2-(β-D-glucopyranosyloxy)-3-(3-fluoro-4-methylbenzyl)-4,6-dimethylpyridine

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-(β-D-glucopyranosyloxy)-3-(3-fluoro-4-methylbenzyl)-4,6-dimethylpyridine
• 英文别名: 2-(beta-D-Glucopyranosyloxy)-3-(3-fluoro-4-methylbenzyl)-4,6-dimethylpyridine；(2S,3R,4S,5S,6R)-2-[3-[(3-fluoro-4-methylphenyl)methyl]-4,6-dimethylpyridin-2-yl]oxy-6-(hydroxymethyl)oxane-3,4,5-triol
• 化学式: C₂₁H₂₆FNO₆
• 分子量: 407.439
• InChiKey: XFRAJRKPCRPLTP-YRIDSSQKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  29
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  112
• 氢给体数：
  4
• 氢受体数：
  8

反应信息

• 作为产物：
  描述：

  2-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyloxy)-3-(3-fluoro-4-methylbenzyl)-4,6-dimethylpyridine 在 sodium methylate 作用下， 以 甲醇 为溶剂， 反应 1.0h， 生成 2-(β-D-glucopyranosyloxy)-3-(3-fluoro-4-methylbenzyl)-4,6-dimethylpyridine
  参考文献：
  名称：

  EP1577317

  摘要：

  公开号：

文献信息

• Nitrogen-containing heterocyclic derivatives, medicinal compositions containing the same and medicinal use thereof
  申请人：Fujikura Hideki

  公开号：US20060035840A1

  公开（公告）日：2006-02-16

  The present invention provides nitrogen-containing heterocyclic derivatives represented by the general formula: wherein X 1 represents Nor CR 1 ; X 2 represents Nor CR 2 ; X 3 represents N or CR 3 ; X 4 represents N or CR 4 ; and with the proviso that one or two of X 1 to X 4 represent N; R represents optionally substituted C 3-8 cycloalkyl, optionally substituted C 6-10 aryl, etc.; R 1 to R 4 represent H, a halogen atom, etc.) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an excellent inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications, obesity or the like, pharmaceutical compositions comprising the same, and medicinal uses thereof.

  本发明提供一种氮含杂环衍生物，其通式表示为：其中，X1表示N或CR1；X2表示N或CR2；X3表示N或CR3；X4表示N或CR4；并且X1到X4中的一个或两个表示N；R表示可选择取代的C3-8环烷基，可选择取代的C6-10芳基等；R1到R4表示氢、卤素原子等。本发明的药物或药物前体具有优异的人类SGLT2抑制活性，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、肥胖症等的药物，以及包含它们的制药组合物和医药用途。
• NITROGEN-CONTAINING HETEROCYCIC DERIVATIVES, MEDICINAL COMPOSITIONS CONTAINING THE SAME AND MEDICINAL USE THEREOF
  申请人：Kissei Pharmaceutical Co., Ltd.

  公开号：EP1577317A1

  公开（公告）日：2005-09-21

  The present invention provides nitrogen-containing heterocyclic derivatives represented by the general formula: wherein X1 represents N or CR1; X2 represents N or CR2; X3 represents N or CR3; X4 represents N or CR4; and with the proviso that one or two of X1 to X4 represent N; R represents optionally substituted C3-8 cycloalkyl, optionally substituted C6-10 aryl, etc.; R1 to R4 represent H, a halogen atom, etc.) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an excellent inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications, obesity or the like, pharmaceutical compositions comprising the same, and medicinal uses thereof.

  本发明提供由通式表示的含氮杂环衍生物： 其中X1代表N或CR1；X2代表N或CR2；X3代表N或CR3；X4代表N或CR4；但条件是X1至X4中的一个或两个代表N；R代表任选取代的C3-8环烷基、任选取代的C6-10芳基等；R1至R4代表H、卤素原子等。)或其药学上可接受的盐，或其原药，它们对人类 SGLT2 具有优异的抑制活性，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、肥胖症或类似疾病的制剂、包含它们的药物组合物及其药用用途。
• US7655633B2
  申请人：——

  公开号：US7655633B2

  公开（公告）日：2010-02-02