1-(3-溴丙氧基)-4-苯氧基-2-丙基苯 | 228579-10-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 1-(3-溴丙氧基)-4-苯氧基-2-丙基苯
• 英文名称: 4-(3-bromopropoxy)-3-propylphenyl phenyl ether
• 英文别名: 1-(3-bromopropoxy)-4-phenoxy-2-propylBenzene
• CAS: 228579-10-0
• 化学式: C₁₈H₂₁BrO₂
• 分子量: 349.268
• InChiKey: XVGAMUCKJLSONZ-UHFFFAOYSA-N

物化性质

• 沸点：
  425.2±45.0 °C(Predicted)
• 密度：
  1.249±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  5.9
• 重原子数：
  21
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  18.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-(3-溴丙氧基)-4-苯氧基-2-丙基苯 在 sodium hydroxide 、 caesium carbonate 作用下， 以 N,N-二甲基甲酰胺 、 异丙醇 为溶剂， 反应 5.0h， 生成 6-(3-(2-Propyl-4-phenoxyphenoxy)propoxy)-chromane-2-carboxylic acid
  参考文献：
  名称：

  (2R)-2-Ethylchromane-2-carboxylic Acids:  Discovery of Novel PPARα/γ Dual Agonists as Antihyperglycemic and Hypolipidemic Agents

  摘要：

  A series of chromane-2-carboxylic acid derivatives was synthesized and evaluated for PPAR agonist activities. A structure-activity relationship was developed toward PPARalpha/gamma dual agonism. As a result, (2R)-7-{3-[2-chloro-4-(4-fluorophenoxy)phenoxy]propoxy}-2-ethylchromane-2-carboxylic acid (48) was identified as a potent, structurally novel, selective PPARalpha/gamma dual agonist. Compound 48 exhibited substantial antihyperglycemic and hypolipidemic activities when orally administered in three different animal models: the db/db mouse type 2 diabetes model, a Syrian hamster lipid model, and a dog lipid model.

  DOI：

  10.1021/jm030621d
• 作为产物：
  描述：

  4-甲氧基苯酚 、 2-propyl-4-(4'-methoxyphenoxy)phenol 生成 1-(3-溴丙氧基)-4-苯氧基-2-丙基苯
  参考文献：
  名称：

  Arylthiazolidinedione and aryloxazolidinedione derivatives

  摘要：

  5-芳基-2,4-噻唑烷二酮或5-芳基-2,4-噁唑烷二酮，在杂环环的5-位置还带有第二取代基，是PPAR的有效激动剂，因此在糖尿病、高血糖、高脂血症（包括高胆固醇血症和高甘油三酯血症）、动脉粥样硬化、肥胖、血管再狭窄和其他PPAR α、δ和/或γ介导的疾病、紊乱和病况的治疗、控制或预防中是有用的。

  公开号：

  US06399640B1

文献信息

• Arylthiazolidinedione derivatives
  申请人：Merck & Co., Inc.

  公开号：US06008237A1

  公开（公告）日：1999-12-28

  Substituted 5-aryl-2,4-thiazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR .alpha., .delta. and/or .gamma. mediated diseases, disorders and conditions.

  取代的5-芳基-2,4-噻唑烷二酮是PPAR的有效激动剂，因此在糖尿病、高血糖、高脂血症（包括高胆固醇血症和高甘油三酯血症）、动脉粥样硬化、肥胖、血管再狭窄和其他PPAR .alpha.、.delta.和/或.gamma.介导的疾病、紊乱和症状的治疗、控制或预防中有用。
• [EN] ORGANIC COMPOUNDS<br/>[FR] COMPOSES ORGANIQUES
  申请人：NOVARTIS AG

  公开号：WO2005026134A1

  公开（公告）日：2005-03-24

  Compounds of the formula (I) provide pharmacological agents which bind to Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the present invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases (IBDs), ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.

  (I)式化合物提供与过氧化物酶体增殖物激活受体（PPARs）结合的药理剂。因此，本发明的化合物对于治疗哺乳动物中由PPAR受体活性介导的疾病是有用的。这些疾病包括脂质代谢异常、高脂血症、高胆固醇血症、动脉粥样硬化、高甘油三酯血症、心力衰竭、心肌梗死、血管疾病、心血管疾病、高血压、肥胖、炎症、关节炎、癌症、阿尔茨海默病、皮肤疾病、呼吸系统疾病、眼科疾病、炎症性肠病（IBDs）、溃疡性结肠炎和克罗恩病。本发明的化合物在哺乳动物中作为降糖剂特别有用，用于治疗和预防与糖耐量受损、高血糖和胰岛素抵抗有关的疾病，如1型和2型糖尿病以及X综合征。
• [EN] BENZENESULFONYLAMINO COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS<br/>[FR] COMPOSES BENZENESULFONYLAMINO, ET COMPOSITIONS PHARMACEUTIQUES CONTENANT CES COMPOSES
  申请人：NOVARTIS AG

  公开号：WO2005005421A1

  公开（公告）日：2005-01-20

  Compounds of the formula (I) provide pharmacological agents which bind to Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer’s disease, skin disorders, respiratory diseases, opthalmic disorders, inflammatory bowel diseases (IBDs) ulcerative colitis and Crohn’s disease, and conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.

  式(I)的化合物提供与过氧化物酶体增殖物活化受体（PPARs）结合的药理剂。因此，本发明的化合物对哺乳动物中由PPAR受体活性介导的疾病的治疗是有用的。这些疾病包括脂质代谢异常、高脂血症、高胆固醇血症、动脉粥样硬化、高甘油三酯血症、心力衰竭、心肌梗死、血管疾病、心血管疾病、高血压、肥胖、炎症、关节炎、癌症、阿尔茨海默病、皮肤疾病、呼吸系统疾病、眼科疾病、炎症性肠病（IBDs）、溃疡性结肠炎和克罗恩病，以及与葡萄糖耐量受损、高血糖和胰岛素抵抗有关的疾病，如1型和2型糖尿病以及X综合征。
• Benzopyrancarboxylic acid derivatives for the treatment of diabetes and lipid disorders
  申请人：——

  公开号：US20020082292A1

  公开（公告）日：2002-06-27

  A class of benzopyrancarboxylic acid derivatives comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.

  苯并吡喃羧酸衍生物类别包括强效PPARα和/或γ激动剂化合物，因此在治疗、控制或预防非胰岛素依赖型糖尿病（NIDDM）、高血糖、血脂异常、高血脂症、高胆固醇血症、高甘油三酯血症、动脉粥样硬化、肥胖、血管再狭窄、炎症和其他PPARα和/或γ介导的疾病、紊乱和状况中具有用处。
• [EN] N-ACYL NITROGEN HETEROCYCLES AS LIGANDS OF PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS<br/>[FR] HETEROCYCLES D'AZOTE N-ACYLE UTILISES COMME LIGANDS DES RECEPTEURS ACTIVES PAR LES PROLIFERATEURS DE PEROXYSOMES
  申请人：NOVARTIS AG

  公开号：WO2004103995A1

  公开（公告）日：2004-12-02

  Compounds of the formula (I) provide pharmacological agents which bind to Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer’s disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis, Crohn’s disease, and conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.

  化合物式（I）的化合物提供了结合到过氧化物酶体增殖物激活受体（PPARs）的药物。因此，本发明的化合物对于治疗哺乳动物中由PPAR受体活性介导的疾病是有用的。这些疾病包括失调脂质代谢、高脂血症、高胆固醇血症、动脉粥样硬化、高甘油三酯血症、心力衰竭、心肌梗塞、血管疾病、心血管疾病、高血压、肥胖症、炎症、关节炎、癌症、阿尔茨海默病、皮肤疾病、呼吸系统疾病、眼科疾病、炎症性肠病、溃疡性结肠炎、克罗恩病以及与糖耐量受损、高血糖和胰岛素抵抗有关的疾病，例如1型和2型糖尿病以及X综合症。