(4-溴-萘-2-基)-甲醇 | 874357-17-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 中文名称: (4-溴-萘-2-基)-甲醇
• 英文名称: (4-bromonaphthalene-2-yl)-methanol
• 英文别名: (4-bromo-naphthalen-2-yl)-methanol；(4-Bromonaphthalen-2-yl)methanol
• CAS: 874357-17-2
• 化学式: C₁₁H₉BrO
• 分子量: 237.096
• InChiKey: VYSCKPUODPPSJS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  20.2
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  (4-溴-萘-2-基)-甲醇 在 氯化亚砜 、 zinc(II) chloride 作用下， 以 1,4-二氧六环 、 水 、 乙腈 为溶剂， 反应 19.67h， 生成 2-(4-溴萘-2-基)乙腈
  参考文献：
  名称：

  Antihyperglycemic activity of novel naphthalenylmethyl-3H-1,2,3,5-oxathiadiazole 2-oxides

  摘要：

  A series of naphthalenyl 3H-1,2,3,5-oxathiadiazole 2-oxides was prepared and tested for antihyperglycemic activity in the db/db mouse, a model for type 2 (non-insulin dependent) diabetes mellitus. Substitution at the 1-, 5-, or 8-positions of the naphthalene ring with a halogen was found to be beneficial to antihyperglycemic activity. 4-[(5-Chloronaphthalen-2-yl)methyl]-3H-1,2,3,5-oxathiadiazole 2-oxide (45), one of the most potent compounds in this series, was selected for further pharmacological evaluation.

  DOI：

  10.1021/jm00069a006
• 作为产物：
  描述：

  4-溴-2-萘甲酸 在 二异丁基氢化铝 作用下， 以 四氢呋喃 为溶剂， 反应 18.0h， 生成 (4-溴-萘-2-基)-甲醇
  参考文献：
  名称：

  Antihyperglycemic activity of novel naphthalenylmethyl-3H-1,2,3,5-oxathiadiazole 2-oxides

  摘要：

  A series of naphthalenyl 3H-1,2,3,5-oxathiadiazole 2-oxides was prepared and tested for antihyperglycemic activity in the db/db mouse, a model for type 2 (non-insulin dependent) diabetes mellitus. Substitution at the 1-, 5-, or 8-positions of the naphthalene ring with a halogen was found to be beneficial to antihyperglycemic activity. 4-[(5-Chloronaphthalen-2-yl)methyl]-3H-1,2,3,5-oxathiadiazole 2-oxide (45), one of the most potent compounds in this series, was selected for further pharmacological evaluation.

  DOI：

  10.1021/jm00069a006

文献信息

• Novel Glucitol Derivative, Prodrug Thereof And Salt Thereof, And Therapeutic Agent Containing The Same For Diabetes
  申请人：Matsuoka Hiroharu

  公开号：US20080319047A1

  公开（公告）日：2008-12-25

  The invention provides a glucitol derivative having the function of reducing a blood sugar level and having preferable properties required of medicines, such as long-lasting drug activity; and a medicinal composition for use in the prevention or treatment of diseases attributable to hyperglycemia, such as diabetes, complications of diabetes, and obesity. The derivative is a compound represented by the formula (I): wherein m is an integer selected among 1-3; R 1 to R 4 each independently is optionally substituted alkyl, etc.; Ar1 is optionally substituted naphthyl; and A is optionally substituted heteroaryl, a prodrug of the compound, or a pharmaceutically acceptable salt of either. Also provided are a medicine, a medicinal composition, and the like each containing the compound.

  本发明提供了一种葡萄糖醇衍生物，具有降低血糖水平的功能，并具有药物所需的优良性质，例如持久的药物活性；以及用于预防或治疗由高血糖引起的疾病，例如糖尿病、糖尿病并发症和肥胖症的药物组合物。该衍生物是由式(I)表示的化合物：其中m是在1-3之间选择的整数；R1至R4各自独立地是可选的取代烷基等；Ar1是可选的取代萘基；A是可选的取代杂环芳基、该化合物的前药或其药学上可接受的盐。还提供了含有该化合物的药物、药物组合物等。
• NOVEL C-ARYL GLUCOSIDE SGLT2 INHIBITORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME
  申请人：Lee Jinhwa

  公开号：US20120101051A1

  公开（公告）日：2012-04-26

  A novel C-aryl glucoside compound, or a pharmaceutically acceptable salt or a prodrug thereof having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney; and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly, diabetes, are provided.

  提供了一种新型的C-芳基葡萄糖苷化合物，或其药学上可接受的盐或前药，具有抑制肠道和肾脏中存在的钠依赖性葡萄糖共转运体2（SGLT2）的活性；以及包含该化合物作为活性成分的制药组合物，可用于预防或治疗代谢性疾病，特别是糖尿病。
• Glucitol derivative, prodrug thereof and salt thereof, and therapeutic agent containing the same for diabetes
  申请人：Chugai Seiyaku Kabushiki Kaisha

  公开号：US07943748B2

  公开（公告）日：2011-05-17

  The invention provides a glucitol derivative having the function of reducing a blood sugar level and having preferable properties required of medicines, such as long-lasting drug activity; and a medicinal composition for use in the prevention or treatment of diseases attributable to hyperglycemia, such as diabetes, complications of diabetes, and obesity. The derivative is a compound represented by the formula (I): wherein m is an integer selected among 1-3; R1 to R4 each independently is optionally substituted alkyl, etc.; Ar1 is optionally substituted naphthyl; and A is optionally substituted heteroaryl, a prodrug of the compound, or a pharmaceutically acceptable salt of either. Also provided are a medicine, a medicinal composition, and the like each containing the compound.

  本发明提供了一种葡萄糖醇衍生物，具有降低血糖水平的功能，并具有药物所需的优良特性，例如长效药物活性；以及用于预防或治疗由高血糖引起的疾病，例如糖尿病、糖尿病并发症和肥胖症的药物组合物。该衍生物是由式（I）表示的化合物：其中m是在1-3之间选择的整数；R1到R4各自独立地是可选的取代烷基等；Ar1是可选的取代萘基；A是可选的取代杂环基，该化合物的前药物或其药学上可接受的盐。还提供了含有该化合物的药物、药物组合物等。
• C-aryl glucoside SGLT2 inhibitors and pharmaceutical compositions comprising same
  申请人：Lee Jinhwa

  公开号：US08541380B2

  公开（公告）日：2013-09-24

  A novel C-aryl glucoside compound, or a pharmaceutically acceptable salt or a prodrug thereof having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney; and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly, diabetes, are provided.

  提供一种新的C-芳基葡萄糖苷化合物，或其药物可接受的盐或前药，具有对存在于肠和肾中的钠依赖性葡萄糖共转运体2（SGLT2）的抑制活性；以及包含其作为活性成分的制药组合物，该组合物对预防或治疗代谢紊乱特别是糖尿病有用。
• NOVEL GLUCITOL DERIVATIVE, PRODRUG THEREOF AND SALT THEREOF, AND THERAPEUTIC AGENT CONTAINING THE SAME FOR DIABETES
  申请人：CHUGAI SEIYAKU KABUSHIKI KAISHA

  公开号：EP1803721A1

  公开（公告）日：2007-07-04

  The invention provides a glucitol derivative having the function of reducing a blood sugar level and having preferable properties required of medicines, such as long-lasting drug activity; and a medicinal composition for use in the prevention or treatment of diseases attributable to hyperglycemia, such as diabetes, complications of diabetes, and obesity. The derivative is a compound represented by the formula (I): wherein m is an integer selected among 1-3; R1 to R4 each independently is optionally substituted alkyl, etc.; Ar1 is optionally substituted naphthyl; and A is optionally substituted heteroaryl, a prodrug of the compound, or a pharmaceutically acceptable salt of either. Also provided are a medicine, a medicinal composition, and the like each containing the compound.

  本发明提供了一种葡萄糖醇衍生物，该衍生物具有降低血糖水平的功能，并具有药物所需的优越性能，如持久的药物活性；还提供了一种药物组合物，用于预防或治疗由高血糖引起的疾病，如糖尿病、糖尿病并发症和肥胖症。衍生物是由式 (I) 所代表的化合物： 其中 m 是选自 1-3 的整数；R1 至 R4 各自独立地是任选取代的烷基等；Ar1 是任选取代的萘基；A 是任选取代的杂芳基、该化合物的原药或二者的药学上可接受的盐。此外，还提供了各自含有该化合物的药物、药物组合物等。