッド

  公开号：JP2003500393A

  公开（公告）日：2003-01-07

  \n (57)【要約】\n中枢神経系障害などの病態および障害に感受性であるかそれを罹患している患者を、ピリジルオキシルアルキルアミン、フェノキシアルキルアミン、ピリジルチオールアルキルアミン、およびフェニルチオアルキルアミンを含むアリールオキシアルキルアミンおよびアリールチオアルキルアミンの必要時の患者への投与によって治療する。\n

  和芳基硫代烷基胺的治疗方法是在必要时给病人用药。\n
• Synthesis and biological evaluation of pyridine-modified analogues of 3-(2-Aminoethoxy)pyridine as novel nicotinic receptor ligands
  作者：Nan-Horng Lin、Liming Dong、William H Bunnelle、David J Anderson、Michael D Meyer

  DOI：10.1016/s0960-894x(02)00740-0

  日期：2002.11

  Analogues of the potent nicotinic receptor agonist 3-(2-aminoethoxy)pyridine substituted at the 5' and 6'-positions of the pyridine ring were synthesized and tested in vitro for nicotinic receptor binding activity (displacement of [H-3](-)cytisine from whole rat brain synaptic membranes). The substituted analogues exhibited K-i values ranging from 0.076 to 319 nM compared to a K-i value of 26 nM for compound 1. Among the compounds tested, 5'-vinyl-6'-chloro substituted I was the most potent. (C) 2002 Elsevier Science Ltd. All rights reserved.
• Synthesis and binding of 6,7,8,9-tetrahydro-5H-pyrido[3,4-d]azepine and related ring-opened analogs at central nicotinic receptors
  作者：Yun-Xing Cheng、Malgorzata Dukat、Matthew Dowd、Wolfgang Fiedler、Billy Martin、Mohamed  Imad Damaj、Richard A Glennon

  DOI：10.1016/s0223-5234(99)80051-8

  日期：1999.2

  6,7,8,9-Tetrahydro-5H-pyrido[3,4-d]azepine (5a) and its N-7-methyl derivative 5b were synthesized and evaluated as potential nicotinic acetylcholinergic receptor (nAChR) ligands. On the basis that 6,7,8,9-tetrahydro-5H-pyrido[3,4-c]azepine (4a), which binds at nAChRs with low affinity (K-i = 1100 nM), possesses an internitrogen distance (4.6 Angstrom) that may be less than optimal, we designed compound 5a due to its similar shape but longer internitrogen distance (5.5 Angstrom). Compound 5a (K-i = 45 nM) was found to bind with enhanced affinity. However, unlike what is seen with nornicotine/nicotine, N-methylation of 5a reduced affinity (5b; K-i = 268 nM) rather than enhancing it. The results suggest that 5 may interact at nicotine receptors in a manner that is somewhat different from that of nicotine. Ring-opening of the pyrido[3,4-d]azepine ring led to a series of 3-(2-aminoethyl)pyridines 21 that retained the affinity of the cyclic compound. Subsequent modification, including further chain lengthening (e.g. aminopropylpyridines 22) and introduction of unsaturation, ultimately led to the development of a series of 3-(2-aminethoxy)pyridines 27. Simple N-substituted derivatives of 27 were found to bind with K-i values of 20 to 35 nM. Because parallel structural changes in several series of related compounds did not result in parallel shifts in nAChR affinity, it is unlikely that all the investigated compounds bind in a similar fashion at these receptors. Nevertheless, some of these compounds represent novel classes of nAChR ligands. (C) Elsevier, Paris.