1-benzyl-3-[(1,1-dimethyl-2-morpholin-4-ylethoxy)methyl]-1H-indazole maleate

• 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-3-[(1,1-dimethyl-2-morpholin-4-ylethoxy)methyl]-1H-indazole maleate
• 英文别名: 4-[2-[(1-benzylindazol-3-yl)methoxy]-2-methylpropyl]morpholine;(Z)-but-2-enedioic acid
• 化学式: (x)C₄H₄O₄*C₂₃H₂₉N₃O₂
• 分子量: 495.6
• InChiKey: VSYGRPQLVSJXFZ-BTJKTKAUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.42
• 重原子数：
  36
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  114
• 氢给体数：
  2
• 氢受体数：
  8

反应信息

• 作为产物：
  描述：

  宾达利 在 lithium aluminium tetrahydride 、 sodium methylate 作用下， 以 四氢呋喃 、 甲醇 、 乙醚 、 乙醇 为溶剂， 反应 0.17h， 生成 1-benzyl-3-[(1,1-dimethyl-2-morpholin-4-ylethoxy)methyl]-1H-indazole maleate
  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。
• 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, CXCR1 AND P40
  申请人：Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.

  公开号：EP2262778B1

  公开（公告）日：2019-08-21
• PROCESSES OF MAKING 2-((1-BENZYL-1H-INDAZOL-3-YL)METHOXY)-2-METHYLPROPANOIC ACID AND ITS DERIVATIVES
  申请人：Translatum Medicus Inc.

  公开号：EP3990433A1

  公开（公告）日：2022-05-04
• COMPOSITIONS AND METHODS FOR TREATING AND DIAGNOSING OCULAR DISORDERS
  申请人：TRANSLATUM MEDICUS, INC.

  公开号：US20180221339A1

  公开（公告）日：2018-08-09

  Disclosed herein are methods, compounds, and compositions that are useful for the diagnosis, treatment, or prevention of an ocular disorder, including in the discovery of agents that are efficacious against these disorders.