3-Aminomethyl-4-(2,4-dichloro-phenyl)-7,8-dimethoxy-5H-indeno[1,2-b]pyridin-2-ylamine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 3-Aminomethyl-4-(2,4-dichloro-phenyl)-7,8-dimethoxy-5H-indeno[1,2-b]pyridin-2-ylamine
• 英文别名: 3-(aminomethyl)-4-(2,4-dichlorophenyl)-7,8-dimethoxy-5H-indeno[1,2-b]pyridin-2-amine
• 化学式: C₂₁H₁₉Cl₂N₃O₂
• 分子量: 416.307
• InChiKey: NMMXMFFMHIZMPW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  83.4
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  5,6-二甲氧基茚酮 在 lithium aluminium tetrahydride 、 ammonium acetate 作用下， 以 四氢呋喃 、 甲苯 为溶剂， 反应 7.0h， 生成 3-Aminomethyl-4-(2,4-dichloro-phenyl)-7,8-dimethoxy-5H-indeno[1,2-b]pyridin-2-ylamine
  参考文献：
  名称：

  Aminomethylpyridines as DPP-IV inhibitors

  摘要：

  In a novel series of DPP-IV inhibitors, a large increase of inhibitory activity was achieved by optimisation of aromatic substituents and conformational restriction. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2004.04.049

文献信息

• Pyridine and quinoline derivatives
  申请人：——

  公开号：US20030195188A1

  公开（公告）日：2003-10-16

  The present invention provides compounds of formula (I) 1 wherein R 1 , R 2 , R 3 and R 4 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.

  本发明提供了公式（I）1的化合物，其中R1，R2，R3和R4如规范中所定义，并且其药学上可接受的盐。这些化合物对于治疗和/或预防与DPP IV相关的疾病非常有用，例如糖尿病，特别是非胰岛素依赖性糖尿病和糖耐量受损。
• Combination therapy for the treatment of diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood GLP-1 level
  申请人：Arena Pharmaceuticals, Inc.

  公开号：EP1808168A1

  公开（公告）日：2007-07-18

  The present invention concerns combination of an amount of a GPR1 19 agonist with an amount of a dipeptidyl peptidase IV (DPP-IV) inhibitor such that the combination provides an effect in lowering a blood glucose level or in increasing a blood GLP-I level in a subject over that provided by the amount of the GPR1 19 agonist or the amount of the DPP-FV inhibitor alone and the use of such a combination for treating or preventing diabetes and conditions related thereto or conditions ameliorated by increasing a blood GLP-I level. The present invention also relates to the use of a G protein-coupled receptor to screen for GLP-I secretagogues.

  本发明涉及一定量的 GPR1 19 激动剂与一定量的二肽基肽酶 IV (DPP-IV) 抑制剂的组合，从而使该组合在降低受试者血糖水平或提高血 GLP-I 水平方面的效果优于单独使用一定量的 GPR1 19 激动剂或 DPP-FV 抑制剂所提供的效果，以及使用这种组合治疗或预防糖尿病及其相关病症或通过提高血 GLP-I 水平而改善的病症。 本发明还涉及使用 G 蛋白偶联受体筛选 GLP-I 促泌剂。
• Method of identifying GLP-1 secretagogues
  申请人：Arena Pharmaceuticals, Inc.

  公开号：EP1997484A2

  公开（公告）日：2008-12-03

  The present invention concerns combination of an amount of a GPR119 agonist with an amount of a dipeptidyl peptidase IV (DPP-IV) inhibitor such that the combination provides an effect in lowering a blood glucose level or in increasing a blood GLP-1 level in a subject over that provided by the amount of the GPR119 agonist or the amount of the DPP-FV inhibitor alone and the use of such a combination for treating or preventing diabetes and conditions related thereto or conditions ameliorated by increasing a blood GLP-1 level. The present invention also relates to the use of a G protein-coupled receptor to screen for GLP-1 secretagogues.

  本发明涉及将一定量的GPR119激动剂与一定量的二肽基肽酶IV（DPP-IV）抑制剂组合，使该组合在降低受试者血糖水平或提高血GLP-1水平方面的效果超过单独使用一定量的GPR119激动剂或DPP-FV抑制剂所提供的效果，以及使用这种组合治疗或预防糖尿病及其相关病症或通过提高血GLP-1水平而改善的病症。 本发明还涉及使用 G 蛋白偶联受体筛选 GLP-1 促泌剂。
• Combination therapy for the treatment of diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood GLP-1 level
  申请人：Arena Pharmaceuticals, Inc.

  公开号：EP2116235A1

  公开（公告）日：2009-11-11

  The present invention concerns combination of an amount of a GPR1 19 agonist with an amount of a dipeptidyl peptidase IV (DPP-IV) inhibitor such that the combination provides an effect in lowering a blood glucose level or in increasing a blood GLP-I level in a subject over that provided by the amount of the GPR1 19 agonist or the amount of the DPP-FV inhibitor alone and the use of such a combination for treating or preventing diabetes and conditions related thereto or conditions ameliorated by increasing a blood GLP-I level. The present invention also relates to the use of a G protein-coupled receptor to screen for GLP-I secretagogues.

  本发明涉及一定量的 GPR1 19 激动剂与一定量的二肽基肽酶 IV (DPP-IV) 抑制剂的组合，从而使该组合在降低受试者血糖水平或提高血 GLP-I 水平方面的效果优于单独使用一定量的 GPR1 19 激动剂或 DPP-FV 抑制剂所提供的效果，以及使用这种组合治疗或预防糖尿病及其相关病症或通过提高血 GLP-I 水平而改善的病症。 本发明还涉及使用 G 蛋白偶联受体筛选 GLP-I 促泌剂。
• Use of GPR119 receptor agonists for increasing bone mass and for treating osteoporosis, as well as combination therapy relating thereto
  申请人：Arena Pharmaceuticals, Inc.

  公开号：EP2253311A2

  公开（公告）日：2010-11-24

  The present invention relates to the use of GPR119 receptor agonists for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. The present invention further relates to the use of a GPR119 receptor agonist in combination with a dipeptidyl peptidase IV (DPP-IV) inhibitor for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. A GPR119 receptor agonist and the combination of a GPR119 receptor agonist and a DPP-IV inhibitor promote bone formation in an individual.

  本发明涉及 GPR119 受体激动剂用于治疗或预防以低骨量为特征的疾病，如骨质疏松症，以及用于增加个体的骨量。本发明进一步涉及 GPR119 受体激动剂与二肽基肽酶 IV (DPP-IV) 抑制剂联合用于治疗或预防以低骨量为特征的疾病，如骨质疏松症，以及增加个体的骨量。GPR119 受体激动剂以及 GPR119 受体激动剂与 DPP-IV 抑制剂的组合可促进个体的骨形成。