4-[6-(2-fluoro-4-methanesulfonyl-phenoxy)-5-methyl-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid (R)-tetrahydro-furan-3-yl ester

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 4-[6-(2-fluoro-4-methanesulfonyl-phenoxy)-5-methyl-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid (R)-tetrahydro-furan-3-yl ester
• 英文别名: [(3R)-oxolan-3-yl] 4-[6-(2-fluoro-4-methylsulfonylphenoxy)-5-methylpyrimidin-4-yl]oxypiperidine-1-carboxylate
• 化学式: C₂₂H₂₆FN₃O₇S
• 分子量: 495.529
• InChiKey: AYBBTCLLYOYTHS-MRXNPFEDSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  34
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  126
• 氢给体数：
  0
• 氢受体数：
  10

反应信息

• 作为产物：
  描述：

  4-(2-fluoro-4-methanesulfonyl-phenoxy)-5-methyl-6-(piperidin-4-yloxy)-pyrimidine 、 (R)-(-)-3-羟基四氢呋喃 在 三乙胺 作用下， 以 四氢呋喃 为溶剂， 反应 48.5h， 以42%的产率得到4-[6-(2-fluoro-4-methanesulfonyl-phenoxy)-5-methyl-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid (R)-tetrahydro-furan-3-yl ester
  参考文献：
  名称：

  [EN] TRISUBSTITUTED ARYL AND HETEROARYL DERIVATIVES AS MODULATORS OF METABOLISM AND THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO
  [FR] DERIVES ARYLES ET HETEROARYLES TRISUBSTITUES UTILISES EN TANT QUE MODULATEURS DU METABOLISME ET PROPHYLAXIE ET TRAITEMENT DE TROUBLES AFFERENTS

  摘要：

  本发明涉及公式（I）的某些三取代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紊乱及其并发症，如糖尿病和肥胖方面是有用的。

  公开号：

  WO2005007647A1

文献信息

• Trisubstituted 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：US20050070562A1

  公开（公告）日：2005-03-31

  The present invention relates to certain trisubstituted 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）的某些三取代芳基和杂环芳基衍生物，其是代谢调节剂。因此，本发明的化合物对于预防或治疗代谢性疾病及其并发症（如糖尿病和肥胖症）是有用的。
• Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the phophylaxis and treatment of disorders related thereto
  申请人：Jones M. Robert

  公开号：US20070155763A1

  公开（公告）日：2007-07-05

  The present invention relates to certain trisubstituted 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）的某些三取代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方面是有用的，如糖尿病和肥胖症。
• 1,2,3-TRISUBSTITUTED 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：US20110112060A1

  公开（公告）日：2011-05-12

  The present invention relates to certain trisubstituted 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）的某些三取代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紊乱及其并发症，如糖尿病和肥胖症方面是有用的。
• 1,2,3-trisubstituted 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：US08546429B2

  公开（公告）日：2013-10-01

  The present invention relates to certain trisubstituted 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.

  本发明涉及化合物公式（I）的某些三取代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。
• Method of identifying GLP-1 secretagogues
  申请人：Arena Pharmaceuticals, Inc.

  公开号：EP2322150A2

  公开（公告）日：2011-05-18

  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-l 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-l level. The present invention also relates to the use of a G protein-coupled receptor to screen for GLP-l secretagogues.

  本发明涉及将一定量的GPR1 19激动剂与一定量的二肽基肽酶IV（DPP-IV）抑制剂组合使用，使该组合在降低受试者血糖水平或提高其血液中GLP-l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抑制剂所产生的效果，以及将这种组合用于治疗或预防糖尿病及其相关病症或通过提高血液中GLP-l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-l 促泌剂。