5-iodo-1-(2-pyrrolidin-1-yl-ethyl)-1H-indazole | 690265-62-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡唑类
• 英文名称: 5-iodo-1-(2-pyrrolidin-1-yl-ethyl)-1H-indazole
• 英文别名: 5-Iodo-1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazole；5-iodo-1-(2-pyrrolidin-1-ylethyl)indazole
• CAS: 690265-62-4
• 化学式: C₁₃H₁₆IN₃
• 分子量: 341.195
• InChiKey: AKCOQKOMNOVTEL-UHFFFAOYSA-N

物化性质

• 沸点：
  422.7±25.0 °C(Predicted)
• 密度：
  1.70±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  21.1
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  5-iodo-1-(2-pyrrolidin-1-yl-ethyl)-1H-indazole 、 5-(4-chloro-phenyl)-2-ethynyl-pyridine 生成 5-[5-(4-chloro-phenyl)-pyridin-2-ylethynyl]-1-(2-pyrrolidin-1-yl-ethyl)-1H-indazole hydroiodide
  参考文献：
  名称：

  Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds

  摘要：

  本发明涉及一般式I的炔化合物，其中组和残基A、B、W、X、Y、Z、R1和R2具有权利要求1中给出的含义。本发明还涉及包含至少一种根据本发明的炔烃的制药组合物。鉴于它们的MCH受体拮抗活性，本发明的制药组合物适用于治疗代谢障碍和/或进食障碍，特别是肥胖症、贪食症、厌食症、过度进食和糖尿病。

  公开号：

  US07452911B2
• 作为产物：
  描述：

  4-碘-2-甲基苯胺 在 sodium nitrite 、 caesium carbonate 作用下， 以 水 、 溶剂黄146 、 二甲基亚砜 为溶剂， 生成 5-iodo-1-(2-pyrrolidin-1-yl-ethyl)-1H-indazole
  参考文献：
  名称：

  5-(Pyridinon-1-yl)indazoles and 5-(furopyridinon-5-yl)indazoles as MCH-1 antagonists

  摘要：

  A new series of 5-(pyridinon-1-yl)indazoles with MCH-1 antagonist activity were synthesized. Potential cardiovascular risk for these compounds was assessed based upon their interaction with the hERG potassium channel in a mini-patch clamp assay. Selected compounds were studied in a 5-day diet-induced obese mouse model to evaluate their potential use as weight loss agents. Structural modification of the 5-(pyridinon-1-yl) indazoles to give 5-(furopyridinon-5-yl) indazoles provided compounds with enhanced pharmacokinetic properties and improved efficacy. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.09.039

文献信息

• 5-FUROPYRIDINONE SUBSTITUTED INDAZOLES
  申请人：Guzzo Peter Robert

  公开号：US20090318439A1

  公开（公告）日：2009-12-24

  Compounds are disclosed. The compounds act as MCH1 modulators. Other embodiments are also disclosed.

  揭示了化合物。这些化合物作为MCH1调节剂。还揭示了其他实施例。
• ALKYNE COMPOUNDS WITH MCH ANTAGONISTIC ACTIVITY AND MEDICAMENTS COMPRISING THESE COMPOUNDS
  申请人：Stenkamp Dirk

  公开号：US20090069282A1

  公开（公告）日：2009-03-12

  The present invention relates to alkyne compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R 1 and R 2 have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one alkyne according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.

  本发明涉及一般式I的炔化合物，其中A、B、W、X、Y、Z、R1和R2的基团和残基具有权利要求1中给出的含义。本发明还涉及包含至少一种根据本发明的炔烃的制药组合物。鉴于它们的MCH受体拮抗活性，根据本发明的制药组合物适用于治疗代谢性疾病和/或进食障碍，特别是肥胖症、暴食症、厌食症、过度进食和糖尿病。
• 5-furopyridinone substituted indazoles
  申请人：Albany Molecular Research, Inc.

  公开号：US08101632B2

  公开（公告）日：2012-01-24

  Compounds are disclosed. The compounds act as MCH1 modulators. Other embodiments are also disclosed.

  本文披露了化合物。这些化合物作为MCH1调节剂。还披露了其他实施方案。
• NEUE ALKIN-VERBINDUNGEN MIT MCH-ANTAGONISTISCHER WIRKUNG UND DIESE VERBINDUNGEN ENTHALTENDE ARZNEIMITTEL
  申请人：Boehringer Ingelheim Pharma GmbH & Co. KG

  公开号：EP1558578B1

  公开（公告）日：2013-03-13
• US7452911B2
  申请人：——

  公开号：US7452911B2

  公开（公告）日：2008-11-18