[2-(2-chlorobenzyloxy)phenyl]methanol | 478189-97-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: [2-(2-chlorobenzyloxy)phenyl]methanol
• 英文别名: [2-[(2-chlorophenyl)methoxy]phenyl]methanol
• CAS: 478189-97-8
• 化学式: C₁₄H₁₃ClO₂
• mdl: MFCD04564809
• 分子量: 248.709
• InChiKey: WEIOZBPWGZEQON-UHFFFAOYSA-N

物化性质

• 沸点：
  387.9±27.0 °C(Predicted)
• 密度：
  1.244±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  17
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.142
• 拓扑面积：
  29.5
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  [2-(2-chlorobenzyloxy)phenyl]methanol 、 三苯基膦氢溴酸盐 以 乙腈 为溶剂， 反应 3.0h， 以91%的产率得到[2-(2-Chlorobenzyloxy)benzyl]triphenylphosphonium bromide
  参考文献：
  名称：

  Heterocyclic compounds with carboxyl isostere groups and their use for the treatment of cardiovascular diseases

  摘要：

  本申请涉及新颖的杂环化合物，它们的制备方法，它们用于治疗和/或预防疾病的用途，以及它们用于生产用于治疗和/或预防疾病的药物的用途，特别是用于治疗和/或预防心血管疾病。

  公开号：

  US20090227640A1
• 作为产物：
  描述：

  水杨醇 、 2-氯苄溴 在 potassium carbonate 作用下， 以 乙腈 为溶剂， 反应 12.0h， 以79%的产率得到[2-(2-chlorobenzyloxy)phenyl]methanol
  参考文献：
  名称：

  Heterocyclic compounds with carboxyl isostere groups and their use for the treatment of cardiovascular diseases

  摘要：

  本申请涉及新颖的杂环化合物，它们的制备方法，它们用于治疗和/或预防疾病的用途，以及它们用于生产用于治疗和/或预防疾病的药物的用途，特别是用于治疗和/或预防心血管疾病。

  公开号：

  US20090227640A1

文献信息

• Glucopyranosyloxypyrazole derivative medicinal composition containing the same medicinal use thereof and intermediate therefor
  申请人：——

  公开号：US20040176308A1

  公开（公告）日：2004-09-09

  The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: 1 wherein R 1 is a hydrogen atom or a hydroxyalkyl group; one of Q and T is a group represented by the general formula; 2 the other is an optionally substituted alkyl group or a cycloalkyl group; and R 2 is a halogen atom, a hydroxy group, an optionally substituted alkyl group, an optionally substituted alkoxy group, an alkylthio group, a group of the general formula: -A-R 3 wherein A is a single bond, an oxygen atom, a methylene group, an ethylene group, —OCH 2 — or —CH 2 O—; and R 3 is a cycloalkyl group, a heterocycloalkyl group, an optionally substituted aryl group, an optionally substituted tiazolyl group or an optionally substituted pyridyl group, pharmaceutically acceptable salts thereof or prodrugs thereof, which exert an excellent inhibitory activity in human SGLT 1 , and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutical compositions comprising the same, pharmaceutical uses thereof and production intermediates thereof.

  本发明提供了由通式1表示的葡萄糖吡唑衍生物，其中R1是氢原子或羟基烷基；Q和T中的一个是由通式2表示的基团，另一个是可选取代的烷基或环烷基；R2是卤素原子、羟基、可选取代的烷基、可选取代的烷氧基、烷硫基、通式-A-R3中的基团，其中A是单键、氧原子、亚甲基、乙烯基、—OCH2—或—CH2O—，而R3是环烷基、杂环烷基、可选取代的芳基、可选取代的噻唑基或可选取代的吡啶基，其药物学上可接受的盐或前药，在人类SGLT1中具有优异的抑制活性，因此可用作预防或治疗与高血糖相关的疾病，如糖尿病、糖尿病并发症或肥胖症的药物，以及包含其的制药组合物、制药用途和生产中间体。
• Biphenyl compounds useful in the treatment or prevention of cardiovascular disorders
  申请人：Bayer Schering Pharma Aktiengellschaft

  公开号：US07998988B2

  公开（公告）日：2011-08-16

  The invention relates to biphenyl compounds of formula (I): wherein U, V and W together form a group of the formula *—CH═CH—CH<, *—CH2—CH2—CH< or *—CH2—CH2—N<, in which * means the point of linkage to the phenyl ring; A is O or CH2; and D, E, X, Y, Z, R1, R2, o, n, and p are as defined in the specification. The invention also relates to pharmaceutical compositions of the compound of the compounds. The compounds and pharmaceutical compositions of the invention can be used in the treatment or prevention of cardiovascular disorders.

  本发明涉及式(I)的联苯化合物：其中U、V和W共同形成公式*—CH═CH—CH<、*—CH2—CH2—CH<或*—CH2—CH2—N<的基团，其中*表示连接到苯环的连接点；A为O或CH2；D、E、X、Y、Z、R1、R2、o、n和p如规范中所定义。本发明还涉及所述化合物的制药组合物。本发明的化合物和制药组合物可用于治疗或预防心血管疾病。
• GLUCOPYRANOSYLOXYPYRAZOLE DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF, AND INTERMEDIATE THEREFOR
  申请人：Kissei Pharmaceutical Co., Ltd.

  公开号：EP1400529A1

  公开（公告）日：2004-03-24

  The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 is a hydrogen atom or a hydroxyalkyl group; one of Q and T is a group represented by the general formula; the other is an optionally substituted alkyl group or a cycloalkyl group; and R2 is a halogen atom, a hydroxy group, an optionally substituted alkyl group, an optionally substituted alkoxy group, an alkylthio group, a group of the general formula: -A-R3 wherein A is a single bond, an oxygen atom, a methylene group, an ethylene group, -OCH2- or -CH2O-; and R3 is a cycloalkyl group, a heterocycloalkyl group, an optionally substituted aryl group, an optionally substituted tiazolyl group or an optionally substituted pyridyl group, pharmaceutically acceptable salts thereof or prodrugs thereof, which exert an excellent inhibitory activity in human SGLT1, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutical compositions comprising the same, pharmaceutical uses thereof and production intermediates thereof.

  本发明提供由通式表示的葡萄糖吡喃氧基吡唑衍生物： 其中 R1 是氢原子或羟烷基；Q 和 T 中的一个是通式表示的基团，另一个是任选取代的烷基或环烷基；以及 R2 是卤原子； R2是卤原子、羟基、任选取代的烷基、任选取代的烷氧基、烷硫基、通式如下的基团：-其中 A 是单键、氧原子、亚甲基、亚乙基、-OCH2- 或 -CH2O-；以及 R3 是环烷基、杂环烷基、任选取代的芳基、任选取代的噻唑基或任选取代的吡啶基、其药学上可接受的盐或其原药，它们对人类 SGLT1 具有极佳的抑制活性，因此可用作预防或治疗与高血糖有关的疾病（如糖尿病、糖尿病并发症或肥胖症）的药物、包含这些药物的药物组合物、其药物用途以及其生产中间体。
• Ginger and Its Bioactive Component Inhibit Enterotoxigenic <i>Escherichia coli</i> Heat-Labile Enterotoxin-Induced Diarrhea in Mice
  作者：Jaw-Chyun Chen、Li-Jiau Huang、Shih-Lu Wu、Sheng-Chu Kuo、Tin-Yun Ho、Chien-Yun Hsiang

  DOI：10.1021/jf071460f

  日期：2007.10.1

  Ginger is one of the most commonly used fresh herbs and spices. Enterotoxigenic Escherichia coli heat-labile enterotoxin (LT)-induced diarrhea is the leading cause of infant death in developing countries. In this study, we demonstrated that ginger significantly blocked the binding of LT to cell-surface receptor G(M1), resulting in the inhibition of fluid accumulation in the closed ileal loops of mice. Biological-activity-guided searching for active components showed that zingerone (vanillylacetone) was the likely active constituent responsible for the antidiarrheal efficacy of ginger. Further analysis of chemically synthesized zingerone derivatives revealed that compound 31 (2-[(4-methoxybenzyl)oxy]benzoic acid) significantly suppressed LT-induced diarrhea in mice via an excellent surface complementarity with the B subunits of LT. In conclusion, our findings provide evidence that ginger and its derivatives may be effective herbal supplements for the clinical treatment of enterotoxigenic Escherichia coli diarrhea.
• HETEROCYCLISCHE VERBINDUNGEN MIT CARBOXYL-ISOSTEREN GRUPPEN UND IHRE VERWENDUNG ZUR BEHANDLUNG VON HERZ-KREISLAUF-ERKRANKUNGEN
  申请人：Bayer Intellectual Property GmbH

  公开号：EP1940811B1

  公开（公告）日：2014-02-26