3-(3-butoxy-4-nitrophenoxy)-N,N-diethylpropan-1-amine | 1101057-75-3

• 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: 3-(3-butoxy-4-nitrophenoxy)-N,N-diethylpropan-1-amine
• CAS: 1101057-75-3
• 化学式: C₁₇H₂₈N₂O₄
• 分子量: 324.42
• InChiKey: UTOVFISSKIYMSP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  23
• 可旋转键数：
  11
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.65
• 拓扑面积：
  67.5
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  3-(3-butoxy-4-nitrophenoxy)-N,N-diethylpropan-1-amine 在 tin(II) chloride dihdyrate 、 三乙胺 作用下， 以 四氢呋喃 、 乙醇 、 二氯甲烷 为溶剂， 反应 4.0h， 生成 N-(2-butoxy-4-(3-(diethylamino)propoxy)phenyl)-3-(4-(4-methoxyphenoxy)phenyl)-1-methyl-1H-pyrazole-5-carboxamide
  参考文献：
  名称：

  Pyrazole-5-carboxamides, novel inhibitors of receptor for advanced glycation end products (RAGE)

  摘要：

  In an effort to develop novel inhibitors of receptor for advanced glycation end products (RAGE) for the treatment of Alzheimer's disease, a series of pyrazole-5-carboxamides were designed, synthesized and biologically evaluated. Analyses of the extensive structure activity relationship (SAR) led us to identify a 4-fluorophenoxy analog (40) that exhibited improved in vitro RAGE inhibitory activity and more favorable aqueous solubility than the parent 2-aminopyrimidine, 1. Surface plasmon resonance (SPR) and molecular docking study strongly supported the RAGE inhibitory activity of pyrazole-5-carboxamides. The brain A beta-lowering effect of 40 is also described. (C) 2014 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2014.03.072
• 作为产物：
  描述：

  5-氟-2-硝基苯酚 在 偶氮二甲酸二异丙酯 、 sodium hydride 、 三苯基膦 作用下， 以 四氢呋喃 、 mineral oil 为溶剂， 反应 27.0h， 生成 3-(3-butoxy-4-nitrophenoxy)-N,N-diethylpropan-1-amine
  参考文献：
  名称：

  신규한 헤테로아릴카르복스아마이드 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 포함하는 ＲＡＧＥ 수용체 관련 질환의 예방 또는 치료용 약학적 조성물

  摘要：

  This is the Chinese translation of the text you provided: 该发明涉及新型的杂环芳基羰胺衍生物或其药学上可接受的盐、其制备方法以及包含它的ＲＡＧＥ受体或乙酰胆碱酯酶活性相关疾病的预防或治疗药学组合物。根据本发明的杂环芳基羰胺衍生物化合物通过对RAGE受体的拮抗作用，抑制与RAGE受体结合并进入大脑的β-淀粉样蛋白导致神经细胞丧失，从而优越地抑制由此导致的β-淀粉样蛋白过度积累形成斑块的效果。此外，由于其出色的抑制分解乙酰胆碱这一对记忆功能至关重要的化学物质的乙酰胆碱酯酶的作用，因此，RAGE受体或乙酰胆碱酯酶活性相关疾病如阿尔茨海默病、脑血管性痴呆症、脑损伤所致痴呆、多发性硬化症痴呆、阿尔茨海默病和多发性硬化症痴呆的混合型或酒精性痴呆等包括痴呆、皮克病、克罗伊茨-雅各布病、甲状腺功能减退症、脑损伤所致帕金森病、亨廷顿病等的预防或治疗可以得到有效应用。

  公开号：

  KR101493882B1

文献信息

• Carboxamide derivatives as therapeutic agents
  申请人：——

  公开号：US20020193432A1

  公开（公告）日：2002-12-19

  This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, &bgr;-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

  这项发明提供了某些化合物、其制备方法、包括这些化合物的药物组合物以及它们在治疗人类或动物疾病中的用途。该发明的化合物可用作调节高级糖基化终产物受体（RAGE）与其配体之间相互作用的调节剂，这些配体包括高级糖基化终产物（AGEs）、S100/calgranulin/EN-RAGE、β-淀粉样蛋白和amphoterin，用于管理、治疗、控制或作为辅助治疗人类因RAGE引起的疾病。这些疾病或疾病状态包括急性和慢性炎症、糖尿病后期并发症的发展，如增加的血管通透性、肾病、动脉粥样硬化和视网膜病变，阿尔茨海默病的发展、勃起功能障碍以及肿瘤侵袭和转移。
• Carboxamide Derivatives as Therapeutic Agents
  申请人：Mjalli M.M. Adnan

  公开号：US20080119512A1

  公开（公告）日：2008-05-22

  This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

  这项发明提供了某些化合物、它们的制备方法、包含这些化合物的药物组合物以及它们在治疗人类或动物疾病中的应用。该发明的化合物可用作高级糖基化终产物（AGEs）、S100/calgranulin/EN-RAGE、β-淀粉样蛋白和amphoterin等配体与其受体——高级糖基化终产物受体（RAGE）之间相互作用的调节剂，并可用于管理、治疗、控制或作为辅助治疗人类因RAGE引起的疾病。这些疾病或疾病状态包括急性和慢性炎症、糖尿病晚期并发症的发展，如增加的血管通透性、肾病、动脉硬化和视网膜病变，阿尔茨海默病的发展、勃起功能障碍以及肿瘤侵袭和转移。
• Carboxamide Derivatives As Therapeutic Agents
  申请人：Mjalli Adnan M.M.

  公开号：US20100286197A1

  公开（公告）日：2010-11-11

  This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

  本发明提供了某些化合物、它们的制备方法、包括这些化合物的药物组合物，以及它们在治疗人类或动物疾病中的应用。该发明的化合物可用作高级糖基化终产物（AGEs）、S100/calgranulin/EN-RAGE、β-淀粉样蛋白和amphoterin等配体与其受体——高级糖基化终产物受体（RAGE）之间相互作用的调节剂，并用于治疗由RAGE引起的人类疾病的管理、治疗、控制或作为辅助治疗。这些疾病或疾病状态包括急性和慢性炎症、糖尿病晚期并发症的发展，如增加的血管通透性、肾病、动脉硬化和视网膜病变，阿尔茨海默病的发展、勃起功能障碍以及肿瘤侵袭和转移。
• CARBOXAMIDE DERIVATIVES AS THERAPEUTIC AGENTS
  申请人：Transtech Pharma

  公开号：EP1377295A2

  公开（公告）日：2004-01-07
• EP1377295A4
  申请人：——

  公开号：EP1377295A4

  公开（公告）日：2007-05-09