methyl 1-(pyridin-2-yl)-1H-pyrrolo[2,3-b]pyridine-3-carboxylate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 英文名称: methyl 1-(pyridin-2-yl)-1H-pyrrolo[2,3-b]pyridine-3-carboxylate
• 英文别名: methyl 1-pyridin-2-ylpyrrolo[2,3-b]pyridine-3-carboxylate
• 化学式: C₁₄H₁₁N₃O₂
• 分子量: 253.26
• InChiKey: NRGFGBSGCARZLM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  57
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  methyl 1-(pyridin-2-yl)-1H-pyrrolo[2,3-b]pyridine-3-carboxylate 在 sodium hydroxide 作用下， 以 四氢呋喃 为溶剂， 反应 200.0h， 生成 1-(pyridin-2-yl)-1H-pyrrolo[2,3-b]pyridine-3-carboxylic acid
  参考文献：
  名称：

  [EN] 3-(GUANIDINOCARBONYL)HETEROCYCLE DERIVATIVES, PREPARATION PROCESS AND INTERMEDIATES OF THIS PROCESS, THEIR USE AS MEDICAMENTS, AND PHARMACEUTICAL COMPOSITIONS INCLUDING THEM
  [FR] DERIVES HETEROCYCLIQUES 3-(GUANIDINOCARBONYLE), LEUR PROCEDE DE PREPARATION ET INTERMEDIAIRES POUR LEDIT PROCEDE, LEUR UTILISATION EN TANT QUE MEDICAMENTS ET COMPOSITIONS PHARMACEUTIQUE LES COMPRENANT

  摘要：

  本发明涉及公式（I）的新化合物及其药学上可接受的盐。这些新化合物适用于例如心律失常药物，其具有心脏保护成分，用于预防和治疗心肌梗死以及治疗心绞痛。它们还能预防性地抑制与缺血性损伤发展相关的病理生理过程，特别是在诱发缺血性心律失常和心力衰竭方面。

  公开号：

  WO2004111048A1
• 作为产物：
  描述：

  1H-吡咯并[2,3-B]吡啶-3-羧酸甲酯 、 2-氟吡啶 在 sodium hydride 作用下， 以 N,N-二甲基甲酰胺 、 mineral oil 为溶剂， 反应 14.17h， 生成 methyl 1-(pyridin-2-yl)-1H-pyrrolo[2,3-b]pyridine-3-carboxylate
  参考文献：
  名称：

  [EN] 5-HT3 RECEPTOR ANTAGONISTS
  [FR] ANTAGONISTES DU RÉCEPTEUR 5-HT3

  摘要：

  本发明提供了式(I)的5-HT3受体拮抗剂，用于治疗通过抑制5-HT3受体可治疗的疾病，如呕吐、疼痛、药物成瘾、神经退行性和精神障碍以及胃肠道疾病。还提供了含有这类化合物的药物组合物和制备这类化合物的方法。

  公开号：

  WO2014014951A1

文献信息

• [EN] 3-(GUANIDINOCARBONYL)HETEROCYCLE DERIVATIVES, PREPARATION PROCESS AND INTERMEDIATES OF THIS PROCESS, THEIR USE AS MEDICAMENTS, AND PHARMACEUTICAL COMPOSITIONS INCLUDING THEM<br/>[FR] DERIVES HETEROCYCLIQUES 3-(GUANIDINOCARBONYLE), LEUR PROCEDE DE PREPARATION ET INTERMEDIAIRES POUR LEDIT PROCEDE, LEUR UTILISATION EN TANT QUE MEDICAMENTS ET COMPOSITIONS PHARMACEUTIQUE LES COMPRENANT
  申请人：AVENTIS PHARMA GMBH

  公开号：WO2004111048A1

  公开（公告）日：2004-12-23

  The present invention relates to the novel compounds of the formula (I) and their pharmaceutically acceptable salts. The inventive compounds are suitable, for example, as antiarrhythmic medicaments with a cardioprotective component for infarction prophylaxis and infarction treatment and for the treatment of angina pectoris. They also inhibit in a preventive manner the pathophysiologicaI processes associated with the development of ischemia-induced damage, in particular in the triggering of ischemia-induced cardiac arrhythmias and of heart failure.

  本发明涉及公式（I）的新化合物及其药学上可接受的盐。这些新化合物适用于例如心律失常药物，其具有心脏保护成分，用于预防和治疗心肌梗死以及治疗心绞痛。它们还能预防性地抑制与缺血性损伤发展相关的病理生理过程，特别是在诱发缺血性心律失常和心力衰竭方面。
• Derivatives of 3-(guanidinocarbonyl) heterocycle, methods of preparation and intermediates thereof, their use as medicaments, and pharmaceutical compositions therefrom
  申请人：Carry Jean-Christophe

  公开号：US20050014758A1

  公开（公告）日：2005-01-20

  The present invention discloses and claims compounds of formula I and their pharmaceutically acceptable salts, and methods of using said compounds of formula I, either alone or in combination with other medicaments, as antiarrhythmic medicaments with a cardioprotective component for prophylaxis or treatment of infarction, for the treatment of angina pectoris, and as inhibitors of pathophysiological processes associated with the development of ischemia-induced damage, in particular in the triggering of ischemia-induced cardiac arrhythmias and of heart failure. Pharmaceutical compositions comprising compounds of formula I or compounds of formula I in combination with one or more other medicaments and processes for the preparation of compounds of formula I are also disclosed and claimed.

  本发明揭示和声明了I式化合物及其药物可接受的盐，以及使用该I式化合物，单独或与其他药物联合使用，作为具有心脏保护成分的抗心律失常药物，用于预防或治疗梗死，治疗心绞痛，并作为与缺血诱导损伤发展相关的病理生理过程的抑制剂，特别是在诱发缺血诱导的心脏心律失常和心力衰竭方面。本发明还揭示和声明了包括I式化合物或I式化合物与一种或多种其他药物组合的制药组合物，以及制备I式化合物的方法。
• Derivatives of 3-(Guanidinocarbonyl) heterocycle, methods of preparation and intermediates thereof, their use as medicaments, and pharmaceutical compositions therefrom
  申请人：Sanofi-Aventis Deutschland GmbH

  公开号：US07230007B2

  公开（公告）日：2007-06-12

  The present invention discloses and claims compounds of formula I and their pharmaceutically acceptable salts, and methods of using said compounds of formula I, either alone or in combination with other medicaments, as antiarrhythmic medicaments with a cardioprotective component for prophylaxis or treatment of infarction, for the treatment of angina pectoris, and as inhibitors of pathophysiological processes associated with the development of ischemia-induced damage, in particular in the triggering of ischemia-induced cardiac arrhythmias and of heart failure. Pharmaceutical compositions comprising compounds of formula I or compounds of formula I in combination with one or more other medicaments and processes for the preparation of compounds of formula I are also disclosed and claimed.

  本发明揭示和声明了式I的化合物及其药学上可接受的盐，并且揭示了使用该式I的化合物，无论是单独使用还是与其他药物联合使用，作为具有心脏保护成分的抗心律失常药物，用于预防或治疗梗死，治疗心绞痛，并作为抑制与缺血引起的损伤发展相关的病理生理过程的药物，特别是在触发缺血诱发的心脏心律失常和心力衰竭方面。还揭示和声明了包含式I化合物或式I化合物与一个或多个其他药物组合的制药组合物，以及制备式I化合物的方法。
• 5-HT3 RECEPTOR ANTAGONISTS
  申请人：ENVOY THERAPEUTICS, INC.

  公开号：US20140024644A1

  公开（公告）日：2014-01-23

  The present invention provides 5-HT3 receptor antagonists of Formula (I): which are useful for the treatment of diseases treatable by inhibition of 5-HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

  本发明提供了5-HT3 受体拮抗剂的化学式 (I)：这些化合物对于治疗可通过抑制5-HT3 受体治疗的疾病，例如呕吐、疼痛、药物成瘾、神经退行性和精神障碍以及胃肠道疾病非常有用。还提供了包含这些化合物的制药组合物以及制备这些化合物的过程。
• 5-HT3 receptor antagonists
  申请人：Envoy Therapeutics, Inc.

  公开号：US09012447B2

  公开（公告）日：2015-04-21

  The present invention provides 5-HT3 receptor antagonists of Formula (I): which are useful for the treatment of diseases treatable by inhibition of 5-HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

  本发明提供了式（I）的5-HT3受体拮抗剂，可用于治疗通过抑制5-HT3受体可治疗的疾病，如恶心、疼痛、药物成瘾、神经退行性和精神障碍以及胃肠疾病。还提供了含有这些化合物的制药组合物和制备这些化合物的过程。