(2S)-2-amino-2-cyclohexyl-1-((3RS)-3-fluoro-pyrrolidin-1-yl)-ethanone | 693783-72-1

• 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: (2S)-2-amino-2-cyclohexyl-1-((3RS)-3-fluoro-pyrrolidin-1-yl)-ethanone
• 英文别名: (2S)-2-amino-2-cyclohexyl-1-(3-fluoropyrrolidin-1-yl)ethanone
• CAS: 693783-72-1
• 化学式: C₁₂H₂₁FN₂O
• 分子量: 228.31
• InChiKey: MSOYZLRUNBBCGC-DTIOYNMSSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.92
• 拓扑面积：
  46.3
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  [(1S)1-cyclohexyl-2-((3RS)-3-fluoro-pyrrolidin-1-yl)-2-oxo-ethyl]-carbamic acid tert-butyl ester 以 乙酸乙酯 为溶剂， 反应 0.68h， 以the the title compound of Example 1 was obtained as a solid which的产率得到(2S)-2-amino-2-cyclohexyl-1-((3RS)-3-fluoro-pyrrolidin-1-yl)-ethanone
  参考文献：
  名称：

  Dipeptidyl peptidase IV inhibiting fluorinated cyclic amides

  摘要：

  本发明涉及新的治疗活性和选择性的二肽基肽酶-IV酶抑制剂，药物组合物包括这些化合物，以及使用这些化合物治疗与DPP-IV处理的蛋白质相关的疾病，如2型糖尿病、高血糖、糖耐量受损、代谢综合征（综合征X或胰岛素抵抗综合征）、葡萄糖尿、代谢性酸中毒、白内障、糖尿病神经病、糖尿病肾病、糖尿病视网膜病变、糖尿病心肌病、1型糖尿病、肥胖、肥胖加剧的疾病、高血压、高脂血症、动脉硬化、骨质疏松症、骨质疏松、虚弱、骨质流失、骨折、急性冠状动脉综合征、多囊卵巢综合征引起的不孕症、短肠综合征、焦虑、抑郁、失眠、慢性疲劳、癫痫、饮食障碍、慢性疼痛、酒精成瘾、与肠道动力相关的疾病、溃疡、肠易激综合征、炎症性肠病，并且预防2型糖尿病的疾病进展。本发明还涉及一种用于识别糖尿病胰岛素分泌剂的方法。

  公开号：

  US20040110817A1

文献信息

• 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。
• Method of preparing a composition comprising a GPR119 agonist
  申请人：Arena Pharmaceuticals, Inc.

  公开号：EP2322152A1

  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-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。