3-(4-ethylbenzyl)-2-(β-D-glucopyranosyloxy)-4,6-dimethylpyridine | 479481-59-9

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 3-(4-ethylbenzyl)-2-(β-D-glucopyranosyloxy)-4,6-dimethylpyridine
• 英文别名: (2S,3R,4S,5S,6R)-2-[3-[(4-ethylphenyl)methyl]-4,6-dimethylpyridin-2-yl]oxy-6-(hydroxymethyl)oxane-3,4,5-triol
• CAS: 479481-59-9
• 化学式: C₂₂H₂₉NO₆
• 分子量: 403.475
• InChiKey: MLWACSVTNMAILY-JPVHLGFFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  29
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  112
• 氢给体数：
  4
• 氢受体数：
  7

文献信息

• Nitrogenous heterocyclic derivative, medicinal composition containing the same, medical use thereof, and intermediate therefor
  申请人：Nishimura Toshihiro

  公开号：US20050049203A1

  公开（公告）日：2005-03-03

  The present invention provides nitrogen-containing heterocyclic derivatives represented by the general formula: wherein X 1 and X 3 independently represent N or CH; X 2 represents N or CR 2 ; X 4 represents N or CR 3 ; and with the proviso that one or two of X 1 , X 2 , X 3 and X 4 represent N; R 1 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a lower alkoxy-substituted (lower alkyl) group, a lower alkoxy-substituted(lower alkoxy) group, a lower alkoxy(lower alkoxy) -substituted (lower alkyl) group, a cyclic lower alkyl group, a halo(lower alkyl) group or a group represented by the general formula: HO-A—wherein A represents a lower alkylene group, a lower alkyleneoxy group or a lower alkylenethio group; R 2 represents a hydrogen atom, a halogen atom, a lower alkyl group, a cyclic lower alkyl group, a lower alkoxy group, an amino group, a (lower acyl)amino group, a mono(lower alkyl)amino group or a di(lower alkyl)amino group; and R 3 represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, or prodrugs thereof which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutical compositions comprising the same, and pharmaceutical uses and production intermediates thereof.

  本发明提供了一种以通式表示的含氮杂环衍生物： 其中，X1和X3独立地表示N或CH；X2表示N或CR2；X4表示N或CR3；并且假定X1、X2、X3和X4中的一个或两个表示N；R1表示氢原子、卤素原子、低碳基、低烷氧基、低硫代烷基、低烷氧基取代的（低烷基）基团、低烷氧基取代的（低烷氧基）基团、低烷氧基（低烷氧基）取代的（低烷基）基团、环状低烷基、卤素（低烷基）基团或由通式HO-A-表示的基团，其中A表示低碳亚烷基、低碳亚烷氧基或低碳亚烷硫基；R2表示氢原子、卤素原子、低碳基、环状低碳基、低烷氧基、氨基、（低酰基）氨基、单（低烷基）氨基或双（低烷基）氨基；R3表示氢原子或低碳基，或其药学上可接受的盐，或其前药，其作为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剂，包括这些药剂的制剂和制备中间体。
• NITROGENOUS HETEROCYCLIC DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF AND INTERMEDIATE THEREFOR
  申请人：Kissei Pharmaceutical Co., Ltd.

  公开号：EP1405859A1

  公开（公告）日：2004-04-07

  The present invention is to provide a nitrogen-containing heterocyclic derivative represented by the general formula (I) or a pharmaceutically acceptable salt thereof, or a prodrug thereof, which exerts an excellent inhibitory activity in human SGLT2 and is useful as an agent for the prevention or treatment of a disease associated with hyperglycemia such as diabetes etc., or a pharmaceutical composition comprising the same and a pharmaceutical use thereof and a production intermediate thereof. In the general formula (I), X1 and X3 are N or CH; X2 is N or CR2; X4 is N or CR3; and with the proviso that one or two of X1, X2, X3 and X4 are N; and R1, R2 and R3 are a hydrogen atom etc.

  本发明旨在提供一种由通式(I)代表的含氮杂环衍生物或其药学上可接受的盐，或其原药，该衍生物对人SGLT2具有优异的抑制活性，可作为预防或治疗糖尿病等与高血糖相关疾病的药物，或由其组成的药物组合物及其药物用途和其生产中间体。在通式（I）中，X1 和 X3 是 N 或 CH；X2 是 N 或 CR2；X4 是 N 或 CR3；但条件是 X1、X2、X3 和 X4 中的一个或两个是 N；R1、R2 和 R3 是氢原子等。
• PROGRESSION INHIBITOR FOR DISEASE ATTRIBUTED TO ABNORMAL ACCUMULATION OF LIVER FAT
  申请人：Kissei Pharmaceutical Co., Ltd.

  公开号：EP1782828A1

  公开（公告）日：2007-05-09

  The present invention provides pharmaceutical compositions useful as agents for the inhibition of progression of diseases associated with abnormal accumulation ofliverlipids. In particular, the pharmaceutical compositions of the present invention which comprise as an active ingredient a sodium/glucose co-transporter 2 inhibitor are highly suitable as an agent for the inhibition of progression of not only common fatty liver but also non-alcholic fatty liver disease (NAFL), non-alcholic steatohepatitis (NASH), hypernutritive fatty liver, diabetic fatty liver, alcholic fatty liver disease toxic fatty liver or the like.

  本发明提供的药物组合物可作为抑制与肝脂异常积聚有关的疾病进展的药物。特别是，本发明的药物组合物包含钠/葡萄糖共转运体 2 抑制剂作为活性成分，非常适合作为不仅是普通脂肪肝，而且是非胆汁性脂肪肝（NAFL）、非胆汁性脂肪性肝炎（NASH）、高营养脂肪肝、糖尿病脂肪肝、胆汁性脂肪肝中毒性脂肪肝或类似疾病的进展抑制剂。
• Progression Inhibitor For Disease Attributed To Abnormal Accumulation Of Liver Fat
  申请人：Katsuno Kenji

  公开号：US20080045466A1

  公开（公告）日：2008-02-21

  The present invention provides pharmaceutical compositions useful as agents for the inhibition of progression of diseases associated with abnormal accumulation of liver lipids. In particular, the pharmaceutical compositions of the present invention which comprise as an active ingredient a sodium/glucose co-transporter 2 inhibitor are highly suitable as an agent for the inhibition of progression of not only common fatty liver but also non-alcholic fatty liver disease (NAFL), non-alcholic steatohepatitis (NASH), hypernutritive fatty liver, diabetic fatty liver, alcholic fatty liver disease toxic fatty liver or the like.
• US7271153B2
  申请人：——

  公开号：US7271153B2

  公开（公告）日：2007-09-18