ethyl 5-(2-methoxyethoxy)-1H-pyrrolo[2,3-c]pyridine-2-carboxylate | 755036-35-2

• 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: ethyl 5-(2-methoxyethoxy)-1H-pyrrolo[2,3-c]pyridine-2-carboxylate
• CAS: 755036-35-2
• 化学式: C₁₃H₁₆N₂O₄
• 分子量: 264.281
• InChiKey: LCGBPIFLBKLZLK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  19
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  73.4
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  ethyl 5-(2-methoxyethoxy)-1H-pyrrolo[2,3-c]pyridine-2-carboxylate 、 (1R,3S)-[3-(5-methyl-2-m-tolyloxazol-4-ylmethoxy)cyclohexyloxy]ethyl toluene-4-sulfonate 在 sodium hydride 作用下， 以 DMF (N,N-dimethyl-formamide) 为溶剂， 反应 0.5h， 生成 ethyl 5-(2-methoxyethoxy)-1-{2-[3-(5-methyl-2-m-tolyloxazol-4-ylmethoxy)cyclohexyloxy]ethyl}-1H-pyrrolo[2,3-c]pyridine-2-carboxylate
  参考文献：
  名称：

  1,3-substitued cycloalkyl derivatives having acidic, mostly heterocyclic groups; processes for their preparation and their use as pharmaceuticals

  摘要：

  本发明涉及具有酸性、大多数是杂环基团的1,3-取代环烷衍生物及其生理上可接受的盐和生理上功能衍生物。所描述的是式I中的化合物，其中基团如定义所示，以及它们的生理上可接受的盐和制备它们的过程。这些化合物适用于治疗和/或预防脂肪酸代谢障碍和葡萄糖利用障碍以及胰岛素抵抗涉及的疾病。

  公开号：

  US20040209932A1
• 作为产物：
  描述：

  ethyl 3-[2-(2-methoxyethoxy)-5-nitropyridin-4-yl]-2-oxopropionate potassium salt 在 palladium hydroxide on carbon 2,2,2-三氟乙醇 、 氢气 、 溶剂黄146 作用下， 以 甲醇 为溶剂， 反应 8.0h， 生成 ethyl 5-(2-methoxyethoxy)-1H-pyrrolo[2,3-c]pyridine-2-carboxylate
  参考文献：
  名称：

  1,3-substitued cycloalkyl derivatives having acidic, mostly heterocyclic groups; processes for their preparation and their use as pharmaceuticals

  摘要：

  本发明涉及具有酸性、大多数是杂环基团的1,3-取代环烷衍生物及其生理上可接受的盐和生理上功能衍生物。所描述的是式I中的化合物，其中基团如定义所示，以及它们的生理上可接受的盐和制备它们的过程。这些化合物适用于治疗和/或预防脂肪酸代谢障碍和葡萄糖利用障碍以及胰岛素抵抗涉及的疾病。

  公开号：

  US20040209932A1

文献信息

• Azaindole-derivatives as factor Xa inhibitors
  申请人：Nazare Marc

  公开号：US20050009828A1

  公开（公告）日：2005-01-13

  The present invention relates to compounds of the formula I wherein R 0 , R 1 , R 2 , R 3 , Q, V, G and M are as defined herein. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

  本发明涉及公式I的化合物，其中R0、R1、R2、R3、Q、V、G和M的定义如本文所述。公式I的化合物是有价值的药理活性化合物。它们表现出强烈的抗血栓作用，例如，适用于治疗和预防心血管疾病，如血栓栓塞性疾病或再狭窄。它们是血液凝固酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可应用于存在因子Xa和/或因子VIIa不良活性的情况，或者为了治疗或预防需要抑制因子Xa和/或因子VIIa的情况。本发明还涉及制备公式I化合物的方法，它们的使用，特别是作为药物的活性成分，并包括它们的制药制剂。
• 1,3-SUBSTITUTED CYCLOALKYL DERIVATIVES HAVING ACIDIC, MOSTLY HETEROCYCLIC GROUPS, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS
  申请人：Goerlitzer Jochen

  公开号：US20080249126A1

  公开（公告）日：2008-10-09

  The invention relates to 1,3-substituted cycloalkyl derivatives having acidic, mostly heterocyclic groups and to their physiologically acceptable salts and physiologically functional derivatives. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved.

  本发明涉及具有酸性、大多数为杂环基团的1,3-取代环烷衍生物及其生理上可接受的盐和生理上功能性衍生物。所描述的是式I的化合物，其中基团如定义所述，以及它们的生理上可接受的盐和制备它们的方法。这些化合物适用于治疗和/或预防脂肪酸代谢紊乱和葡萄糖利用紊乱以及涉及胰岛素抵抗的紊乱。
• Azaindole-Derivatives As Factor Xa Inhibitors
  申请人：NAZARE Marc

  公开号：US20080280946A1

  公开（公告）日：2008-11-13

  Indazole-derivatives as factor Xa inhibitors The present invention relates to compounds of the formula I wherein R 0 , R 1 , R 2 , R 3 , Q, V, G and M are as defined herein. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

  Indazole衍生物作为因子Xa抑制剂 本发明涉及公式I的化合物，其中R0，R1，R2，R3，Q，V，G和M的定义如本文所述。公式I的化合物是有价值的药理活性化合物。它们表现出强烈的抗血栓作用，并适用于例如治疗和预防心血管疾病，如血栓栓塞疾病或再狭窄。它们是血凝酶酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，通常可以应用于存在因子Xa和/或因子VIa的不良活性或需要抑制因子Xa和/或因子VIIa的治疗或预防的情况。此外，本发明还涉及制备公式I化合物的方法，它们的使用，特别是作为药物活性成分，并包括它们的制药制剂。
• 1,3-substituted cycloalkyl derivatives having acidic, mostly heterocyclic groups, processes for their preparation and their use as pharmaceuticals
  申请人：Aventis Pharma Deutschland GmbH

  公开号：US08048901B2

  公开（公告）日：2011-11-01

  The invention relates to 1,3-substituted cycloalkyl derivatives having acidic, mostly heterocyclic groups and to their physiologically acceptable salts and physiologically functional derivatives. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved.

  本发明涉及具有酸性、大多数为杂环基团的1,3-取代环烷衍生物及其生理上可接受的盐和生理上功能衍生物。所描述的化合物为公式I中的基团所定义，以及它们的生理上可接受的盐和制备它们的过程。这些化合物适用于治疗和/或预防脂肪酸代谢和葡萄糖利用障碍以及胰岛素抵抗相关的疾病。
• 1,3-SUBSTITUIERTE CYCLOALKYLDERIVATE MIT SAUREN, MEIST HETEROCYCLISCHEN GRUPPEN; VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG ALS ARZNEIMITTEL
  申请人：Sanofi-Aventis Deutschland GmbH

  公开号：EP1599203B1

  公开（公告）日：2013-10-23