4-[[6-[(6-甲基磺酰基-2-甲基吡啶-3-基)氨基]-5-甲氧基嘧啶-4-基]氧基]哌啶-1-羧酸异丙酯 | 897732-93-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 中文名称: 4-[[6-[(6-甲基磺酰基-2-甲基吡啶-3-基)氨基]-5-甲氧基嘧啶-4-基]氧基]哌啶-1-羧酸异丙酯
• 英文名称: APD597
• 英文别名: JNJ-38431055；Isopropyl 4-((5-methoxy-6-((2-methyl-6-(methylsulfonyl)pyridin-3-yl)amino)pyrimidin-4-yl)oxy)piperidine-1-carboxylate；propan-2-yl 4-[5-methoxy-6-[(2-methyl-6-methylsulfonylpyridin-3-yl)amino]pyrimidin-4-yl]oxypiperidine-1-carboxylate
• CAS: 897732-93-3
• 化学式: C₂₁H₂₉N₅O₆S
• 分子量: 479.557
• InChiKey: WPDCHTSXOPUOII-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  33
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  141
• 氢给体数：
  1
• 氢受体数：
  10

反应信息

• 作为反应物：
  描述：

  4-[[6-[(6-甲基磺酰基-2-甲基吡啶-3-基)氨基]-5-甲氧基嘧啶-4-基]氧基]哌啶-1-羧酸异丙酯 在 盐酸 作用下， 生成 4-[6-(6-methanesulfonyl-2-methyl-pyridin-3-ylamino)-5-methoxy-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester hydrochloride
  参考文献：
  名称：

  Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto

  摘要：

  本发明涉及某些取代的吡啶基和嘧啶基衍生物，其化学式为（Ia），这些衍生物是代谢调节剂。因此，本发明的化合物在治疗与代谢相关的疾病和并发症方面非常有用，如糖尿病和肥胖症。

  公开号：

  US20060155128A1
• 作为产物：
  描述：

  (6-chloro-5-methoxy-pyrimidin-4-yl)-(6-methanesulfonyl-2-methyl-pyridin-3-yl)-amine 、 4-羟基哌啶-1-甲酸异丙酯 在 4-羟基哌啶-1-甲酸异丙酯 作用下， 生成 4-[[6-[(6-甲基磺酰基-2-甲基吡啶-3-基)氨基]-5-甲氧基嘧啶-4-基]氧基]哌啶-1-羧酸异丙酯
  参考文献：
  名称：

  PROCESS FOR THE PREPARATION OF TRI-SUBSTITUTED PYRIDINE AND TRI-SUBSTITUTED PYRIMIDINE DERIVATIVES USEFUL AS GDIR AGONISTS

  摘要：

  本发明涉及一种制备三取代吡啶和三取代嘧啶衍生物的新型方法，其作为葡萄糖依赖性胰岛素促进受体激动剂，用于治疗代谢相关疾病及其并发症，例如糖尿病和肥胖症。

  公开号：

  US20100113479A1

文献信息

• MODULATORS OF METABOLISM AND THE TREATMENT OF DISORDERS RELATED THERETO
  申请人：Jones Robert M.

  公开号：US20090286816A1

  公开（公告）日：2009-11-19

  The present invention relates to 4-[5-Methoxy-6-(2-methyl-6-[1,2,4]triazol-1-yl-pyridin-3-ylamino)-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester, pharmaceutically acceptable salts, solvates and hydrates thereof that are modulators of glucose metabolism. Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity. (Formula I)

  本发明涉及4-[5-甲氧基-6-(2-甲基-6-[1,2,4]三唑-1-基吡啶-3-基氨基)-嘧啶-4-氧基]-哌啶-1-羧酸异丙酯，其药学上可接受的盐、溶剂合物和水合物，它们是葡萄糖代谢调节剂。因此，本发明的化合物在治疗与代谢相关的疾病和并发症方面具有用处，如糖尿病和肥胖。 (化学式 I)
• MODIFIED-RELEASE DOSAGE FORMS OF 5-HT2C AGONISTS USEFUL FOR WEIGHT MANAGEMENT
  申请人：Arena Pharmaceuticals, Inc.

  公开号：EP3485878A1

  公开（公告）日：2019-05-22

  The present invention relates to methods for weight management that utilize modified-release dosage forms comprising (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine salts and crystalline forms thereof. The present invention further relates to (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine salts, crystalline forms thereof and modified-release dosage forms comprising them.

  本发明涉及利用含有(R)-8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并哌啶盐及其结晶形式的改良释放剂型的体重管理方法。本发明还涉及(R)-8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并哌啶盐、其结晶形式以及含有它们的改良释放剂型。
• [EN] PROCESS FOR THE PREPARATION OF 4- [6-(6-METHANESULFONYL-2-METHYL-PYRIDIN-3-YLAMINO) -5-METHOXY-PYRIMIDIN-4-YLOXY]-PIPERIDINE-1-CARBOXYLIC ACID ISOPROPYL ESTER<br/>[FR] PROCÉDÉ DE PRÉPARATION DE L'ESTER ISOPROPYLIQUE DE L'ACIDE 4-[6-(6-MÉTHANESULFONYL-2-MÉTHYL-PYRIDIN-3-YLAMINO)-5-MÉTHOXY-PYRIMIDIN-4-YLOXY]-PIPÉRIDINE-1-CARBOXYLIQUE
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2010135506A1

  公开（公告）日：2010-11-25

  The present invention is directed to a process for the preparation of 4-[6- (6-methanesulfonyl-2-methyl-pyhdin-3-ylamino)-5-methoxy-pyrimidin-4-yloxy]- piperidine-1 -carboxylic acid isopropyl ester, useful as glucose dependent insulinotropic receptor agonist, for the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity.

  本发明涉及一种制备4-[6-(6-甲磺酰基-2-甲基吡啶-3-基氨基)-5-甲氧基嘧啶-4-氧基]-哌啶-1-羧酸异丙酯的方法，该方法可用作葡萄糖依赖性胰岛素受体激动剂，用于治疗代谢相关疾病及其并发症，如糖尿病和肥胖症。
• Substituted pyrindinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto
  申请人：Jones M. Robert

  公开号：US20070078150A1

  公开（公告）日：2007-04-05

  The present invention relates to certain substituted pyridinyl and pyrimidinyl derivatives of Fomula (Ia) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity.

  本发明涉及某些取代的吡啶基和嘧啶基衍生物，其化学式为(Ia)，它们是代谢调节剂。因此，本发明的化合物在代谢相关疾病及其并发症的治疗中是有用的，例如糖尿病和肥胖症。
• Modulators of metabolism and the treatment of disorders related thereto
  申请人：Jones Robert M.

  公开号：US20100004272A1

  公开（公告）日：2010-01-07

  The present invention relates to 4-[6-(6-methanesulfonyl-2-methyl-pyridin-3-ylamino)-5-methyl-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester, pharmaceutically acceptable salts, solvates and hydrates thereof that are modulators of glucose metabolism. Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity.

  本发明涉及4-[6-(6-甲烷磺酰基-2-甲基-吡啶-3-基氨基)-5-甲基嘧啶-4-氧基]-哌啶-1-羧酸异丙酯、其药学上可接受的盐、溶剂合物和水合物，这些化合物是葡萄糖代谢调节剂。因此，本发明的化合物在代谢相关疾病及其并发症的治疗中是有用的，如糖尿病和肥胖症。