5-pyrrol-1-yl-1H-[1,2,4]triazole-3-carboxylic acid | 383142-90-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯
• 英文名称: 5-pyrrol-1-yl-1H-[1,2,4]triazole-3-carboxylic acid
• 英文别名: 5-(1H-pyrrol-1-yl)-4H-1,2,4-triazole-3-carboxylic acid；3-pyrrol-1-yl-1H-1,2,4-triazole-5-carboxylic acid
• CAS: 383142-90-3
• 化学式: C₇H₆N₄O₂
• mdl: MFCD04967082
• 分子量: 178.15
• InChiKey: XIKZTCXYFVSBJT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  83.8
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  4-氨基-1-异丙基哌啶 、 5-pyrrol-1-yl-1H-[1,2,4]triazole-3-carboxylic acid 在 双(2-氧代-3-恶唑烷基)次磷酰氯 、 三乙胺 作用下， 以 DMF (N,N-dimethyl-formamide) 为溶剂， 反应 16.0h， 生成 5-Pyrrol-1-yl-1H-[1,2,4]triazole-3-carboxylic acid (1-isopropyl-piperidin-4-yl)-amide
  参考文献：
  名称：

  Triazole-derivatives as factor Xa inhibitors

  摘要：

  本发明涉及具有式I和II的化合物，其中R0; R1; R2; R3; Q; J1; J2; J3; J4; J5; V; G和M具有索权要求中所指示的含义。具有式I和II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。它们是血凝酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，通常可应用于因子Xa和/或因子VIIa的不良活性存在或需要抑制因子Xa和/或因子VIIa的治疗或预防的情况。此外，本发明还涉及制备具有式I和II的化合物的方法，它们的使用，特别是作为药物中的活性成分，以及包含它们的制剂。

  公开号：

  EP1479679A1

文献信息

• Imidazo 4,5-C Pyridine Compounds and Methods of Antiviral Treatment
  申请人：Bondy S. Steven

  公开号：US20070244148A1

  公开（公告）日：2007-10-18

  The present invention relates to a pharmaceutical composition for the treatment or prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyridine prodrug having the general formula (Z): The invention also relates to processes for the preparation of compounds according to the invention having above mentioned general formula and their use as a medicine or to treat or prevent viral infections.

  本发明涉及一种用于治疗或预防病毒感染的药物组合物，其包含至少一种具有以下通式（Z）的咪唑[4,5-c]吡啶前药作为活性成分：本发明还涉及制备符合上述通式的化合物的方法以及它们作为药物或用于治疗或预防病毒感染的用途。
• IMIDAZO[4,5-c]PYRIDINE COMPOUNDS AND METHODS OF ANTIVIRAL TREATMENT
  申请人：Bondy Steven S.

  公开号：US20100028301A1

  公开（公告）日：2010-02-04

  The present invention relates to pharmaceutical compositions for the treatment or prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyridine prodrug having the general Formula (A) wherein the substituents are described in the specification. The invention also relates to processes for the preparation and screening of compounds according to the invention having above mentioned general Formula and their use in the treatment or prophylaxis of viral infections.

  本发明涉及一种制备用于治疗或预防病毒感染的药物组合物，其包含至少一种咪唑并[4,5-c]吡啶前药作为活性成分，其通式为（A），其中取代基在规范中描述。该发明还涉及根据上述通式制备和筛选化合物的方法以及它们在治疗或预防病毒感染中的应用。
• Triazole-derivatives as blood clotting enzyme factor Xa inhibitors
  申请人：Sanofi-Aventis Deutschland GmbH

  公开号：US07223780B2

  公开（公告）日：2007-05-29

  The present invention is directed to the compound of formula I which is useful for inhibiting the activity of blood clotting enzyme Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as for inhibiting the formation of thrombin or for therapeutically treating a patient suffering from, or subject to, a disease state associated with a cardiovascular disorder.

  本发明涉及化合物I的使用，该化合物对于抑制血凝酶酶因子Xa的活性是有用的。本发明还涉及含有该化合物的组合物、其制备过程以及它们的用途，例如用于抑制凝血酶的形成或治疗患有与心血管疾病相关的疾病状态的患者。
• Imidazo[4,5-d]pyrimidines, their uses and methods of preparation
  申请人：Puerstinger Gerhard

  公开号：US20090208456A1

  公开（公告）日：2009-08-20

  The present invention relates to pharmaceutical compositions for the treatment of prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyrimidine having the general formula (A), wherein the substituents are described in the specification. The invention also relates to processes for the preparation of compounds according to the invention having above mentioned general formula, their pharmaceutically acceptable formulations and their use as a medicine or to treat or prevent viral infections.

  本发明涉及制备用于治疗或预防病毒感染的药物组合物，其中至少包括一种具有通式（A）的咪唑并[4,5-c]嘧啶类活性成分，其中取代基如规范所述。本发明还涉及制备符合上述通式的化合物的过程，其药学上可接受的配方以及它们作为药物或用于治疗或预防病毒感染的用途。
• TRIAZOLE-DERIVATIVES AS FACTOR Xa INHIBITORS
  申请人：Sanofi-Aventis Deutschland GmbH

  公开号：EP1628971A1

  公开（公告）日：2006-03-01