trans-8-(2-(R)-amino-cyclohexyl-(R)-amino)-7-(2-iodo-benzyl)-3-methyl-3,7-dihydro-purine-2,6-dione | 502980-57-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并嘧啶类
• 英文名称: trans-8-(2-(R)-amino-cyclohexyl-(R)-amino)-7-(2-iodo-benzyl)-3-methyl-3,7-dihydro-purine-2,6-dione
• 英文别名: 8-[[(1R,2R)-2-aminocyclohexyl]amino]-7-[(2-iodophenyl)methyl]-3-methylpurine-2,6-dione
• CAS: 502980-57-6
• 化学式: C₁₉H₂₃IN₆O₂
• 分子量: 494.335
• InChiKey: ZHUDJJDZNLLXLC-ZIAGYGMSSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  105
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• Hetrocyclic compounds that are inhibitors of the enzyme DPP-IV
  申请人：——

  公开号：US20030199528A1

  公开（公告）日：2003-10-23

  The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity. The present inhibitors are novel purine derivatives, attached at position 8 of the purine skeleton to a diamine.

  本发明涉及治疗活性和选择性抑制酶DPP-IV的化合物，包括药物组合物和利用这些化合物制造用于治疗与受DPP-IV失活的蛋白质相关的疾病的药物，如2型糖尿病和肥胖症。本发明的抑制剂是新颖的嘌呤衍生物，在嘌呤骨架的位置8处连接到二胺。
• Method and composition for treatment of diabetes, hypertension, chronic heart failure and fluid retentive states
  申请人：——

  公开号：US20030236272A1

  公开（公告）日：2003-12-25

  The present invention is related to a method and composition for treatment of diabetes, hypertension, chronic heart failure and fluid retentive states comprising administering inhibitors of the enzymes NEP and DPP-IV to individuals suffering from one or more of those conditions. Inhibition of the activity of the two enzymes will potentiate the insulin releasing activity of endogenous GLP-1 and other DPP-IV substrates like GIP.

  本发明涉及一种治疗糖尿病、高血压、慢性心力衰竭和液体潴留状态的方法和组合物，包括向患有这些疾病中的一个或多个的个体中施用NEP和DPP-IV酶抑制剂。抑制这两种酶的活性将增强内源性GLP-1和其他DPP-IV底物如GIP的胰岛素释放活性。
• HETEROCYCLIC COMPOUNDS THAT ARE INHIBITORS OF THE ENZYME DPP-IV
  申请人：NOVO NORDISK A/S

  公开号：EP1463727A2

  公开（公告）日：2004-10-06
• METHOD AND COMPOSITION FOR TREATMENT OF DIABETES, HYPERTENSION, CHRONIC HEART FAILURE AND FLUID RETENTIVE STATES
  申请人：NOVO NORDISK A/S

  公开号：EP1496877B1

  公开（公告）日：2008-10-01
• [EN] HETEROCYCLIC COMPOUNDS THAT ARE INHIBITORS OF THE ENZYME DPP-IV<br/>[FR] COMPOSES HETEROCYCLIQUES CONSTITUANT DES INHIBITEURS DE L'ENZYME DPP-IV
  申请人：NOVO NORDISK AS

  公开号：WO2003024965A2

  公开（公告）日：2003-03-27

  The present invention relates to therapeutically active and selective inhibitors (Formula II)of the enzyme DPP-IV, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity. The present inhibitors are novel purine derivatives, attached at position 8 of the purine skeleton to a diamine.