4-(trifluoromethyl)-1H-indazol-3-amine | 60330-34-9

• 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: 4-(trifluoromethyl)-1H-indazol-3-amine
• CAS: 60330-34-9
• 化学式: C₈H₆F₃N₃
• 分子量: 201.151
• InChiKey: HVSPPLIBICHWSB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  54.7
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  4-(trifluoromethyl)-1H-indazol-3-amine 以 焦碳酸二乙酯 为溶剂， 生成 3-amino-4-trifluoromethyl-indazole-1-carboxylic acid ethyl ester
  参考文献：
  名称：

  3-Aminoindazole-1 and 2-carboxylic acid derivatives

  摘要：

  1-或2-位上带有羧基（较低的烷氧基）、较低的烷基酰胺或二（较低烷基）酰胺基团的3-氨基吲唑，可选地在4、5、6和/或7位上进一步取代，具有镇痛、抗炎和退热作用。这些化合物，其中3-氨基-6-氯吲唑-1-羧酸乙酯是典型的实施例，通过将适当的3-氨基吲唑与碳酸衍生物处理或通过热异构化制备。

  公开号：

  US04051252A1
• 作为产物：
  描述：

  3-amino-4-trifluoromethyl-indazole-1-carboxylic acid ethyl ester 以 焦碳酸二乙酯 为溶剂， 反应 2.0h， 以Analogously to Example 21, 0.06 mol of 3-amino-4-trifluoromethylindazole in 50 ml of pyrocarbonic acid diethyl ester gives 3-amino-4-trifluoromethylindazole-1-carboxylic acid ethyl ester (melting point: 185°-186° C; 68% of theory) in 2 hours at 75° C.的产率得到4-(trifluoromethyl)-1H-indazol-3-amine
  参考文献：
  名称：

  3-Aminoindazole-1 and 2-carboxylic acid derivatives

  摘要：

  1-或2-位上带有碳酸(lower alkoxy)，低烷基酰胺或二(lower alkyl)酰胺基团，并且在4-、5-、6-和/或7-位上可以选择性地取代的3-氨基吲唑是镇痛、抗炎和退热剂。这些化合物，其中3-氨基-6-氯吲唑-1-羧酸乙酯是一个典型的实施例，是通过用碳酸衍生物或热异构化处理适当的3-氨基吲唑制备的。

  公开号：

  US04051252A1

文献信息

• [EN] (AZA)PYRIDOPYRAZOLOPYRIMIDINONES AND INDAZOLOPYRIMIDINONES AS INHIBITORS OF FIBRINOLYSIS<br/>[FR] (AZA)PYRIDOPYRAZOLOPYRIMIDINONES ET INDAZOLOPYRIMIDINONES UTILISÉES COMME INHIBITEURS DE LA FIBRINOLYSE
  申请人：BAYER PHARMA AG

  公开号：WO2015067549A1

  公开（公告）日：2015-05-14

  The present application relates to novel substituted (aza)pyridopyrazolopyrimidinones and indazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired bleeding disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of menorrhagia, postpartum hemorrhage, hemorrhagic shock, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.

  本申请涉及新型取代的(氮杂)吡啶吡唑吡嘧啶酮和吲唑吡嘧啶酮，以及它们的制备方法，这些化合物可单独或组合使用于治疗和/或预防疾病的方法中，特别是用于治疗和/或预防患有或不患有基础遗传或获得性出血性疾病的患者的急性和复发性出血，其中出血与来自以下组中选择的疾病或医疗干预相关，该组包括月经过多、产后出血、出血性休克、创伤、手术、移植、中风、肝病、遗传性血管性水肿、鼻血、以及血液积聚后的滑膜炎和软骨损伤。
• (Aza)pyridopyrazolopyrimidinones and indazolopyrimidinones and their use
  申请人：BAYER PHARMA AKTIENGESELLSCHAFT

  公开号：US20150126449A1

  公开（公告）日：2015-05-07

  The present application relates to novel substituted (aza)pyridopyrazolopyrimidinones and indazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired bleeding disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of menorrhagia, postpartum hemorrhage, hemorrhagic shock, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.

  本申请涉及新型取代的(氮杂)吡啶吡唑吡嘧啶酮和吲唑吡嘧啶酮，以及它们的制备方法，这些化合物可单独或组合使用于治疗和/或预防疾病的方法中，特别是用于治疗和/或预防患有或不患有基础遗传或获得性出血性疾病的患者的急性和复发性出血，其中出血与来自月经过多、产后出血、出血性休克、创伤、手术、移植、中风、肝病、遗传性血管性水肿、鼻血和血液性关节积血后的滑膜炎和软骨损伤等疾病或医疗干预有关。
• GLUCOKINASE ACTIVATORS
  申请人：Feng Jun

  公开号：US20070244169A1

  公开（公告）日：2007-10-18

  Compounds, pharmaceutical compositions, kits and methods are provided for use with glucokinase that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.

  本发明提供了用于与葡萄糖激酶一起使用的化合物、制药组合物、试剂盒和方法，其中包括所述化合物中选自以下组的化合物：其中所述变量如本文所定义。
• (AZA)PYRIDOPYRAZOLOPYRIMIDINONES AND INDAZOLOPYRIMIDINONES AS INHIBITORS OF FIBRINOLYSIS
  申请人：Bayer Pharma Aktiengesellschaft

  公开号：EP3066100B1

  公开（公告）日：2019-04-17
• (AZA)PYRIDOPYRAZOLOPYRIMIDINONES AND INDAZOLOPYRIMIDINONES AND THEIR USE
  申请人：BAYER PHARMA AKTIENGESELLSCHAFT

  公开号：US20170239251A1

  公开（公告）日：2017-08-24

  The present application relates to novel substituted (aza)pyridopyrazolopyrimidinones and indazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired bleeding disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of menorrhagia, postpartum hemorrhage, hemorrhagic shock, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.