依泮洛尔 | 86880-51-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 中文名称: 依泮洛尔
• 中文别名: 益派洛尔
• 英文名称: Epanolol
• 英文别名: N(2-((3-(2-cyanophenoxy)-2-hydroxypropyl)-amino)-ethyl)-2-(4-hydroxyphenyl)-acetamide；N-(2-((3-(2-cyanophenoxy)-2-hydroxy-propyl)amino)ethyl)-2-(4-hydroxyphenyl)-acetamide；1-(2-cyanophenoxy)-3-β(4-hydroxyphenylacetamido)ethylamino-2-propanol；N-[2-[[3-(2-cyanophenoxy)-2-hydroxypropyl]amino]ethyl]-2-(4-hydroxyphenyl)acetamide
• CAS: 86880-51-5
• 化学式: C₂₀H₂₃N₃O₄
• 分子量: 369.42
• InChiKey: YARKMNAWFIMDKV-UHFFFAOYSA-N

物化性质

• 熔点：
  118-120°
• 沸点：
  689.7±55.0 °C(Predicted)
• 密度：
  1.28±0.1 g/cm3(Predicted)
• 溶解度：
  溶于二甲基亚砜

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  27
• 可旋转键数：
  10
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  115
• 氢给体数：
  4
• 氢受体数：
  6

制备方法与用途

生物活性 Epanolol (Visacor; ICI141292) 是一种强效的β1-肾上腺素能受体激动剂，属于新型抗心绞痛药物，表现出选择性的β1-肾上腺素能受体部分激动和阻断活性。

靶点 β1 肾上腺素能受体

体外研究 Epanolol 是一种选择性的β1-肾上腺素能受体部分激动剂，并具有选择性的拮抗作用。

反应信息

• 作为产物：
  描述：

  对羟基苯乙酸乙酯 、 3-<(2-aminoethyl)-amino>-1-(2-cyanophenoxy)propan-2-ol 在 对羟基苯乙酸乙酯 作用下， 以78的产率得到依泮洛尔
  参考文献：
  名称：

  Alkanolamine derivatives and pharmaceutical compositions and uses thereof

  摘要：

  1-芳氧基-3-氨基烷基氨基-2-丙醇衍生物，其制备方法，含有它们的制药组合物以及在心脏疾病治疗中使用它们的方法。这些化合物具有β-肾上腺素受体阻滞活性，其中一些还具有心脏兴奋剂活性。其中一种化合物是1-(2-氰基苯氧基)-3-β-(4-羟基苯乙酰胺)乙基氨基-2-丙醇。

  公开号：

  US04167581A1

文献信息

• DISUBSTITUTED TRIFLUOROMETHYL PYRIMIDINONES AND THEIR USE
  申请人：BAYER PHARMA AKTIENGESELLSCHAFT

  公开号：US20160221965A1

  公开（公告）日：2016-08-04

  The present application relates to novel 2,5-disubstituted 6-(trifluoromethyl)pyrimidin-4(3H)-one derivatives, to processes for their preparation, to their use alone or in combinations for the treatment and/or prevention of diseases, and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for treatment and/or prevention of cardiovascular, renal, inflammatory and fibrotic diseases.

  本申请涉及新颖的2,5-二取代6-(三氟甲基)嘧啶-4(3H)-酮衍生物，其制备方法，其单独或与其他药物联合用于治疗和/或预防疾病，以及用于制备治疗和/或预防疾病的药物，特别是用于治疗和/或预防心血管、肾脏、炎症和纤维化疾病。
• Dibenzyl Amine Compounds and Derivatives
  申请人：Chang George

  公开号：US20070213371A1

  公开（公告）日：2007-09-13

  Dibenzyl amine compounds and derivatives, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.

  二苯基胺化合物及其衍生物，含有这种化合物的药物组合物以及使用这种化合物提高某些血浆脂质水平，包括高密度脂蛋白胆固醇，并降低其他一些血浆脂质水平，如低密度脂蛋白胆固醇和甘油三酯，并据此治疗由高密度脂蛋白胆固醇水平低和/或低密度脂蛋白胆固醇和甘油三酯水平高加重的疾病，如动脉粥样硬化和心血管疾病在某些哺乳动物，包括人类。
• METHOD FOR THE PREPARATION OF (4S)-4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-2,8-DIMETHYL-1,4-DIHYDRO-1-6-NAPHTHYRIDINE-3-CARBOXAMIDE AND THE PURIFICATION THEREOF FOR USE AS AN ACTIVE PHARMACEUTICAL INGREDIENT
  申请人：BAYER PHARMA AKTIENGESELLSCHAFT

  公开号：US20180244670A1

  公开（公告）日：2018-08-30

  The present invention relates to a novel and improved process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I)

  本发明涉及一种用于制备式(I)的(4S)-4-(4-氰基-2-甲氧基苯基)-5-乙氧基-2,8-二甲基-1,4-二氢-1,6-萘啉-3-羧酰胺的新型改进工艺。
• Amino-substituted imidazo[1,2-a]pyridinecarboxamides and their use
  申请人：BAYER PHARMA AKTIENGESELLSCHAFT

  公开号：US20140128372A1

  公开（公告）日：2014-05-08

  The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.

  本申请涉及新型取代咪唑[1,2-a]吡啶-3-羧酰胺，其制备方法，单独或组合使用以治疗和/或预防疾病，以及用于制备治疗和/或预防疾病的药物，特别是用于治疗和/或预防心血管疾病。
• SUBSTITUTED BIPIPERIDINYL DERIVATIVES
  申请人：Bayer Pharma Aktiengesellschaft

  公开号：US20160318866A1

  公开（公告）日：2016-11-03

  The invention relates to novel substituted bipiperidinyl derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of diabetic microangiopathies, diabetic ulcers on the extremities, in particular for promoting wound healing of diabetic foot ulcers, diabetic heart failure, diabetic coronary microvascular heart disorders, peripheral and cardiac vascular disorders, thromboembolic disorders and ischaemias, peripheral circulatory disturbances, Raynaud's phenomenon, CREST syndrome, microcirculatory disturbances, intermittent claudication, and peripheral and autonomous neuropathies.

  该发明涉及新型取代的双哌啶衍生物，涉及它们的制备方法，涉及它们用于治疗和/或预防疾病以及用于制备治疗和/或预防疾病的药物的用途，特别是用于治疗和/或预防糖尿病微血管病变、四肢糖尿病溃疡，特别是促进糖尿病足溃疡愈合、糖尿病心力衰竭、糖尿病冠状微血管心脏疾病、外周和心脏血管疾病、血栓栓塞疾病和缺血、外周循环障碍、雷诺现象、CREST综合征、微循环障碍、间歇性跛行以及外周和自主神经病变的治疗和/或预防。