N-methoxy-N, 2-dimethyl-1H-benzo[d]imidazole-6-carboxamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• 英文名称: N-methoxy-N, 2-dimethyl-1H-benzo[d]imidazole-6-carboxamide
• 英文别名: 2-Methyl-1H-benzoimidazole-5-carboxylic acid methoxy-methyl-amide；N-methoxy-N,2-dimethyl-3H-benzimidazole-5-carboxamide
• 化学式: C₁₁H₁₃N₃O₂
• 分子量: 219.243
• InChiKey: KJSGRTWNVNJUAX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  58.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N-methoxy-N, 2-dimethyl-1H-benzo[d]imidazole-6-carboxamide 在 氢溴酸 、 溴 、 溶剂黄146 作用下， 以 四氢呋喃 为溶剂， 反应 3.5h， 生成 2-bromo-1-(2-methyl-1H-benzo[d]imidazol-6-yl)ethanone hydrobromide
  参考文献：
  名称：

  [EN] KINASE INHIBITOR COMPOUNDS AND COMPOSITIONS AND METHODS OF USE
  [FR] COMPOSÉS INHIBITEURS DE KINASE, COMPOSITIONS ET PROCÉDÉS D'UTILISATION

  摘要：

  本发明涉及具有以下结构的激酶抑制剂化合物：或其立体异构体、药用盐、氧化物或溶剂合物，其中R1、R2、X、n、R3、Y、Z、R4、R5、R6和=如本文所定义。本发明还涉及含有激酶抑制剂化合物的组合物，抑制细胞中激酶活性的方法，增加胰岛β细胞群体中细胞增殖的方法，治疗由于胰岛素分泌不足引起的病症的方法，以及治疗神经疾病的方法。

  公开号：

  WO2019100062A1
• 作为产物：
  描述：

  二甲羟胺盐酸盐 、 2-甲基-3H-苯并咪唑-5-羧酸 在 氯化亚砜 、 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 23.0h， 以24%的产率得到N-methoxy-N, 2-dimethyl-1H-benzo[d]imidazole-6-carboxamide
  参考文献：
  名称：

  [EN] KINASE INHIBITOR COMPOUNDS AND COMPOSITIONS AND METHODS OF USE
  [FR] COMPOSÉS INHIBITEURS DE KINASE, COMPOSITIONS ET PROCÉDÉS D'UTILISATION

  摘要：

  本发明涉及具有以下结构的激酶抑制剂化合物：或其立体异构体、药用盐、氧化物或溶剂合物，其中R1、R2、X、n、R3、Y、Z、R4、R5、R6和=如本文所定义。本发明还涉及含有激酶抑制剂化合物的组合物，抑制细胞中激酶活性的方法，增加胰岛β细胞群体中细胞增殖的方法，治疗由于胰岛素分泌不足引起的病症的方法，以及治疗神经疾病的方法。

  公开号：

  WO2019100062A1

文献信息

• FUSED HETEROARYL INHIBITORS OF PRO-MATRIX METALLOPROTEINASE ACTIVATION
  申请人：Leonard Kristi Anne

  公开号：US20120129872A1

  公开（公告）日：2012-05-24

  This invention relates to thiazole I and its therapeutic and prophylactic uses, wherein the variables A, Q, J, R 1 , R 3 , and R 5 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.

  该发明涉及噻唑I及其治疗和预防用途，其中变量A、Q、J、R1、R3和R5在规范中有定义。治疗和/或预防的疾病包括类风湿性关节炎。
• KINASE INHIBITOR COMPOUNDS AND COMPOSITIONS AND METHODS OF USE
  申请人：ICHAN SCHOOL OF MEDICINE AT MOUNT SINAI

  公开号：US20200306257A1

  公开（公告）日：2020-10-01

  The present invention is directed to kinase inhibitor compounds having the following structure: or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof, where R 1 , R 2 , X, n, R 3 , Y, Z, R 4 , R 5 , R 6 , and = are as defined herein. The present invention also relates to compositions containing the kinase inhibitor compounds, methods of inhibiting activity of a kinase in a cell, methods of increasing cell proliferation in a population of pancreatic beta cells, methods of treating a subject for a condition associated with insufficient insulin secretion, and methods of treating a subject for a neurological disorder.
• METHOD OF INCREASING PROLIFERATION OF PANCREATIC BETA CELLS, TREATMENT METHOD, AND COMPOSITION
  申请人：ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI

  公开号：US20210032601A1

  公开（公告）日：2021-02-04

  Disclosed herein are methods of increasing cell proliferation in a population of pancreatic beta cells. Also disclosed are methods of treating a subject for a condition associated with insufficient insulin secretion. Also disclosed is a composition comprising a DYRK1 A inhibitor and a GLP1R agonist. The disclosure further describes a method of regenerating pancreatic beta cells in a transplant patient.
• [EN] FUSED HETEROARYL INHIBITORS OF PRO-MATRIX METALLOPROTEINASE ACTIVATION<br/>[FR] INHIBITEURS HÉTÉROARYLE CONDENSÉ D'ACTIVATION DES MÉTALLOPROTÉINASES PRO-MATRICIELLES
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2012068204A1

  公开（公告）日：2012-05-24

  This invention relates to thiazole I and its therapeutic and prophylactic uses, wherein the variables A, Q, J, R1, R3, and R5 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.
• [EN] METHOD OF INCREASING PROLIFERATION OF PANCREATIC BETA CELLS, TREATMENT METHOD, AND COMPOSITION<br/>[FR] PROCÉDÉ D'AUGMENTATION DE LA PROLIFÉRATION DE CELLULES BÊTA PANCRÉATIQUES, PROCÉDÉ DE TRAITEMENT ET COMPOSITION
  申请人：ICAHN SCHOOL MED MOUNT SINAI

  公开号：WO2019136320A1

  公开（公告）日：2019-07-11

  Disclosed herein are methods of increasing cell proliferation in a population of pancreatic beta cells. Also disclosed are methods of treating a subject for a condition associated with insufficient insulin secretion. Also disclosed is a composition comprising a DYRK1 A inhibitor and a GLP1R agonist. The disclosure further describes a method of regenerating pancreatic beta cells in a transplant patient.