4-[3-(4-methanesulfonyl-phenyl)-isoxazolo[4,5-d]pyrimidin-7-ylsulfanyl]-piperidine-1-carboxylic acid tert-butyl ester

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 4-[3-(4-methanesulfonyl-phenyl)-isoxazolo[4,5-d]pyrimidin-7-ylsulfanyl]-piperidine-1-carboxylic acid tert-butyl ester
• 英文别名: Tert-butyl 4-[[3-(4-methylsulfonylphenyl)-[1,2]oxazolo[4,5-d]pyrimidin-7-yl]sulfanyl]piperidine-1-carboxylate
• 化学式: C₂₂H₂₆N₄O₅S₂
• 分子量: 490.604
• InChiKey: AWEXVOQVKODMQO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  33
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  149
• 氢给体数：
  0
• 氢受体数：
  9

反应信息

• 作为产物：
  描述：

  7-chloro-3-(4-methanesulfonyl-phenyl)-isoxazolo[4,5-d]pyrimidine 、 1-N-boc-4-疏基哌啶 在 potassium carbonate 作用下， 以 DMF (N,N-dimethyl-formamide) 为溶剂， 反应 1.5h， 以35%的产率得到4-[3-(4-methanesulfonyl-phenyl)-isoxazolo[4,5-d]pyrimidin-7-ylsulfanyl]-piperidine-1-carboxylic acid tert-butyl ester
  参考文献：
  名称：

  [EN] FUSED-ARYL AND HETEROARYL DERIVATIVES AS MODULATORS OF METABOLISM AND THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO
  [FR] DERIVES ARYLE ET HETEROARYLE CONDENSES UTILISES COMME MODULATEURS DU METABOLISME ET PROPHYLAXIE ET TRAITEMENT DES TROUBLES METABOLIQUES

  摘要：

  公开号：

  WO2005007658A3

文献信息

• Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
  申请人：Jones M. Robert

  公开号：US20060142262A1

  公开（公告）日：2006-06-29

  The present invention relates to certain fused aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.

  本发明涉及公式（I）的某些融合芳基和杂芳基衍生物，它们是代谢调节剂。因此，本发明的化合物在预防或治疗代谢性疾病及其并发症方面非常有用，如糖尿病和肥胖症。
• FUSED-ARYL AND HETEROARYL DERIVATIVES AS MODULATORS OF METABOLISM AND THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO
  申请人：Jones Robert M.

  公开号：US20100093761A1

  公开（公告）日：2010-04-15

  The present invention relates to certain fused aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.

  本发明涉及公式（I）的某些融合芳基和杂环芳基衍生物，它们是代谢调节剂。因此，本发明的化合物在预防或治疗代谢性疾病及其并发症，如糖尿病和肥胖症方面是有用的。
• 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。
• 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。