8-(2-Ethyl-6-methylbenzylamino)-2,3-dimethylimidazo[1,2-a]pyridine-6-carboxamide mesylate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡啶类
• 英文名称: 8-(2-Ethyl-6-methylbenzylamino)-2,3-dimethylimidazo[1,2-a]pyridine-6-carboxamide mesylate
• 英文别名: 8-[(2-ethyl-6-methylphenyl)methylamino]-2,3-dimethylimidazo[1,2-a]pyridine-6-carboxamide;methanesulfonic acid
• 化学式: C21H28N4O4S
• 分子量: 432.5
• InChiKey: YZHMZULORBVRSC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.04
• 重原子数：
  30
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  135
• 氢给体数：
  3
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  8-(2-Ethyl-6-methylbenzylamino)-2,3-dimethylimidazo[1,2-a]pyridine-6-carboxamide mesylate 、 sodium hydroxide 在 水 、 盐酸 、 溶剂黄146 作用下， 以 乙醇 为溶剂， 反应 20.0h， 以to give 7.6 g (88%) of the title compound的产率得到2,3-dimethyl-8-(2-ethyl-6-methylbenzylamino)-imidazo[1,2-a]pyridine-6-carboxylic acid
  参考文献：
  名称：

  Process for preparing a substituted imidazopyridine compound

  摘要：

  本发明提供了一种新的大规模制备式（1）中取代咪唑吡啶化合物的过程，其中R1是C1-C6烷氧基或NH2基团，包括将式（2）化合物与3-卤代-2-丁酮化合物在环已酮中反应的步骤。

  公开号：

  US20040039013A1

文献信息

• Process for preparing a substituted imidazopyridine compound
  申请人：——

  公开号：US20040039013A1

  公开（公告）日：2004-02-26

  The present invention provides a new process for large-scale preparation of substituted imidazopyridine compound of formula (1) wherein R 1 is C 1 -C 6 alkoxy or NH 2 group, comprising the step of reacting a compound of formula (2) with a 3-halo-2-butanone compound in cyclohexanone.

  本发明提供了一种新的大规模制备配体式为(1)的取代咪唑吡啶化合物的工艺，其中R1是C1-C6烷氧基或NH2基团，包括将式(2)的化合物与3-卤代-2-丁酮在环己酮中反应的步骤。
• [EN] PROCESS FOR PREPARING A SUBSTITUTED IMIDAZOPYRIDINE COMPOUND<br/>[FR] PROCEDE DE PREPARATION D'UN COMPOSE D'IMIDAZOPYRIDINE SUBSTITUE
  申请人：ASTRAZENECA AB

  公开号：WO2002020523A1

  公开（公告）日：2002-03-14

  The present invention provides a new process for large-scale preparation of substituted imidazopyridine compound of formula (I) wherein R1 is C1-C6 alkoxy or NH2 group, comprising the step of reacting a compound of formula (2) with a 3-halo-2-butanone compound in cyclohexanone.

  本发明提供了一种用于大规模制备式（I）的取代咪唑吡啶化合物的新工艺，其中R1是C1-C6烷氧基或NH2基的化合物，包括将式（2）的化合物与3-卤代-2-丁酮化合物在环已酮中反应的步骤。
• Imidazo pyridine derivatives which inhibit gastric acid secretion
  申请人：AstraZeneca AB

  公开号：US06313136B1

  公开（公告）日：2001-11-06

  The present invention relates to imidazo pyridine derivatives of the formula (I), in which the phenyl moiety is substituted, and in which the imidazo pyridine moiety is substituted with a carboxamide group in 6-position, which inhibit exogenously or endogenously stimulated gastric acid secretion and thus can be used in the prevention and treatment of gastrointestinal inflammatory diseases.

  本发明涉及公式(I)的咪唑吡啶衍生物，其中苯基取代，咪唑吡啶基团在6位取代羧酰胺基团，能够抑制外源性或内源性刺激的胃酸分泌，因此可用于预防和治疗胃肠道炎症性疾病。
• Novel modified release formulation
  申请人：——

  公开号：US20040067252A1

  公开（公告）日：2004-04-08

  The present invention is directed to a multiparticulate, modified release solid dispersion formulation, comprising a drug substance having a pH-dependent solubility, said drug substance being a compound of the formula I, or a pharmaceutically acceptable salt thereof; a hydrophobic matrix former which is a water-insoluble, non-swelling amphiphilic lipid; and a hydrophilic matrix former which is a meltable, water-soluble excipient; wherein the weight ratio hydrophobic matrix former/hydrophilic matrix former is ≧1; and the particle size is less than 300 &mgr;m. Also a unit dosage of the same, as well as a process for the preparation thereof and the use of the formulation and unit dosage is claimed.

  本发明涉及一种多颗粒、改进释放型固体分散制剂，包括一种溶解度取决于 pH 值的药物，所述药物为式 I 的化合物或其药学上可接受的盐； 疏水基质前体，它是一种不溶于水、无溶胀性的两性脂质；以及亲水基质前体，它是一种可熔化的水溶性赋形剂；其中疏水基质前体/亲水基质前体的重量比为≧1;，粒度小于300&mgr;m。 此外，还要求得到一种相同的单位剂量及其制备工艺，以及该制剂和单位剂量的使用方法。
• IMIDAZO PYRIDINE DERIVATIVES WHICH INHIBIT GASTRIC ACID SECRETION
  申请人：AstraZeneca AB

  公开号：EP1073656B1

  公开（公告）日：2005-10-19