ethyl 7-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-6,8-dihydro-5H-imidazo[1,2-a]pyrazine-2-carboxylate

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: ethyl 7-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-6,8-dihydro-5H-imidazo[1,2-a]pyrazine-2-carboxylate
• 化学式: C₁₉H₂₂F₂N₄O₃
• 分子量: 392.4
• InChiKey: NHKYGICOBKKEDL-CQSZACIVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  28
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  90.4
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

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

  公开号：WO2004058266A1

  公开（公告）日：2004-07-15

  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.

  本发明涉及3-氨基-4-苯基丁酸衍生物，这些衍生物是二肽基肽酶-IV酶（'DP-IV抑制剂'）的抑制剂，并且在治疗或预防二肽基肽酶-IV酶参与的疾病中有用，如糖尿病，特别是2型糖尿病。该发明还涉及包含这些化合物的药物组合物以及在预防或治疗二肽基肽酶-IV酶参与的这类疾病中使用这些化合物和组合物。
• 3-Amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
  申请人：Duffy L Joseph

  公开号：US20060052382A1

  公开（公告）日：2006-03-09

  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.

  本发明涉及3-氨基-4-苯基丁酸衍生物，它们是二肽酶IV酶（“DP-IV抑制剂”）的抑制剂，对于涉及二肽酶IV酶的疾病，如糖尿病，特别是2型糖尿病的治疗或预防有用。本发明还涉及包含这些化合物的制药组合物以及这些化合物和组合物在涉及二肽酶IV酶的这类疾病的预防或治疗中的使用。
• 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。