1-Methyl-2-(trifluoromethyl)-4,5,6,7-tetrahydroimidazo[4,5-c]pyridine | 733758-24-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡啶类
• 英文名称: 1-Methyl-2-(trifluoromethyl)-4,5,6,7-tetrahydroimidazo[4,5-c]pyridine
• CAS: 733758-24-2
• 化学式: C₈H₁₀F₃N₃
• 分子量: 205.183
• InChiKey: BRDRWPYPCUWICQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  29.8
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  1-Methyl-2-(trifluoromethyl)-4,5,6,7-tetrahydroimidazo[4,5-c]pyridine 、 西他列汀脱氟杂质4 在 1-羟基苯并三唑 、 1-(3-二甲基氨基丙基)-3-乙基碳二亚胺 、 三乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成
  参考文献：
  名称：

  咪唑并哌啶酰胺作为二肽基肽酶IV抑制剂，用于治疗糖尿病。

  摘要：

  已经制备了一系列取代的咪唑并哌啶酰胺，并评价了其对二肽基肽酶IV（DPP-4）的抑制作用。相对于DPP-8和DPP-9，在1位和3位取代可提高DPP-4的选择性。该系列化合物抑制DPP-4的IC（50）值低至5.8 nM。

  DOI：

  10.1016/j.bmcl.2007.08.030
• 作为产物：
  描述：

  1-Methyl-2-(trifluoromethyl)imidazo[4,5-c]pyridine 在 platinum(IV) oxide 氢气 作用下， 以 乙醇 为溶剂， 40.0 ℃ 、6.89 MPa 条件下， 生成 1-Methyl-2-(trifluoromethyl)-4,5,6,7-tetrahydroimidazo[4,5-c]pyridine
  参考文献：
  名称：

  咪唑并哌啶酰胺作为二肽基肽酶IV抑制剂，用于治疗糖尿病。

  摘要：

  已经制备了一系列取代的咪唑并哌啶酰胺，并评价了其对二肽基肽酶IV（DPP-4）的抑制作用。相对于DPP-8和DPP-9，在1位和3位取代可提高DPP-4的选择性。该系列化合物抑制DPP-4的IC（50）值低至5.8 nM。

  DOI：

  10.1016/j.bmcl.2007.08.030

文献信息

• 3-Amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
  申请人：Ashton T Wallace

  公开号：US20060069116A1

  公开（公告）日：2006-03-30

  The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
• US7265128B2
  申请人：——

  公开号：US7265128B2

  公开（公告）日：2007-09-04
• [EN] 3-AMINO-4-PHENYLBUTANOIC ACID DERIVATIVES AS DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES<br/>[FR] DERIVES D'ACIDE 3-AMINO-4-PHENYLBUTANOIQUE UTILISES COMME INHIBITEURS DE LA DIPEPTIDYL PEPTIDASE POUR LE TRAITEMENT OU LA PREVENTION DU DIABETE
  申请人：MERCK & CO INC

  公开号：WO2004064778A2

  公开（公告）日：2004-08-05

  The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme ('DP-IV inhibitors') and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
• Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes
  作者：Ping Chen、Charles G. Caldwell、Robert J. Mathvink、Barbara Leiting、Frank Marsilio、Reshma A. Patel、Joseph K. Wu、Huaibing He、Kathryn A. Lyons、Nancy A. Thornberry、Ann E. Weber

  DOI：10.1016/j.bmcl.2007.08.030

  日期：2007.11

  A series of substituted imidazopiperidine amides has been prepared and evaluated for inhibition of dipeptidyl peptidase IV (DPP-4). Substitution at the 1- and 3-positions produced increased selectivity for DPP-4 relative to DPP-8 and DPP-9. Compounds in this series had IC(50) values as low as 5.8 nM for inhibition of DPP-4.

  已经制备了一系列取代的咪唑并哌啶酰胺，并评价了其对二肽基肽酶IV（DPP-4）的抑制作用。相对于DPP-8和DPP-9，在1位和3位取代可提高DPP-4的选择性。该系列化合物抑制DPP-4的IC（50）值低至5.8 nM。