1-benzyl-5-methoxy-1H-indazol-3-yl-methanol | 1186507-40-3

• 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: 1-benzyl-5-methoxy-1H-indazol-3-yl-methanol
• 英文别名: (1-benzyl-5-methoxy-1H-indazol-3-yl)methanol；(1-benzyl-5-methoxyindazol-3-yl)methanol
• CAS: 1186507-40-3
• 化学式: C₁₆H₁₆N₂O₂
• 分子量: 268.315
• InChiKey: LGIQKIRJXXPXTN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  20
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  47.3
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-benzyl-5-methoxy-1H-indazol-3-yl-methanol 在 氯化亚砜 作用下， 以 氯仿 为溶剂， 生成 1-benzyl-3-(chloromethyl)-5-methoxy-1H-indazole
  参考文献：
  名称：

  [EN] 1-BENZYL-3-HYDROXYMETHYLINDAZOI?E DERIVATIVES AND USE THEREOF IN THE TREATMENT OF DISEASES BASED ON THE EXPRESSION OF MCP-1, CX3CR1
  [FR] NOUVEAUX DÉRIVÉS DE 1-BENZYL-3-HYDROXYMÉTHYLINDAZOLE ET LEUR UTILISATION DANS LE TRAITEMENT DES MALADIES BASÉES SUR L'EXPRESSION DE MCP-1, CX3CR1 ET P40

  摘要：

  公开号：

  WO2009109613A3
• 作为产物：
  描述：

  5-甲氧基-3-吲唑羧酸 在 lithium aluminium tetrahydride 、 sodium hydride 作用下， 以 四氢呋喃 、 乙醚 、 N,N-二甲基甲酰胺 为溶剂， 反应 5.0h， 生成 1-benzyl-5-methoxy-1H-indazol-3-yl-methanol
  参考文献：
  名称：

  [EN] 1-BENZYL-3-HYDROXYMETHYLINDAZOLE DERIVATIVES AND USE THEREOF IN THE TREATMENT OF DISEASES BASED ON THE EXPRESSION OF MCP-1, CX3CR1 AND P40
  [FR] NOUVEAUX DÉRIVÉS DE 1-BENZYL-3-HYDROXYMÉTHYLINDAZOLE ET LEUR UTILISATION DANS LE TRAITEMENT DES MALADIES BASÉES SUR L'EXPRESSION DE MCP-1, CX3CR1 ET P40

  摘要：

  公开号：

  WO2009109616A8

文献信息

• [EN] PROCESSES OF MAKING 2-((1-BENZYL-1H-INDAZOL-3-YL)METHOXY)-2-METHYLPROPANOIC ACID AND ITS DERIVATIVES<br/>[FR] PROCÉDÉS DE FABRICATION D'ACIDE 2-((1-BENZYL-1H-INDAZOL-3-YL)MÉTHOXY)-2-MÉTHYLPROPANOÏQUE ET DE SES DÉRIVÉS
  申请人：TRANSLATUM MEDICUS INC

  公开号：WO2020261158A1

  公开（公告）日：2020-12-30

  The invention in this disclosure is related to the processes of making Bindarit or derivatives thereof. Specifically, the present invention provides, in part, new processes for making 2-((1-benzyl-1H-indazol-3-yl)methoxy)-2-methylpropanoic acid and its derivatives. By way of non-limiting example, synthesis and purification processes of 2-((1-benzyl-1H-indazol-3-yl)methoxy)-2-methylpropanoic acid are provided by the invention in this disclosure.

  本公开的发明涉及制备Bindarit或其衍生物的过程。具体来说，本发明部分提供了制备2-((1-苄基-1H-吲哚-3-基)甲氧基)-2-甲基丙酸及其衍生物的新工艺。举例而言，本公开的发明提供了2-((1-苄基-1H-吲哚-3-基)甲氧基)-2-甲基丙酸的合成和纯化过程。
• NOVEL 1-BENZYL-3-HYDROXYMETHYLINDAZOLE DERIVATIVES AND USE THEREOF IN THE TREATMENT OF DISEASES BASED ON THE EXPRESSION OF MCP-1, CX3CR1 AND P40
  申请人：GUGLIELMOTTI Angelo

  公开号：US20110160205A1

  公开（公告）日：2011-06-30

  The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40, and to their use in a method for treating or preventing diseases based on the expression of MCP-1, CX3CR1 and p40.

  本发明涉及一种新颖的1-苄基-3-羟甲基吲唑衍生物，其结构式（I）如权利要求书所述，并且涉及包含它们的制药组合物，以及与药学上可接受的载体一起使用。此外，本发明还涉及1-苄基-3-羟甲基吲唑衍生物的使用，用于制备在基于MCP-1、CX3CR1和p40的表达的疾病治疗中具有活性的制药组合物，并且用于治疗或预防基于MCP-1、CX3CR1和p40的表达的疾病的方法。
• 1-BENZYL-3-HYDROXYMETHYLINDAZOLE DERIVATIVES AND USE THEREOF IN THE TREATMENT OF DISEASES BASED ON THE EXPRESSION OF MCP-1, CX3CR1 AND P40
  申请人：Guglielmotti Angelo

  公开号：US20110082141A1

  公开（公告）日：2011-04-07

  The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to Formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40, and to their use in a method for treating or preventing diseases based on the expression of MCP-1, CX3CR1 and p40.

  本发明涉及根据权利要求中所述的式(I)所描述的新型1-苄基-3-羟甲基吲唑衍生物，以及包含它们的制药组合物和与药学上可接受的载体一起使用。此外，本发明还涉及使用1-苄基-3-羟甲基吲唑衍生物制备活性用于治疗基于MCP-1、CX3CR1和p40表达的疾病的制药组合物，并将其用于治疗或预防基于MCP-1、CX3CR1和p40表达的疾病的方法。
• 1-benzyl-3-hydroxymethylindazole derivatives and use thereof in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40
  申请人：Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.

  公开号：US08283348B2

  公开（公告）日：2012-10-09

  The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40, and to their use in a method for treating or preventing diseases based on the expression of MCP-1, CX3CR1 and p40.

  本发明涉及一种新型的1-苄基-3-羟甲基吲唑衍生物，其公式如（I）所述，并且涉及包含它们的制药组合物，以及与药学上可接受的载体一起使用。此外，本发明还涉及使用1-苄基-3-羟甲基吲唑衍生物制备具有活性的制药组合物，用于治疗基于MCP-1、CX3CR1和p40表达的疾病，并且涉及将它们用于治疗或预防基于MCP-1、CX3CR1和p40表达的疾病的方法。
• 1-benzyl-3-hydroxymethylindazole derivatives and use thereof in the treatment of diseases based on the expression of MCP-1, CX3CR1 and P40
  申请人：Guglielmotti Angelo

  公开号：US08835481B2

  公开（公告）日：2014-09-16

  The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to Formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40, and to their use in a method for treating or preventing diseases based on the expression of MCP-1, CX3CR1 and p40.

  本发明涉及一种新型1-苄基-3-羟甲基吲唑衍生物，其符合权利要求书中所述的公式（I），以及包含它们的制药组合物和与其一起使用的药用载体。此外，本发明还涉及使用1-苄基-3-羟甲基吲唑衍生物制备对基于MCP-1、CX3CR1和p40表达的疾病具有活性的制药组合物，并将其用于治疗或预防基于MCP-1、CX3CR1和p40表达的疾病的方法。