3-(5-{2-[5-methyl-2-(4-methylphenyl)-1,3-oxazol-4-yl]ethoxy}-3,4-dihydronaphthalen-1-yl)propanoic acid | 439802-32-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 3-(5-{2-[5-methyl-2-(4-methylphenyl)-1,3-oxazol-4-yl]ethoxy}-3,4-dihydronaphthalen-1-yl)propanoic acid
• 英文别名: 3-(5-(2-(2-(4-methylphenyl)-5-methyloxazol-4-yl)ethoxy)-3,4-dihydronaphthalen-1-yl)propanoic acid；3-[5-[2-[5-methyl-2-(4-methylphenyl)-1,3-oxazol-4-yl]ethoxy]-3,4-dihydronaphthalen-1-yl]propanoic acid
• CAS: 439802-32-1
• 化学式: C₂₆H₂₇NO₄
• 分子量: 417.505
• InChiKey: FBCZFPSQICQIDM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.1
• 重原子数：
  31
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  72.6
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  3-(5-{2-[5-methyl-2-(4-methylphenyl)-1,3-oxazol-4-yl]ethoxy}-3,4-dihydronaphthalen-1-yl)propanoic acid 在 盐酸 、 甲醇 、 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 三乙胺 作用下， 以 1,4-二氧六环 、 N,N-二甲基甲酰胺 为溶剂， 反应 1.0h， 生成 N-hydroxy-3-(5-(2-(2-(4-methylphenyl)-5-methyloxazol-4-yl)ethoxy)-3,4-dihydronaphthalen-1-yl)propanamide
  参考文献：
  名称：

  DIHYDRONAPHTHALENE DERIVATIVE COMPOUNDS AND DRUGS CONTAINING THESE COMPOUNDS AS THE ACTIVE INGREDIENT

  摘要：

  公开号：

  EP1354879B1
• 作为产物：
  描述：

  3-(5-methoxy-3,4-dihydronaphthalen-1-yl)propanoic acid 在 甲醇 、 sodium hydroxide 、 氯化亚砜 、 水 、 吡啶盐酸盐 、 三苯基膦 、 1,1'-azodicarbonyl-dipiperidine 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 反应 7.33h， 生成 3-(5-{2-[5-methyl-2-(4-methylphenyl)-1,3-oxazol-4-yl]ethoxy}-3,4-dihydronaphthalen-1-yl)propanoic acid
  参考文献：
  名称：

  DIHYDRONAPHTHALENE DERIVATIVE COMPOUNDS AND DRUGS CONTAINING THESE COMPOUNDS AS THE ACTIVE INGREDIENT

  摘要：

  公开号：

  EP1354879B1

文献信息

• METHOD FOR INCREASING SPECIFIC SURFACE AREA OF SLIGHTLY SOLUBLE DRUG
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP1741704A1

  公开（公告）日：2007-01-10

  The preparation method of the powder of which dissolution rate improves is characterized by including of the process that slightly soluble drug having acidic group (e.g., 3-(5-2-[5-methyl-2-(4-methylphenyl)-1,3-oxazol-4-yl]ethoxy}-3,4-dihydronaphthalen-1-yl)propanoic acid etc.) is made to metal salt solution and is neutralized to precipitate. By the method of the present invention, since a powder of which specific surface area increases and dissolution rate improves can be obtained, it is excellent as a preparation method of drug bulk

  这种提高溶解速率的粉末的制备方法的特点在于包括以下过程：将具有酸性基团的微溶性药物（例如，3-（5- 2- [5-甲基-2-（4-甲基苯基）-1,3-噁唑-4-基]乙氧基} -3,4-二氢萘-1-基）丙酸等）加入金属盐溶液中，并中和以沉淀。通过本发明的方法，由于可以获得比表面积增加和溶解速率提高的粉末，因此作为药物块的制备方法非常出色。
• Dihydronaphthalene derivative compounds and drugs containing these compounds as the active ingredient
  申请人：——

  公开号：US20040138213A1

  公开（公告）日：2004-07-15

  A compound of formula (I) 1 (wherein all symbols are as defined in the specification) and salt thereof, and peroxisome proliferator activated receptor regulator comprising thereof as active ingredient. Because a compound of formula (I) have an activity of regulating peroxisome proliferator activated receptor regulator, the compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or treatment agent for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diabetes or syndrome X.

  化合物式为（I）1（其中所有符号如规范所定义）及其盐，以及包含其作为活性成分的过氧化物酶增殖物激活受体调节剂。由于化合物（I）具有调节过氧化物酶增殖物激活受体调节剂的活性，因此化合物（I）可用作降糖剂、降脂剂、预防和/或治疗代谢紊乱相关疾病（糖尿病、肥胖症、X综合征、高胆固醇血症、高脂蛋白血症等）、高脂血症、动脉粥样硬化、高血压、循环系统疾病、暴饮暴食、冠心病等，是一种升高HDL胆固醇的药物，降低LDL胆固醇和/或VLDL胆固醇的药物，并可缓解糖尿病或X综合征的风险因素。
• Dihydronaphthalene derivative compounds and agent comprising the derivative as active ingredient
  申请人：Tajima Hisao

  公开号：US20060287304A1

  公开（公告）日：2006-12-21

  A compound of formula (I) (wherein all symbols are as defined in the specification) and salt thereof, and peroxisome proliferator activated receptor regulator comprising thereof as active ingredient. Because a compound of formula (I) have an activity of regulating peroxisome proliferator activated receptor regulator, the compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or treatment agent for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diabetes or syndrome X.

  化合物公式（I）（其中所有符号如规范中定义）及其盐，以及包含其作为活性成分的过氧化物酶增殖物激活受体调节剂。由于化合物公式（I）具有调节过氧化物酶增殖物激活受体调节剂的活性，因此化合物公式（I）可用作降血糖剂、降血脂剂、预防和/或治疗代谢紊乱疾病（糖尿病、肥胖症、X综合征、高胆固醇血症、高脂蛋白血症等）、高脂血症、动脉硬化、高血压、循环系统疾病、暴饮暴食、冠心病等，以及升高高密度脂蛋白胆固醇的药物、降低低密度脂蛋白和/或极低密度脂蛋白胆固醇的药物以及缓解糖尿病或X综合征风险因素的药物。
• Method for Increasing Specific Surface Area of Slightly Soluble Drug
  申请人：Kuwabe Shin-itsu

  公开号：US20080026067A1

  公开（公告）日：2008-01-31

  The preparation method of the powder of which dissolution rate improves is characterized by including of the process that slightly soluble drug having acidic group (e.g., 3-(5-2-[5-methyl-2-(4-methylphenyl)-1,3-oxazol-4-yl]ethoxy}-3,4-dihydronaphthalen-1-yl)propanoic acid etc.) is made to metal salt solution and is neutralized to precipitate. By the method of the present invention, since a powder of which specific surface area increases and dissolution rate improves can be obtained, it is excellent as a preparation method of drug bulk.

  该粉末的制备方法的特点在于包括以下过程：将具有酸性基团的微溶性药物（例如3-（5-2-[5-甲基-2-（4-甲基苯基）-1,3-噁唑-4-基]乙氧基}-3,4-二氢萘-1-基）丙酸等）加入金属盐溶液中，中和后沉淀。通过本发明的方法，由于可以获得比表面积增加和溶解速度提高的粉末，因此作为药物原料的制备方法非常优秀。
• US7220864B2
  申请人：——

  公开号：US7220864B2

  公开（公告）日：2007-05-22